L-glutamic acid [Ligand Id: 1369] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL575060 (Acide glutamique, Acido glutamico, E 620, E-620, E620, FEMA NO. 3285, Glutamic acid, Glutamic acid, l-, Glutamidex, INS-620, INS NO.620, L-2-amino-pentanedioic acid, L-alpha-aminoglutaric acid, L-glutamate, L-glutamic acid, NSC-143503) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Excitatory amino acid transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3085] [GtoPdb: 868] [UniProtKB: P43003] | ||||||||
| ChEMBL | Inhibition of [3H]D-Asp uptake at EAAT1 in HEK293 cells | B | 4.46 | pKi | 35000 | nM | Ki | J Med Chem (2008) 51: 4085-4092 [PMID:18578477] |
| ChEMBL | Inhibition of [3H]D-Asp uptake at EAAT1 in HEK293 cells | B | 4.5 | pKi | 31622.78 | nM | Ki | J Med Chem (2008) 51: 4085-4092 [PMID:18578477] |
| ChEMBL | Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method | B | 4.94 | pIC50 | 11481.54 | nM | IC50 | J Med Chem (2018) 61: 7741-7753 [PMID:30011368] |
| ChEMBL | Inhibition of human EAAT1 transfected in HEK293 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 4 mins by TopCount scintillation counting analysis | B | 4.95 | pIC50 | 11220.18 | nM | IC50 | ACS Med Chem Lett (2020) 11: 2212-2220 [PMID:33214831] |
| ChEMBL | Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method | B | 4.96 | pIC50 | 11000 | nM | IC50 | J Med Chem (2018) 61: 7741-7753 [PMID:30011368] |
| ChEMBL | Inhibition of human EAAT1 transfected in HEK293 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 4 mins by TopCount scintillation counting analysis | B | 4.96 | pIC50 | 11000 | nM | IC50 | ACS Med Chem Lett (2020) 11: 2212-2220 [PMID:33214831] |
| ChEMBL | Substrate uptake by the Excitatory Amino Acid Transporter 1 (EAAT1, SLC1A3) as assessed by the fluorescent FLIPR membrane potential dye in HEK-293 JumpIN-SLC1A3 cells (PubChem AID: 1745864) | F | 4.8 | pEC50 | 16000 | nM | EC50 | Membrane potential based transport assay for SLC1A3 using HEK293 JumpIn SLC1A3 OE cells |
| Excitatory amino acid transporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4973] [GtoPdb: 869] [UniProtKB: P43004] | ||||||||
| ChEMBL | Inhibition of [3H]D-Asp uptake at human EAAT2 in HEK293 cells | B | 4.2 | pKi | 63095.73 | nM | Ki | J Med Chem (2008) 51: 4085-4092 [PMID:18578477] |
| ChEMBL | Inhibition of [3H]D-Asp uptake at human EAAT2 in HEK293 cells | B | 4.21 | pKi | 62000 | nM | Ki | J Med Chem (2008) 51: 4085-4092 [PMID:18578477] |
| ChEMBL | Inhibition of human EAAT2 transfected in HEK293 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 4 mins by TopCount scintillation counting analysis | B | 4.1 | pIC50 | 80000 | nM | IC50 | ACS Med Chem Lett (2020) 11: 2212-2220 [PMID:33214831] |
| ChEMBL | Inhibition of human EAAT2 transfected in HEK293 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 4 mins by TopCount scintillation counting analysis | B | 4.1 | pIC50 | 79432.82 | nM | IC50 | ACS Med Chem Lett (2020) 11: 2212-2220 [PMID:33214831] |
| ChEMBL | Inhibition of human EAAT2 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method | B | 4.28 | pIC50 | 52480.75 | nM | IC50 | J Med Chem (2018) 61: 7741-7753 [PMID:30011368] |
| ChEMBL | Inhibition of human EAAT2 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method | B | 4.28 | pIC50 | 52000 | nM | IC50 | J Med Chem (2018) 61: 7741-7753 [PMID:30011368] |
| Excitatory amino acid transporter 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2721] [GtoPdb: 870] [UniProtKB: P43005] | ||||||||
| ChEMBL | Inhibition of [3H]D-Asp uptake at human EAAT3 in HEK293 cells | B | 4.3 | pKi | 50118.72 | nM | Ki | J Med Chem (2008) 51: 4085-4092 [PMID:18578477] |
| ChEMBL | Inhibition of [3H]D-Asp uptake at human EAAT3 in HEK293 cells | B | 7.29 | pKi | 51 | nM | Ki | J Med Chem (2008) 51: 4085-4092 [PMID:18578477] |
| ChEMBL | Inhibition of human EAAT3 transfected in HEK293 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 4 mins by TopCount scintillation counting analysis | B | 4.3 | pIC50 | 50118.72 | nM | IC50 | ACS Med Chem Lett (2020) 11: 2212-2220 [PMID:33214831] |
| ChEMBL | Inhibition of human EAAT3 transfected in HEK293 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 4 mins by TopCount scintillation counting analysis | B | 4.3 | pIC50 | 50000 | nM | IC50 | ACS Med Chem Lett (2020) 11: 2212-2220 [PMID:33214831] |
| ChEMBL | Inhibition of human EAAT3 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method | B | 4.49 | pIC50 | 32359.37 | nM | IC50 | J Med Chem (2018) 61: 7741-7753 [PMID:30011368] |
| ChEMBL | Inhibition of human EAAT3 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method | B | 4.49 | pIC50 | 32000 | nM | IC50 | J Med Chem (2018) 61: 7741-7753 [PMID:30011368] |
| Excitatory amino acid transporter 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3700] [GtoPdb: 871] [UniProtKB: O35921] | ||||||||
| ChEMBL | Inhibition of rat EAAT4 expressed in tsA201 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method | B | 4.88 | pIC50 | 13182.57 | nM | IC50 | J Med Chem (2018) 61: 7741-7753 [PMID:30011368] |
| ChEMBL | Inhibition of rat EAAT4 expressed in tsA201 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method | B | 4.89 | pIC50 | 13000 | nM | IC50 | J Med Chem (2018) 61: 7741-7753 [PMID:30011368] |
| ChEMBL | Inhibition of rat EAAT4 transfected in human tsA201 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 4 mins by TopCount scintillation counting analysis | B | 4.9 | pIC50 | 12589.25 | nM | IC50 | ACS Med Chem Lett (2020) 11: 2212-2220 [PMID:33214831] |
| ChEMBL | Inhibition of rat EAAT4 transfected in human tsA201 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 4 mins by TopCount scintillation counting analysis | B | 4.92 | pIC50 | 12000 | nM | IC50 | ACS Med Chem Lett (2020) 11: 2212-2220 [PMID:33214831] |
| GluN2D/GluN3B/GluN1/GluN2A/GluN2B/GluN2C/GluN3A/Glutamate [NMDA] receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094124] [GtoPdb: 459, 461, 455, 456, 457, 458, 460] [UniProtKB: O15399, O60391, Q05586, Q12879, Q13224, Q14957, Q8TCU5] | ||||||||
| ChEMBL | Antagonist activity at NMDA receptor (unknwon origin) | F | 7.15 | pIC50 | 70 | nM | IC50 | J Med Chem (2011) 54: 2529-2591 [PMID:21413808] |
| ChEMBL | Binding affinity to NMDA receptor (unknown origin) | B | 7.15 | pIC50 | 70 | nM | IC50 | Eur J Med Chem (2021) 209: 112872-112872 [PMID:33035923] |
| 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 | Displacement of L-[3H]glutamate from N-methyl-D-aspartate glutamate receptor in rat brain synaptic membranes | B | 6.06 | pKi | 870 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 2279-2283 [PMID:15837309] |
| ChEMBL | Displacement of [3H]CGP 39653 from NMDA receptor agonist binding site in Wistar rat cerebral cortex after 20 mins | B | 6.43 | pKi | 370 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
| ChEMBL | Displacement of [3H]CGP39653 from NMDA receptor in rat brain membranes | B | 6.54 | pKi | 290 | nM | Ki | Bioorg Med Chem (2009) 17: 242-250 [PMID:19042134] |
| ChEMBL | Displacement of [3H]CGP39653 from NMDA receptor in Sprague-Dawley rat brain membranes | B | 6.7 | pKi | 200 | nM | Ki | J Med Chem (2010) 53: 4110-4118 [PMID:20408529] |
| ChEMBL | Displacement of [3H]CGP39653 from NMDA receptor in rat brain cortex after 60 mins by Packard TopCount microplate scintillator counting | B | 6.7 | pKi | 200 | nM | Ki | J Med Chem (2013) 56: 1614-1628 [PMID:23414088] |
| ChEMBL | Displacement of [3H]CGP-39653 from NMDA receptor in rat brain cortical membranes | B | 6.7 | pKi | 200 | nM | Ki | Medchemcomm (2011) 2: 1120-1124 |
| ChEMBL | Displacement of [3H]CGP39653 from NMDA receptor in rat cortical synaptosomes | B | 6.7 | pKi | 200 | nM | Ki | Medchemcomm (2015) 6: 1285-1292 |
| ChEMBL | Binding affinity towards NMDA receptor by displacement of [3H]CGP-39653 radioligand. | B | 6.7 | pKi | 200 | nM | Ki | J Med Chem (2001) 44: 2507-2510 [PMID:11472204] |
| ChEMBL | Displacement of [3H]CGP39653 from NMDA receptor in rat brain synaptic cortical membranes after 60 mins by scintillation counting method | B | 6.7 | pKi | 200 | nM | Ki | J Med Chem (2019) 62: 4467-4482 [PMID:30943028] |
| ChEMBL | Displacement of [3H]CGP-39653 from rat NMDA receptor expressed in BHK cells | B | 6.7 | pKi | 200 | nM | Ki | J Med Chem (2007) 50: 4630-4641 [PMID:17725337] |
| ChEMBL | Displacement of [3H]CGP39653 from NMDA receptor in rat cortical synaptosome | B | 6.7 | pKi | 200 | nM | Ki | J Med Chem (2008) 51: 4179-4187 [PMID:18578474] |
| ChEMBL | Displacement of [3H]CPP from N-methyl-D-aspartate glutamate receptor in rat brain membrane | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (1992) 35: 1345-1370 [PMID:1533422] |
| ChEMBL | Displacement of [3H]CGP 39653 from NMDA receptor agonist binding site in Wistar rat cerebral cortex after 20 mins | B | 6.39 | pIC50 | 410 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
| ChEMBL | Displacement of [3H]CPP from rat brain cortical membranes NMDA receptor incubated for 30 mins by equilibrium binding assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Nat Prod (2020) 83: 3156-3165 [PMID:33030894] |
| ChEMBL | Compound was evaluated for the inhibition of [3H]-CGS-19,755 binding at N-methyl-D-aspartate glutamate receptor | B | 6.76 | pIC50 | 172 | nM | IC50 | J Med Chem (1992) 35: 4608-4612 [PMID:1361579] |
| ChEMBL | Inhibition of N-methyl-D-aspartate glutamate receptor by using [3H]CPP as a radioligand from the rat cortical membranes. | B | 6.77 | pIC50 | 171 | nM | IC50 | J Med Chem (1990) 33: 2916-2924 [PMID:2145436] |
| ChEMBL | Compound was evaluated for the inhibition of [3H]CGS-19,755 binding to NMDA receptor from rat brain synaptic membrane. | B | 7.1 | pIC50 | 80 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 2381-2386 |
| ChEMBL | Inhibition of [3H]CPP binding to rat N-methyl-D-aspartate glutamate receptor | B | 7.15 | pIC50 | 70 | nM | IC50 | J Med Chem (1992) 35: 4720-4726 [PMID:1361582] |
| ChEMBL | Displacement of [3H]CGP39653 from NMDA receptor in Sprague-Dawley rat brain membrane | B | 7.16 | pIC50 | 69 | nM | IC50 | J Nat Prod (2003) 66: 784-787 [PMID:12828462] |
| ChEMBL | Compound was evaluated for the inhibition of [3H]MK-801 binding at N-methyl-D-aspartate glutamate receptor | B | 6.92 | pEC50 | 120 | nM | EC50 | J Med Chem (1992) 35: 4608-4612 [PMID:1361579] |
| GluN1/GluN2A/Glutamate NMDA receptor; Grin1/Grin2a in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096680] [GtoPdb: 455, 456] [UniProtKB: P35439, Q00959] | ||||||||
| ChEMBL | Activity at rat recombinant NR1/NR2A receptor expressed in Xenopus oocytes assessed as effect on glutamate-induced current by two voltage clamp electrophysiology | B | 5.54 | pEC50 | 2900 | nM | EC50 | J Med Chem (2008) 51: 4179-4187 [PMID:18578474] |
| ChEMBL | Agonist activity at rat NR1/NR2A receptor expressed in BHK21 cells assessed as change in intracellular calcium levels by FLIPR assay | F | 5.74 | pEC50 | 1800 | nM | EC50 | J Med Chem (2010) 53: 4110-4118 [PMID:20408529] |
| ChEMBL | Agonist activity at rat NR1/NR2A receptor expressed in BHK21 cells assessed as change in intracellular calcium levels by FLIPR assay | F | 5.75 | pEC50 | 1778.28 | nM | EC50 | J Med Chem (2010) 53: 4110-4118 [PMID:20408529] |
| GluN1/GluN2B/Glutamate NMDA receptor; Grin1/Grin2b in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096666] [GtoPdb: 455, 457] [UniProtKB: P35439, Q00960] | ||||||||
| ChEMBL | Activity at rat recombinant NR1/NR2B receptor expressed in Xenopus oocytes assessed as effect on glutamate-induced current by two voltage clamp electrophysiology | B | 5.74 | pEC50 | 1800 | nM | EC50 | J Med Chem (2008) 51: 4179-4187 [PMID:18578474] |
| GluN1/GluN2C/Glutamate NMDA receptor; Grin1/Grin2c in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096911] [GtoPdb: 455, 458] [UniProtKB: P35439, Q00961] | ||||||||
| ChEMBL | Activity at rat recombinant NR1/NR2C receptor expressed in Xenopus oocytes assessed as effect on glutamate-induced current by two voltage clamp electrophysiology | B | 6 | pEC50 | 1000 | nM | EC50 | J Med Chem (2008) 51: 4179-4187 [PMID:18578474] |
| Glutamate racemase in Lactobacillus fermentum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3353] [UniProtKB: Q03469] | ||||||||
| ChEMBL | Inhibition towards glutamate racemase from Lactobacillus fermenti was determined and expressed as KI | B | 4.55 | pKi | 28000 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2265-2270 |
| GluA1/GluA2/Glutamate receptor AMPA 1/2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3883294] [GtoPdb: 444, 445] [UniProtKB: P42261, P42262] | ||||||||
| ChEMBL | Agonist activity at recombinant GluA1A2 receptor flop isoform expressed in Xenopus oocytes | F | 4.74 | pEC50 | 18000 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| ChEMBL | Agonist activity at recombinant GluA1A2 receptor flip isoform expressed in Xenopus oocytes | F | 5.21 | pEC50 | 6160 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| GluA2/GluA3/Glutamate receptor AMPA 2/3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3883291] [GtoPdb: 445, 446] [UniProtKB: P42262, P42263] | ||||||||
| ChEMBL | Agonist activity at recombinant GluA2A3 receptor flop isoform expressed in Xenopus oocytes | F | 4.96 | pEC50 | 11000 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| GluA1/GluA2/GluA3/GluA4/Glutamate receptor ionotropic AMPA in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2096670] [GtoPdb: 444, 445, 446, 447] [UniProtKB: P42261, P42262, P42263, P48058] | ||||||||
| ChEMBL | Percent inhibition against AMPA receptor at 1 uM | B | 6.21 | pIC50 | 613 | nM | IC50 | J Med Chem (2005) 48: 6887-6896 [PMID:16250647] |
| 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 | Binding affinity towards AMPA receptor by displacement of [3H]AMPA radioligand. | B | 5.96 | pKi | 1100 | nM | Ki | J Med Chem (2001) 44: 2507-2510 [PMID:11472204] |
| ChEMBL | Tested for inhibition of Specific DL-[H]Ionotropic glutamate receptor AMPA binding to rat brain membranes | B | 5.89 | pIC50 | 1300 | nM | IC50 | J Med Chem (1983) 26: 901-903 [PMID:6133955] |
| ChEMBL | Inhibition of specific binding of [3H]AMPA to Ionotropic glutamate receptor AMPA in rat brain membranes | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (1997) 40: 3182-3191 [PMID:9379437] |
| ChEMBL | Binding affinity was measured by [3H]- Ionotropic glutamate receptor AMPA binding assay. | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (1992) 35: 107-111 [PMID:1370693] |
| ChEMBL | Displacement of [3H]AMPA from AMPA receptor in rat brain synaptic cortical membranes after 30 mins by scintillation counting method | B | 6.47 | pIC50 | 340 | nM | IC50 | J Med Chem (2019) 62: 4467-4482 [PMID:30943028] |
| ChEMBL | Antagonist activity against AMPA receptor expressed in motoneurones by inhibition of fDR-VRP in the neonatal rat spinal cord | F | 6.67 | pIC50 | 214 | nM | IC50 | J Med Chem (2006) 49: 2579-2592 [PMID:16610801] |
| ChEMBL | Compound was evaluated for the inhibition of [3H]AMPA binding to Ionotropic glutamate receptor AMPA from rat brain synaptic membrane. | B | 6.82 | pIC50 | 150 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 2381-2386 |
| GluA1/Glutamate receptor ionotropic, AMPA 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261] | ||||||||
| ChEMBL | Compound was tested for binding affinity against human Ionotropic glutamate receptor AMPA 1 in HEK293 cells using [3H]-AMPA as radioligand | B | 5.87 | pKi | 1362 | nM | Ki | J Med Chem (2000) 43: 1958-1968 [PMID:10821708] |
| ChEMBL | Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 1 expressed in HEK293 cells | B | 5.87 | pKi | 1360 | nM | Ki | J Med Chem (1997) 40: 3645-3650 [PMID:9357531] |
| ChEMBL | Binding affinity of compound was determined against Ionotropic glutamate receptor AMPA 1 using cell membranes prepared from HEK293 cells | B | 5.87 | pKi | 1360 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1807-1810 [PMID:10969973] |
| ChEMBL | Agonist activity at GluR1 E683A/M686V/I687A mutant expressed in HEK293 cells by Fluo-4/Ca2+ assay | F | 4 | pEC50 | 100000 | nM | EC50 | J Med Chem (2007) 50: 4177-4185 [PMID:17672447] |
| ChEMBL | Agonist activity at GluR1 expressed in HEK293 cells by Fluo-4/Ca2+ assay | F | 4.15 | pEC50 | 71000 | nM | EC50 | J Med Chem (2007) 50: 4177-4185 [PMID:17672447] |
| ChEMBL | Agonist activity at GluR1 D399S mutant expressed in HEK293 cells by Fluo-4/Ca2+ assay | F | 4.16 | pEC50 | 69000 | nM | EC50 | J Med Chem (2007) 50: 4177-4185 [PMID:17672447] |
| ChEMBL | Agonist activity at GluR1 D399S/M686V/I687A mutant expressed in HEK293 cells by Fluo-4/Ca2+ assay | F | 4.2 | pEC50 | 63095.73 | nM | EC50 | J Med Chem (2007) 50: 4177-4185 [PMID:17672447] |
| ChEMBL | Agonist activity at GluR1 D399S mutant expressed in HEK293 cells by Fluo-4/Ca2+ assay | F | 4.2 | pEC50 | 63095.73 | nM | EC50 | J Med Chem (2007) 50: 4177-4185 [PMID:17672447] |
| ChEMBL | Agonist activity at GluR1 M686V mutant expressed in HEK293 cells by Fluo-4/Ca2+ assay | F | 4.2 | pEC50 | 63095.73 | nM | EC50 | J Med Chem (2007) 50: 4177-4185 [PMID:17672447] |
| ChEMBL | Agonist activity at GluR1 M686V mutant expressed in HEK293 cells by Fluo-4/Ca2+ assay | F | 4.2 | pEC50 | 63000 | nM | EC50 | J Med Chem (2007) 50: 4177-4185 [PMID:17672447] |
| ChEMBL | Agonist activity at GluR1 D399S/M686V/I687A mutant expressed in HEK293 cells by Fluo-4/Ca2+ assay | F | 4.22 | pEC50 | 60000 | nM | EC50 | J Med Chem (2007) 50: 4177-4185 [PMID:17672447] |
| ChEMBL | Agonist activity at GluR1 E683A mutant expressed in HEK293 cells by Fluo-4/Ca2+ assay | F | 4.4 | pEC50 | 39810.72 | nM | EC50 | J Med Chem (2007) 50: 4177-4185 [PMID:17672447] |
| ChEMBL | Agonist activity at GluR1 E683A mutant expressed in HEK293 cells by Fluo-4/Ca2+ assay | F | 4.41 | pEC50 | 39000 | nM | EC50 | J Med Chem (2007) 50: 4177-4185 [PMID:17672447] |
| ChEMBL | Agonist activity at GluA1 receptor (unknown origin) expressed in HEK293 cells assessed induction of S-glutamate-induced calcium flux measured after 90 secs in presence of cyclothiazide by Fluo4-AM dye-based fluorescence assay | B | 4.48 | pEC50 | 33113.11 | nM | EC50 | J Med Chem (2019) 62: 4467-4482 [PMID:30943028] |
| ChEMBL | Agonist activity at GluA1 receptor (unknown origin) expressed in HEK293 cells assessed induction of S-glutamate-induced calcium flux measured after 90 secs in presence of cyclothiazide by Fluo4-AM dye-based fluorescence assay | B | 4.48 | pEC50 | 33000 | nM | EC50 | J Med Chem (2019) 62: 4467-4482 [PMID:30943028] |
| ChEMBL | Agonist activity at recombinant GluA1 receptor flop isoform expressed in Xenopus oocytes | F | 4.66 | pEC50 | 22000 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| ChEMBL | Agonist activity at recombinant GluA1 receptor flip isoform expressed in Xenopus oocytes co-expressing gamma2-TARP | F | 5.65 | pEC50 | 2260 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| GluA1/Glutamate receptor ionotropic, AMPA 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3753] [GtoPdb: 444] [UniProtKB: P19490] | ||||||||
| ChEMBL | Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR1 expressed in Sf9 cells | B | 6.77 | pKi | 169 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
| ChEMBL | Agonist activity at rat recombinant GluR1 flip isoform expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assay | F | 4.29 | pEC50 | 51000 | nM | EC50 | J Med Chem (2009) 52: 4911-4922 [PMID:19588945] |
| ChEMBL | Agonist activity at rat recombinant GluA1 receptor flip isoform expressed in HEK293 cells assessed as effect on cyclothiazide-induced calcium flux by Fluo-4/AM staining-based fluorescence assay | F | 4.29 | pEC50 | 51000 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| ChEMBL | Activity at rat cloned iGluR1 expressed in human HEK293 cells by calcium imaging assay | B | 4.46 | pEC50 | 35000 | nM | EC50 | J Med Chem (2008) 51: 2311-2315 [PMID:18338843] |
| ChEMBL | Activity at rat cloned iGluR1 expressed in human HEK293 cells by calcium imaging assay | B | 4.49 | pEC50 | 32359.37 | nM | EC50 | J Med Chem (2008) 51: 2311-2315 [PMID:18338843] |
| ChEMBL | Agonist activity at recombinant rat GluA1 receptor flip isoform expressed in Xenopus laevis oocytes by two-electrode voltage clamp assay | B | 4.9 | pEC50 | 12500 | nM | EC50 | J Med Chem (2016) 59: 2244-2254 [PMID:26862980] |
| ChEMBL | Agonist activity at rat recombinant GluA1 receptor flop isoform expressed in Xenopus oocytes | F | 5.19 | pEC50 | 6400 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| ChEMBL | Agonist activity at recombinant rat GluA1 receptor flop isoform expressed in Xenopus laevis oocytes by two-electrode voltage clamp assay | B | 5.47 | pEC50 | 3400 | nM | EC50 | J Med Chem (2016) 59: 2244-2254 [PMID:26862980] |
| GluA2/Glutamate receptor ionotropic, AMPA 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262] | ||||||||
| ChEMBL | Compound was tested for binding affinity against human Ionotropic glutamate receptor AMPA 2 in HK293 cells using [3H]AMPA as radioligand | B | 6.03 | pKi | 940 | nM | Ki | J Med Chem (2000) 43: 1958-1968 [PMID:10821708] |
| ChEMBL | Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 2 expressed in HEK293 cells | B | 6.03 | pKi | 940 | nM | Ki | J Med Chem (1997) 40: 3645-3650 [PMID:9357531] |
| ChEMBL | Binding affinity of compound was determined against Ionotropic glutamate receptor AMPA 2 using cell membranes prepared from HEK293 cells | B | 6.03 | pKi | 940 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1807-1810 [PMID:10969973] |
| ChEMBL | Agonist activity at GluA2(Q) receptor (unknown origin) expressed in HEK293 cells assessed induction of S-glutamate-induced calcium flux measured after 90 secs in presence of cyclothiazide by Fluo4-AM dye-based fluorescence assay | B | 4.24 | pEC50 | 57000 | nM | EC50 | J Med Chem (2019) 62: 4467-4482 [PMID:30943028] |
| ChEMBL | Agonist activity at GluA2(Q) receptor (unknown origin) expressed in HEK293 cells assessed induction of S-glutamate-induced calcium flux measured after 90 secs in presence of cyclothiazide by Fluo4-AM dye-based fluorescence assay | B | 4.25 | pEC50 | 56234.13 | nM | EC50 | J Med Chem (2019) 62: 4467-4482 [PMID:30943028] |
| ChEMBL | Activity at recombinant iGluR2 receptor expressed in Xenopus laevis oocytes using holding potential of -15 to -20 mV by TEVC electrophysiology | B | 4.85 | pEC50 | 14000 | nM | EC50 | J Med Chem (2010) 53: 4110-4118 [PMID:20408529] |
| ChEMBL | Activity at recombinant iGluR2 receptor expressed in Xenopus laevis oocytes using holding potential of -15 to -20 mV by TEVC electrophysiology | B | 4.86 | pEC50 | 13803.84 | nM | EC50 | J Med Chem (2010) 53: 4110-4118 [PMID:20408529] |
| ChEMBL | Agonist activity at recombinant GluA2 receptor flop isoform expressed in Xenopus oocytes | F | 5.21 | pEC50 | 6200 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| ChEMBL | Agonist activity at recombinant GluA2 receptor flop isoform expressed in Xenopus oocytes co-expressing gamma2-TARP | F | 5.66 | pEC50 | 2190 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| GluA2/Glutamate receptor ionotropic, AMPA 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3503] [GtoPdb: 445] [UniProtKB: P19491] | ||||||||
| ChEMBL | Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR2(R) expressed in Sf9 cells | B | 6.55 | pKi | 282 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
| ChEMBL | Displacement of [3H]AMPA from full length recombinant rat GluKA2(R) receptor expressed in sf9 cells by liquid scintillation counting | B | 6.55 | pKi | 282 | nM | Ki | J Med Chem (2013) 56: 1614-1628 [PMID:23414088] |
| ChEMBL | Displacement of [3H]AMPA from rat iGluR2 receptor expressed in Sf9 cells baculovirus system after 1 to 2 hrs by liquid scintillation counting | B | 6.55 | pKi | 281.84 | nM | Ki | J Med Chem (2010) 53: 4110-4118 [PMID:20408529] |
| ChEMBL | Displacement of [3H]AMPA from rat iGluR2 receptor expressed in Sf9 cells baculovirus system after 1 to 2 hrs by liquid scintillation counting | B | 6.55 | pKi | 280 | nM | Ki | J Med Chem (2010) 53: 4110-4118 [PMID:20408529] |
| ChEMBL | Agonist activity at recombinant rat GluA2(Q) receptor flip isoform expressed in Xenopus laevis oocytes by two-electrode voltage clamp assay | B | 4.83 | pEC50 | 14700 | nM | EC50 | J Med Chem (2016) 59: 2244-2254 [PMID:26862980] |
| GluA3/Glutamate receptor ionotropic, AMPA 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3595] [GtoPdb: 446] [UniProtKB: P42263] | ||||||||
| ChEMBL | Agonist activity at GluR3 expressed in HEK293 cells by Fluo-4/Ca2+ assay | F | 4.17 | pEC50 | 67000 | nM | EC50 | J Med Chem (2007) 50: 4177-4185 [PMID:17672447] |
| ChEMBL | Agonist activity at recombinant GluA3 receptor flop isoform expressed in Xenopus oocytes | F | 4.46 | pEC50 | 35000 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| ChEMBL | Agonist activity at GluA3 receptor (unknown origin) expressed in HEK293 cells assessed induction of S-glutamate-induced calcium flux measured after 90 secs in presence of cyclothiazide by Fluo4-AM dye-based fluorescence assay | B | 4.62 | pEC50 | 24000 | nM | EC50 | J Med Chem (2019) 62: 4467-4482 [PMID:30943028] |
| ChEMBL | Agonist activity at GluA3 receptor (unknown origin) expressed in HEK293 cells assessed induction of S-glutamate-induced calcium flux measured after 90 secs in presence of cyclothiazide by Fluo4-AM dye-based fluorescence assay | B | 4.63 | pEC50 | 23442.29 | nM | EC50 | J Med Chem (2019) 62: 4467-4482 [PMID:30943028] |
| ChEMBL | Agonist activity at recombinant GluA3 receptor flop isoform expressed in Xenopus oocytes co-expressing gamma2-TARP | F | 5.44 | pEC50 | 3660 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| GluA3/Glutamate receptor ionotropic, AMPA 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3504] [GtoPdb: 446] [UniProtKB: P19492] | ||||||||
| ChEMBL | Binding affinity to rat GluA3-LBD (GluK3-S1S2) | B | 5.13 | pKi | 7400 | nM | Ki | J Med Chem (2013) 56: 1614-1628 [PMID:23414088] |
| ChEMBL | Binding affinity to full length rat GluA3 | B | 6.3 | pKi | 500 | nM | Ki | J Med Chem (2013) 56: 1614-1628 [PMID:23414088] |
| ChEMBL | Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR3 expressed in Sf9 cells | B | 6.6 | pKi | 249 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
| ChEMBL | Activity at rat cloned iGluR3 expressed in human HEK293 cells by calcium imaging assay | B | 4 | pEC50 | 100000 | nM | EC50 | J Med Chem (2008) 51: 2311-2315 [PMID:18338843] |
| ChEMBL | Agonist activity at rat recombinant GluR3 flip isomer expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assay | F | 4.28 | pEC50 | 52000 | nM | EC50 | J Med Chem (2009) 52: 4911-4922 [PMID:19588945] |
| ChEMBL | Agonist activity at rat recombinant GluA3 receptor flip isoform expressed in HEK293 cells assessed as effect on cyclothiazide-induced calcium flux by Fluo-4/AM staining-based fluorescence assay | F | 4.28 | pEC50 | 52000 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| ChEMBL | Agonist activity at recombinant rat GluA3 receptor flip isoform expressed in Xenopus laevis oocytes by two-electrode voltage clamp assay | B | 4.67 | pEC50 | 21200 | nM | EC50 | J Med Chem (2016) 59: 2244-2254 [PMID:26862980] |
| ChEMBL | Agonist activity at rat recombinant GluA3 receptor flop isoform expressed in Xenopus oocytes | F | 5.89 | pEC50 | 1300 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| GluA4/Glutamate receptor ionotropic, AMPA 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3190] [GtoPdb: 447] [UniProtKB: P48058] | ||||||||
| ChEMBL | Compound was tested for binding affinity against human Ionotropic glutamate receptor AMPA 4 in HEK293 cells using [3H]AMPA as radioligand | B | 6.06 | pKi | 868 | nM | Ki | J Med Chem (2000) 43: 1958-1968 [PMID:10821708] |
| ChEMBL | Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 4 expressed in HEK293 cells | B | 6.06 | pKi | 868 | nM | Ki | J Med Chem (1997) 40: 3645-3650 [PMID:9357531] |
| ChEMBL | Binding affinity of compound was determined against Ionotropic glutamate receptor AMPA 4 using cell membranes prepared from HEK293 cells | B | 6.06 | pKi | 868 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1807-1810 [PMID:10969973] |
| ChEMBL | Agonist activity at GluR4 expressed in HEK293 cells by Fluo-4/Ca2+ assay | F | 4.55 | pEC50 | 28000 | nM | EC50 | J Med Chem (2007) 50: 4177-4185 [PMID:17672447] |
| ChEMBL | Agonist activity at GluA4 receptor (unknown origin) expressed in HEK293 cells assessed induction of S-glutamate-induced calcium flux measured after 90 secs in presence of cyclothiazide by Fluo4-AM dye-based fluorescence assay | B | 5.31 | pEC50 | 4897.79 | nM | EC50 | J Med Chem (2019) 62: 4467-4482 [PMID:30943028] |
| ChEMBL | Agonist activity at GluA4 receptor (unknown origin) expressed in HEK293 cells assessed induction of S-glutamate-induced calcium flux measured after 90 secs in presence of cyclothiazide by Fluo4-AM dye-based fluorescence assay | B | 5.32 | pEC50 | 4800 | nM | EC50 | J Med Chem (2019) 62: 4467-4482 [PMID:30943028] |
| GluA4/Glutamate receptor ionotropic, AMPA 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3505] [GtoPdb: 447] [UniProtKB: P19493] | ||||||||
| ChEMBL | Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR4 expressed in Sf9 cells | B | 6.45 | pKi | 354 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
| ChEMBL | Agonist activity at rat recombinant GluR4 flip isomer expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assay | F | 4.7 | pEC50 | 20000 | nM | EC50 | J Med Chem (2009) 52: 4911-4922 [PMID:19588945] |
| ChEMBL | Agonist activity at rat recombinant GluA4 receptor flip isoform expressed in HEK293 cells assessed as effect on cyclothiazide-induced calcium flux by Fluo-4/AM staining-based fluorescence assay | F | 4.7 | pEC50 | 20000 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| ChEMBL | Agonist activity at recombinant rat GluA4 receptor flip isoform expressed in Xenopus laevis oocytes by two-electrode voltage clamp assay | B | 4.71 | pEC50 | 19600 | nM | EC50 | J Med Chem (2016) 59: 2244-2254 [PMID:26862980] |
| ChEMBL | Activity at rat cloned iGluR4 expressed in human HEK293 cells by calcium imaging assay | B | 4.77 | pEC50 | 17000 | nM | EC50 | J Med Chem (2008) 51: 2311-2315 [PMID:18338843] |
| ChEMBL | Activity at rat cloned iGluR4 expressed in human HEK293 cells by calcium imaging assay | B | 4.78 | pEC50 | 16595.87 | nM | EC50 | J Med Chem (2008) 51: 2311-2315 [PMID:18338843] |
| 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 | Binding affinity towards Ionotropic glutamate receptor kainate by displacement of [3H]-kainic acid radioligand | B | 7.2 | pKi | 63 | nM | Ki | J Med Chem (2001) 44: 2507-2510 [PMID:11472204] |
| ChEMBL | Inhibition of specific binding of [3H]kainate to Ionotropic glutamate receptor kainate in rat brain membranes | B | 6.15 | pIC50 | 700 | nM | IC50 | J Med Chem (1997) 40: 3182-3191 [PMID:9379437] |
| ChEMBL | Binding affinity was measured by [3H]- KAIN receptor binding assay. | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (1992) 35: 107-111 [PMID:1370693] |
| ChEMBL | Compound tested for binding affinity towards Ionotropic glutamate receptor kainate | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (1984) 27: 585-591 [PMID:6325690] |
| ChEMBL | Binding affinity against Ionotropic glutamate receptor kainate by displacing [3H]KA from purified rat synaptic membranes | B | 6.46 | pIC50 | 350 | nM | IC50 | J Med Chem (1985) 28: 673-679 [PMID:2985786] |
| ChEMBL | In vitro binding affinity against synaptic membrane from rat brain using [3H]KAIN as the radioligand | B | 6.57 | pIC50 | 270 | nM | IC50 | J Med Chem (1989) 32: 2254-2260 [PMID:2552114] |
| ChEMBL | Compound was evaluated for the inhibition of [3H]-KA binding to Ionotropic glutamate receptor kainate from rat brain synaptic membrane. | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 2381-2386 |
| GluK1/Glutamate receptor ionotropic kainate 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1918] [GtoPdb: 450] [UniProtKB: P39086] | ||||||||
| ChEMBL | Binding affinity against human ionotropic glutamate receptor kainate 1 in HK293 cells using [3H]kainate as radioligand | B | 6.15 | pKi | 701 | nM | Ki | J Med Chem (2000) 43: 1958-1968 [PMID:10821708] |
| ChEMBL | Binding affinity of compound was determined against Ionotropic glutamate receptor ionotropic kainate 1 using cell membranes prepared from HEK293 cells | B | 6.15 | pKi | 701 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1807-1810 [PMID:10969973] |
| ChEMBL | Effective concentration against GluR5 expressed in HEK293 cells | F | 4.12 | pEC50 | 75000 | nM | EC50 | J Med Chem (2000) 43: 1958-1968 [PMID:10821708] |
| ChEMBL | Compound was tested for agonistic activity at Glutamate receptor 5 using HEK293 cells | F | 4.12 | pEC50 | 75000 | nM | EC50 | Bioorg Med Chem Lett (2000) 10: 1807-1810 [PMID:10969973] |
| ChEMBL | Induction of calcium influx in HEK293 cells expressing human GLUK5 by FLIPR assay | F | 4.66 | pEC50 | 22000 | nM | EC50 | J Med Chem (2006) 49: 2579-2592 [PMID:16610801] |
| GluK1/Glutamate receptor ionotropic kainate 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2919] [GtoPdb: 450] [UniProtKB: P22756] | ||||||||
| ChEMBL | Displacement of [3H]SYM2081 from rat recombinant iGluR5(Q)1b expressed in Sf9 cells | B | 6.85 | pKi | 140 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
| ChEMBL | Displacement of [3H]SYM2081 from rat recombinant iGluR5 | B | 6.85 | pKi | 140 | nM | Ki | J Med Chem (2008) 51: 4093-4103 [PMID:18578478] |
| ChEMBL | Displacement of [3H]SYM2081 from rat iGluR5 receptor expressed in Sf9 cells baculovirus system after 1 to 2 hrs by liquid scintillation counting | B | 6.85 | pKi | 140 | nM | Ki | J Med Chem (2010) 53: 4110-4118 [PMID:20408529] |
| ChEMBL | Displacement of [3H]-(2S,4R)-4-methylglutamic acid from full length recombinant rat GluKK1(Q)1b receptor expressed in sf9 cells by liquid scintillation counting | B | 6.85 | pKi | 140 | nM | Ki | J Med Chem (2013) 56: 1614-1628 [PMID:23414088] |
| ChEMBL | Displacement of [3H]SYM2081 from rat recombinant iGluR5 | B | 6.86 | pKi | 138.04 | nM | Ki | J Med Chem (2008) 51: 4093-4103 [PMID:18578478] |
| ChEMBL | Displacement of [3H]SYM2081 from rat iGluR5 receptor expressed in Sf9 cells baculovirus system after 1 to 2 hrs by liquid scintillation counting | B | 6.86 | pKi | 138.04 | nM | Ki | J Med Chem (2010) 53: 4110-4118 [PMID:20408529] |
| ChEMBL | Compound was tested for agonistic activity on rat dorsal root ganglion neurons (thought to express GluR5 receptors) | F | 4.45 | pEC50 | 35200 | nM | EC50 | Bioorg Med Chem Lett (2000) 10: 1807-1810 [PMID:10969973] |
| GluK2/Glutamate receptor ionotropic kainate 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3683] [GtoPdb: 451] [UniProtKB: Q13002] | ||||||||
| ChEMBL | Binding affinity against human GluR6 | B | 5.96 | pKi | 1106 | nM | Ki | J Med Chem (2000) 43: 1958-1968 [PMID:10821708] |
| ChEMBL | Binding affinity of compound was determined against Ionotropic glutamate receptor ionotropic kainate 2 using cell membranes prepared from HEK293 cells | B | 5.96 | pKi | 1106 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1807-1810 [PMID:10969973] |
| ChEMBL | Effective concentration against human GluR6 expressed in HEK293 cells | F | 4.6 | pEC50 | 25000 | nM | EC50 | J Med Chem (2000) 43: 1958-1968 [PMID:10821708] |
| ChEMBL | Compound was tested for agonistic activity at Glutamate receptor 6 using HEK293 cells | F | 4.6 | pEC50 | 25000 | nM | EC50 | Bioorg Med Chem Lett (2000) 10: 1807-1810 [PMID:10969973] |
| GluK2/Glutamate receptor ionotropic kainate 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3607] [GtoPdb: 451] [UniProtKB: P42260] | ||||||||
| ChEMBL | Displacement of [3H]kainate from rat GLUK6 receptor expressed in HEK293 cells | B | 5.48 | pKi | 3280 | nM | Ki | J Med Chem (2005) 48: 7867-7881 [PMID:16302825] |
| ChEMBL | Displacement of [3H]kainate from rat GLUK6 expressed in HEK293 cells | B | 5.48 | pKi | 3280 | nM | Ki | J Med Chem (2006) 49: 2579-2592 [PMID:16610801] |
| ChEMBL | Displacement of [3H]kainic acid from rat recombinant iGluR6(V,C,R) receptor expressed in Sf9 cells | B | 6.48 | pKi | 332 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
| ChEMBL | Displacement of [3H]SYM2081 from rat recombinant iGluR6 | B | 6.48 | pKi | 331.13 | nM | Ki | J Med Chem (2008) 51: 4093-4103 [PMID:18578478] |
| ChEMBL | Displacement of [3H]SYM2081 from rat iGluR6 receptor expressed in Sf9 cells baculovirus system after 1 to 2 hrs by liquid scintillation counting | B | 6.48 | pKi | 331.13 | nM | Ki | J Med Chem (2010) 53: 4110-4118 [PMID:20408529] |
| ChEMBL | Displacement of [3H]-(2S,4R)-4-methylglutamic acid from full length recombinant rat GluKK2(VCR) receptor expressed in sf9 cells by liquid scintillation counting | B | 6.48 | pKi | 331 | nM | Ki | J Med Chem (2013) 56: 1614-1628 [PMID:23414088] |
| ChEMBL | Displacement of [3H]SYM2081 from rat recombinant iGluR6 | B | 6.48 | pKi | 331 | nM | Ki | J Med Chem (2008) 51: 4093-4103 [PMID:18578478] |
| ChEMBL | Displacement of [3H]SYM2081 from rat iGluR6 receptor expressed in Sf9 cells baculovirus system after 1 to 2 hrs by liquid scintillation counting | B | 6.48 | pKi | 330 | nM | Ki | J Med Chem (2010) 53: 4110-4118 [PMID:20408529] |
| ChEMBL | Agonist activity at rat recombinant GluR6(Q) RNA-edited isoform expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assay | F | 4.14 | pEC50 | 73000 | nM | EC50 | J Med Chem (2009) 52: 4911-4922 [PMID:19588945] |
| ChEMBL | Activity at rat cloned iGluR6 expressed in human HEK293 cells by calcium imaging assay | B | 4.18 | pEC50 | 66000 | nM | EC50 | J Med Chem (2008) 51: 2311-2315 [PMID:18338843] |
| ChEMBL | Activity at rat cloned iGluR6 expressed in human HEK293 cells by calcium imaging assay | B | 4.23 | pEC50 | 58884.37 | nM | EC50 | J Med Chem (2008) 51: 2311-2315 [PMID:18338843] |
| GluK3/Glutamate receptor ionotropic kainate 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3684] [GtoPdb: 452] [UniProtKB: Q13003] | ||||||||
| ChEMBL | Ability to bind to Ionotropic glutamate receptor ionotropic kainate 3 was evaluated | B | 6.1 | pKi | 789 | nM | Ki | J Med Chem (2000) 43: 1958-1968 [PMID:10821708] |
| ChEMBL | Binding affinity of compound was determined against Ionotropic glutamate receptor ionotropic kainate 3 using cell membranes prepared from HEK293 cells | B | 6.1 | pKi | 789 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1807-1810 [PMID:10969973] |
| GluK3/Glutamate receptor ionotropic kainate 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3744] [GtoPdb: 452] [UniProtKB: P42264] | ||||||||
| ChEMBL | Displacement of [3H]SYM2081 from rat recombinant iGluR7 | B | 6.31 | pKi | 494 | nM | Ki | J Med Chem (2008) 51: 4093-4103 [PMID:18578478] |
| ChEMBL | Displacement of [3H]-(2S,4R)-4-methylglutamic acid from full length recombinant rat GluK3 receptor expressed in sf9 cells by liquid scintillation counting | B | 6.31 | pKi | 494 | nM | Ki | J Med Chem (2013) 56: 1614-1628 [PMID:23414088] |
| ChEMBL | Displacement of [3H]SYM2081 from rat iGluR7 receptor expressed in Sf9 cells baculovirus system after 1 to 2 hrs by liquid scintillation counting | B | 6.31 | pKi | 490 | nM | Ki | J Med Chem (2010) 53: 4110-4118 [PMID:20408529] |
| ChEMBL | Displacement of [3H]SYM2081 from rat recombinant iGluR7 | B | 6.31 | pKi | 489.78 | nM | Ki | J Med Chem (2008) 51: 4093-4103 [PMID:18578478] |
| ChEMBL | Displacement of [3H]SYM2081 from rat iGluR7 receptor expressed in Sf9 cells baculovirus system after 1 to 2 hrs by liquid scintillation counting | B | 6.31 | pKi | 489.78 | nM | Ki | J Med Chem (2010) 53: 4110-4118 [PMID:20408529] |
| GluK5/Glutamate receptor ionotropic kainate 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2675] [GtoPdb: 454] [UniProtKB: Q16478] | ||||||||
| ChEMBL | Ability to bind to Ionotropic glutamate receptor kainate (kainate 2) was evaluated. | B | 6.12 | pKi | 750 | nM | Ki | J Med Chem (2000) 43: 1958-1968 [PMID:10821708] |
| ChEMBL | Binding affinity of compound was determined against Glutamate receptor (KA2) using cell membranes prepared from HEK293 cells | B | 6.12 | pKi | 750 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1807-1810 [PMID:10969973] |
| ChEMBL | Displacement of [3H]kainate from human Ionotropic glutamate receptor ionotropic kainate 1 expressed in HEK293 cells | B | 6.15 | pKi | 701 | nM | Ki | J Med Chem (1997) 40: 3645-3650 [PMID:9357531] |
| glutathione-disulfide reductase/Glutathione reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2755] [GtoPdb: 2613] [UniProtKB: P00390] | ||||||||
| ChEMBL | Competitive inhibition of human erythrocyte Glutathione reductase using GSSG substrate by Lineweaver-Burk plot analysis | B | 4.37 | pKi | 42700 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 5398-5402 [PMID:21795044] |
| ChEMBL | Inhibition of human erythrocyte Glutathione reductase | B | 4.27 | pIC50 | 53700 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 5398-5402 [PMID:21795044] |
| GluN1/GluN2D/Ionotropic glutamate receptor NMDA 1/2D in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038506] [GtoPdb: 455, 459] [UniProtKB: P35439, Q62645] | ||||||||
| ChEMBL | Activity at rat NR1/NR2D receptor expressed in Xenopus oocytes assessed as effect on glutamate-induced current by two voltage clamp electrophysiology | B | 6.35 | pEC50 | 450 | nM | EC50 | J Med Chem (2008) 51: 4179-4187 [PMID:18578474] |
| 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 | 5 | pKi | 10000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells | B | 5.8 | pKi | 1584.89 | nM | Ki | Medchemcomm (2011) 2: 1120-1124 |
| ChEMBL | Displacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cells | B | 6.24 | pKi | 570 | nM | Ki | Bioorg Med Chem (2009) 17: 242-250 [PMID:19042134] |
| ChEMBL | Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells | B | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2007) 50: 4630-4641 [PMID:17725337] |
| ChEMBL | Agonistic activity at mGlu1-alpha receptor expressed in CHO cells | F | 4.72 | pEC50 | 19000 | nM | EC50 | J Med Chem (1996) 39: 3188-3194 [PMID:8759641] |
| GtoPdb | - | - | 5 | pEC50 | - | - | - | Eur J Pharmacol (1999) 375: 277-94 [PMID:10443583] |
| ChEMBL | Compound was tested for the inhibition of Metabotropic glutamate receptor 1 | B | 5.31 | pEC50 | 4900 | nM | EC50 | J Med Chem (1998) 41: 1641-1650 [PMID:9572889] |
| ChEMBL | Agonist activity at human mGluR1 receptor expressed in HEK cells | B | 5.8 | pEC50 | 1600 | nM | EC50 | Medchemcomm (2011) 2: 1120-1124 |
| ChEMBL | Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate | F | 5.98 | pEC50 | 1050 | nM | EC50 | Bioorg Med Chem Lett (2000) 10: 129-133 [PMID:10673095] |
| mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385] | ||||||||
| ChEMBL | Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells | B | 6.47 | pKi | 340 | nM | Ki | J Med Chem (2002) 45: 3171-3183 [PMID:12109902] |
| GtoPdb | - | - | 6.5 | pKi | - | - | - |
Mol Pharmacol (2003) 63: 1082-93 [PMID:12695537]; J Neurochem (2000) 75: 2590-601 [PMID:11080213] |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR1b in rat | B | 4.25 | pEC50 | 56000 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| ChEMBL | Agonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay | F | 4.64 | pEC50 | 23160 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 2523-2526 [PMID:25958247] |
| ChEMBL | Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay | F | 4.86 | pEC50 | 13870 | nM | EC50 | J Med Chem (2016) 59: 914-924 [PMID:26814576] |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR1c in rat | B | 4.89 | pEC50 | 13000 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR1a in rat | B | 4.92 | pEC50 | 12000 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| ChEMBL | Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1 | B | 5 | pEC50 | 10000 | nM | EC50 | J Med Chem (2002) 45: 4240-4245 [PMID:12213064] |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR1a in rat | B | 5.05 | pEC50 | 9000 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| ChEMBL | Activity at rat mGluR1 by measuring intracellular calcium concentration in CHO cells | F | 5.14 | pEC50 | 7300 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 196-199 [PMID:16213710] |
| ChEMBL | Activity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentration | F | 5.14 | pEC50 | 7300 | nM | EC50 | Bioorg Med Chem (2007) 15: 3161-3170 [PMID:17350267] |
| ChEMBL | Agonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cells | F | 5.52 | pEC50 | 3000 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 1569-1572 [PMID:11412983] |
| ChEMBL | Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay | F | 5.8 | pEC50 | 1600 | nM | EC50 | J Med Chem (2016) 59: 914-924 [PMID:26814576] |
| ChEMBL | Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay | F | 5.8 | pEC50 | 1584.89 | nM | EC50 | J Med Chem (2016) 59: 914-924 [PMID:26814576] |
| mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416] | ||||||||
| GtoPdb | - | - | 4.9 | pKi | - | - | - | Neuropharmacology (1999) 38: 1519-29 [PMID:10530814] |
| ChEMBL | Potency against cloned Metabotropic glutamate receptor 2 agonist | F | 4.92 | pKi | 12000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Displacement of [3H]LY341495 from mGluR2 receptor expressed in BHK cells | B | 4.96 | pKi | 11000 | nM | Ki | J Med Chem (2007) 50: 4630-4641 [PMID:17725337] |
| ChEMBL | Displacement of [3H]Quisqualate from human mGluR2 receptor expressed in BHK cells | B | 5.19 | pKi | 6400 | nM | Ki | Bioorg Med Chem (2009) 17: 242-250 [PMID:19042134] |
| ChEMBL | Displacement of [3H]-LY341495 from human mGluR2 receptor expressed in HEK cells | B | 5.74 | pKi | 1819.7 | nM | Ki | Medchemcomm (2011) 2: 1120-1124 |
| ChEMBL | Binding affinity at Metabotropic glutamate receptor 2 | B | 5.92 | pKi | 1200 | nM | Ki | J Med Chem (2002) 45: 3171-3183 [PMID:12109902] |
| ChEMBL | Activity at human mGluR2 from BHK cells in [35S]GTP-gamma-S stimulation assay | F | 4.59 | pEC50 | 26000 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 196-199 [PMID:16213710] |
| ChEMBL | Activity at human recombinant mGluR2 expressed in BHK cells assessed as stimulation of [35S]GTP-gamma-S binding | F | 4.59 | pEC50 | 26000 | nM | EC50 | Bioorg Med Chem (2007) 15: 3161-3170 [PMID:17350267] |
| ChEMBL | Agonist activity at human mGluR2 expressed in CHO cells at by [S35]GTPgammaS binding assay | F | 4.9 | pEC50 | 12589.25 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 971-976 [PMID:21232953] |
| ChEMBL | Agonistic activity at mGlu2 receptor expressed in CHO cells | F | 5.07 | pEC50 | 8500 | nM | EC50 | J Med Chem (1996) 39: 3188-3194 [PMID:8759641] |
| ChEMBL | Antagonistic activity against stimulation of GTP (gamma) 35 S binding by glutamate in membranes from CHO cells expressing human mGluR2 | B | 5.13 | pEC50 | 7400 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 3179-3182 [PMID:11720869] |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR2 in human | B | 5.33 | pEC50 | 4700 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| GtoPdb | - | - | 5.4 | pEC50 | - | - | - | Eur J Pharmacol (1999) 375: 277-94 [PMID:10443583] |
| ChEMBL | Agonist activity at human recombinant mGlu2 receptor E273D and L300Q mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay | F | 5.59 | pEC50 | 2575 | nM | EC50 | J Med Chem (2015) 58: 7526-7548 [PMID:26313429] |
| ChEMBL | Agonist activity at human recombinant mGlu2 receptor E273D mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay | F | 5.63 | pEC50 | 2351 | nM | EC50 | J Med Chem (2015) 58: 7526-7548 [PMID:26313429] |
| ChEMBL | Agonist activity at wild type human recombinant mGlu2 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay | F | 5.74 | pEC50 | 1827 | nM | EC50 | J Med Chem (2015) 58: 7526-7548 [PMID:26313429] |
| ChEMBL | Agonist activity at human mGluR2 receptor expressed in HEK cells | B | 5.74 | pEC50 | 1800 | nM | EC50 | Medchemcomm (2011) 2: 1120-1124 |
| ChEMBL | Agonist activity at human recombinant mGlu2 receptor L300Q mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay | F | 5.75 | pEC50 | 1767 | nM | EC50 | J Med Chem (2015) 58: 7526-7548 [PMID:26313429] |
| ChEMBL | Compound was tested for the inhibition of metabotropic glutamate receptor 2 (mGluR2). | B | 6.54 | pEC50 | 290 | 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 | - | - | 5.9 | pKi | - | - | - |
Mol Pharmacol (1994) 45: 1177-1182 [PMID:8022410]; Trends Neurosci (2000) 23: 80-8 [PMID:10652549] |
| ChEMBL | Agonist activity at rat mGluR2 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay | F | 4.74 | pEC50 | 18250 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 2523-2526 [PMID:25958247] |
| ChEMBL | Agonist activity at rat mGlu2 receptor by FRET based mGlu sensor assay | B | 4.79 | pEC50 | 16090 | nM | EC50 | J Med Chem (2016) 59: 914-924 [PMID:26814576] |
| ChEMBL | Agonist activity in rat at Metabotropic glutamate receptor 2 expressed in HEK293 cells | F | 4.8 | pEC50 | 16000 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 1569-1572 [PMID:11412983] |
| ChEMBL | Agonist activity at rat mGlu2 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay | F | 4.88 | pEC50 | 13080 | nM | EC50 | J Med Chem (2016) 59: 914-924 [PMID:26814576] |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR2 in rat | B | 4.93 | pEC50 | 11800 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| ChEMBL | Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 2 | B | 5.4 | pEC50 | 4000 | nM | EC50 | J Med Chem (2002) 45: 4240-4245 [PMID:12213064] |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR2 in rat | B | 5.4 | pEC50 | 4000 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| ChEMBL | Agonist activity at rat mGlu2 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assay | B | 5.74 | pEC50 | 1819.7 | nM | EC50 | J Med Chem (2016) 59: 914-924 [PMID:26814576] |
| ChEMBL | Agonist activity at rat mGlu2 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assay | B | 5.74 | pEC50 | 1800 | nM | EC50 | J Med Chem (2016) 59: 914-924 [PMID:26814576] |
| ChEMBL | Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing mGluR2 receptor | F | 6.21 | pEC50 | 610 | nM | EC50 | Bioorg Med Chem Lett (1999) 9: 1721-1726 [PMID:10397508] |
| 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 | 5.05 | pKi | 9000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Binding affinity to human mGluR3 receptor expressed in HEK cells | B | 7.24 | pKi | 57.54 | nM | Ki | Medchemcomm (2011) 2: 1120-1124 |
| GtoPdb | - | - | 7.4 | pKi | - | - | - | Neuropharmacology (1999) 38: 1519-29 [PMID:10530814] |
| ChEMBL | Agonist activity at human recombinant mGlu3 receptor D279E and Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay | F | 5.29 | pEC50 | 5118 | nM | EC50 | J Med Chem (2015) 58: 7526-7548 [PMID:26313429] |
| ChEMBL | Agonist activity at human recombinant mGlu3 receptor D279E mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay | F | 5.38 | pEC50 | 4182 | nM | EC50 | J Med Chem (2015) 58: 7526-7548 [PMID:26313429] |
| GtoPdb | - | - | 5.4 | pEC50 | - | - | - | Eur J Pharmacol (1999) 375: 277-94 [PMID:10443583] |
| ChEMBL | Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptor | F | 5.6 | pEC50 | 2500 | nM | EC50 | Bioorg Med Chem Lett (1999) 9: 1721-1726 [PMID:10397508] |
| ChEMBL | Agonist activity at human recombinant mGlu3 receptor Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay | F | 5.83 | pEC50 | 1484 | nM | EC50 | J Med Chem (2015) 58: 7526-7548 [PMID:26313429] |
| ChEMBL | Agonist activity at wild type human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay | F | 6 | pEC50 | 1002 | nM | EC50 | J Med Chem (2015) 58: 7526-7548 [PMID:26313429] |
| ChEMBL | Agonist activity at human mGluR3 receptor expressed in HEK cells | B | 7.22 | pEC50 | 60 | nM | EC50 | Medchemcomm (2011) 2: 1120-1124 |
| mGlu3 receptor/Metabotropic glutamate receptor 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3067] [GtoPdb: 291] [UniProtKB: P31422] | ||||||||
| GtoPdb | - | - | 6.4 | pKi | - | - | - | Neuropharmacology (2000) 39: 1700-6 [PMID:10884552] |
| ChEMBL | Agonist activity at rat mGlu3 receptor by FRET based mGlu sensor assay | B | 5.47 | pEC50 | 3400 | nM | EC50 | J Med Chem (2016) 59: 914-924 [PMID:26814576] |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR3 in rat | B | 5.52 | pEC50 | 3000 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| ChEMBL | Agonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assay | B | 7.22 | pEC50 | 60 | nM | EC50 | J Med Chem (2016) 59: 914-924 [PMID:26814576] |
| ChEMBL | Agonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assay | B | 7.24 | pEC50 | 57.54 | nM | EC50 | J Med Chem (2016) 59: 914-924 [PMID:26814576] |
| 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 | 4.77 | pKi | 17000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Displacement of [3H]-L-AP4 from human mGluR4 receptor expressed in HEK cells | B | 5.49 | pKi | 3235.94 | nM | Ki | Medchemcomm (2011) 2: 1120-1124 |
| ChEMBL | Displacement of [3H]LAP4 from mGluR4 receptor expressed in BHK cells | B | 5.62 | pKi | 2400 | nM | Ki | J Med Chem (2007) 50: 4630-4641 [PMID:17725337] |
| ChEMBL | Binding affinity at Metabotropic glutamate receptor 4 | B | 5.8 | pKi | 1600 | nM | Ki | J Med Chem (2002) 45: 3171-3183 [PMID:12109902] |
| ChEMBL | Displacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cells | B | 5.85 | pKi | 1400 | nM | Ki | Bioorg Med Chem (2009) 17: 242-250 [PMID:19042134] |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR4a in human | B | 4.7 | pEC50 | 20000 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| ChEMBL | Agonistic activity at mGlu4a receptor expressed in CHO cells | F | 4.82 | pEC50 | 15000 | nM | EC50 | J Med Chem (1996) 39: 3188-3194 [PMID:8759641] |
| ChEMBL | Compound was tested for the inhibition of Metabotropic glutamate receptor 4 | B | 5.01 | pEC50 | 9800 | nM | EC50 | J Med Chem (1998) 41: 1641-1650 [PMID:9572889] |
| ChEMBL | Agonist activity at human mGluR4 receptor expressed in HEK cells | B | 5.49 | pEC50 | 3200 | nM | EC50 | Medchemcomm (2011) 2: 1120-1124 |
| GtoPdb | - | - | 5.5 | pEC50 | - | - | - | Eur J Pharmacol (1999) 375: 277-94 [PMID:10443583] |
| mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423] | ||||||||
| ChEMBL | Displacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cells | B | 5.47 | pKi | 3400 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 196-199 [PMID:16213710] |
| ChEMBL | Displacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assay | B | 5.47 | pKi | 3400 | nM | Ki | Bioorg Med Chem (2007) 15: 3161-3170 [PMID:17350267] |
| GtoPdb | - | - | 5.5 | pKi | - | - | - |
Neuropharmacology (1997) 36: 21-30 [PMID:9144638]; J Biol Chem (1999) 274: 10008-13 [PMID:10187777]; Eur J Pharmacol (1992) 227: 361-2 [PMID:1361913]; J Med Chem (1997) 40: 3700-5 [PMID:9357538] |
| ChEMBL | Agonist activity at rat mGluR4 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay | F | 4.9 | pEC50 | 12570 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 2523-2526 [PMID:25958247] |
| ChEMBL | Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 4 | B | 4.92 | pEC50 | 12000 | nM | EC50 | J Med Chem (2002) 45: 4240-4245 [PMID:12213064] |
| ChEMBL | Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay | F | 5.02 | pEC50 | 9490 | nM | EC50 | J Med Chem (2016) 59: 914-924 [PMID:26814576] |
| ChEMBL | Agonist activity at rat recombinant mGluR4 expressed in BHK cells | F | 5.21 | pEC50 | 6100 | nM | EC50 | Bioorg Med Chem (2007) 15: 3161-3170 [PMID:17350267] |
| ChEMBL | Functional activity at rat mGluR4 | F | 5.21 | pEC50 | 6100 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 196-199 [PMID:16213710] |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR4a in rat | B | 5.3 | pEC50 | 5000 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| ChEMBL | Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production | F | 5.49 | pEC50 | 3235.94 | nM | EC50 | J Med Chem (2016) 59: 914-924 [PMID:26814576] |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR4a in rat | B | 5.49 | pEC50 | 3200 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| ChEMBL | Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production | F | 5.49 | pEC50 | 3200 | nM | EC50 | J Med Chem (2016) 59: 914-924 [PMID:26814576] |
| ChEMBL | Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry | F | 5.54 | pEC50 | 2880 | nM | EC50 | Bioorg Med Chem (2012) 20: 4716-4726 [PMID:22750138] |
| 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 | 4.94 | pKi | 11400 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Displacement of [3H]-Quisqualate from human mGluR5 receptor expressed in HEK cells | B | 5.33 | pKi | 4677.35 | nM | Ki | Medchemcomm (2011) 2: 1120-1124 |
| ChEMBL | Displacement of [3H]Quisqualate from human mGluR5 receptor expressed in BHK cells | B | 5.94 | pKi | 1160 | nM | Ki | Bioorg Med Chem (2009) 17: 242-250 [PMID:19042134] |
| ChEMBL | Binding affinity to mGluR5 receptor expressed in BHK cells | B | 6.41 | pKi | 390 | nM | Ki | J Med Chem (2007) 50: 4630-4641 [PMID:17725337] |
| ChEMBL | Agonist activity at mGlu5 receptor (unknown origin) expressed in CHO cells assessed as increase in Gq-mediated PI hydrolysis after 45 mins by yttrium scintillation proximity assay | B | 4.8 | pEC50 | 16000 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| ChEMBL | Agonist activity at human mGluR5 receptor expressed in HEK cells | B | 5.33 | pEC50 | 4700 | nM | EC50 | Medchemcomm (2011) 2: 1120-1124 |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR5a in human | B | 5.39 | pEC50 | 4100 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| GtoPdb | - | - | 5.5 | pEC50 | - | - | - | Eur J Pharmacol (1999) 375: 277-94 [PMID:10443583] |
| ChEMBL | Compound was tested for the inhibition of Metabotropic glutamate receptor 5 | B | 5.51 | pEC50 | 3100 | nM | EC50 | J Med Chem (1998) 41: 1641-1650 [PMID:9572889] |
| mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424] | ||||||||
| GtoPdb | - | - | 6.1 | pIC50 | - | - | - | J Neurochem (2000) 75: 2590-601 [PMID:11080213] |
| ChEMBL | Agonist activity at rat mGluR5 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay | F | 4.86 | pEC50 | 13650 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 2523-2526 [PMID:25958247] |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR5a in rat | B | 5 | pEC50 | 10000 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| ChEMBL | Agonist activity at rat mGlu5 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay | F | 5.05 | pEC50 | 8990 | nM | EC50 | J Med Chem (2016) 59: 914-924 [PMID:26814576] |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR5b in rat | B | 5.1 | pEC50 | 8000 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR5a in rat | B | 5.1 | pEC50 | 8000 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| ChEMBL | Agonist activity at rat mGlu5 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay | F | 5.33 | pEC50 | 4700 | nM | EC50 | J Med Chem (2016) 59: 914-924 [PMID:26814576] |
| ChEMBL | Agonist activity at rat mGlu5 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay | F | 5.33 | pEC50 | 4677.35 | nM | EC50 | J Med Chem (2016) 59: 914-924 [PMID:26814576] |
| ChEMBL | Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 5 | B | 5.36 | pEC50 | 4400 | nM | EC50 | J Med Chem (2002) 45: 4240-4245 [PMID:12213064] |
| ChEMBL | Activity at rat recombinant mGluR5 expressed in CHO cells assessed as intracellular calcium concentration | F | 5.92 | pEC50 | 1200 | nM | EC50 | Bioorg Med Chem (2007) 15: 3161-3170 [PMID:17350267] |
| ChEMBL | Activity at rat mGluR5 by measuring intracellular calcium concentration in CHO cells | F | 5.92 | pEC50 | 1200 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 196-199 [PMID:16213710] |
| 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 | 4.42 | pKi | 38000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Agonistic activity at mGlu6 receptor expressed in CHO cells | F | 4.7 | pEC50 | 20000 | nM | EC50 | J Med Chem (1996) 39: 3188-3194 [PMID:8759641] |
| GtoPdb | - | - | 4.8 | pEC50 | - | - | - | Eur J Pharmacol (1999) 375: 277-94 [PMID:10443583] |
| GtoPdb | - | - | 5.2 | pEC50 | - | - | - | Neuropharmacology (1997) 36: 145-52 [PMID:9144651] |
| ChEMBL | Compound was tested for the inhibition of Metabotropic glutamate receptor 6 | B | 5.31 | pEC50 | 4900 | nM | EC50 | J Med Chem (1998) 41: 1641-1650 [PMID:9572889] |
| mGlu6 receptor/Metabotropic glutamate receptor 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3842] [GtoPdb: 294] [UniProtKB: P35349] | ||||||||
| ChEMBL | Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay | F | 4.09 | pEC50 | 82210 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 2523-2526 [PMID:25958247] |
| ChEMBL | Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay | F | 4.19 | pEC50 | 65090 | nM | EC50 | J Med Chem (2016) 59: 914-924 [PMID:26814576] |
| GtoPdb | - | - | 4.4 | pEC50 | - | - | - | Neuropharmacology (1998) 37: 1043-51 [PMID:9833633] |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR6 in rat | B | 4.8 | pEC50 | 16000 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| ChEMBL | Activity at rat mGluR6 by measuring cAMP formation in CHO cells | F | 5.12 | pEC50 | 7600 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 196-199 [PMID:16213710] |
| ChEMBL | Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production | F | 5.12 | pEC50 | 7600 | nM | EC50 | Bioorg Med Chem (2007) 15: 3161-3170 [PMID:17350267] |
| mGlu7 receptor/Metabotropic glutamate receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3777] [GtoPdb: 295] [UniProtKB: Q14831] | ||||||||
| GtoPdb | - | - | 3.1 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2000) 362: 546-54 [PMID:11138847] |
| GtoPdb | - | - | 3 | pEC50 | - | - | - | Eur J Pharmacol (1999) 375: 277-94 [PMID:10443583] |
| ChEMBL | Agonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP production | F | 5.93 | pEC50 | 1180 | nM | EC50 | J Med Chem (2016) 59: 914-924 [PMID:26814576] |
| mGlu7 receptor/Metabotropic glutamate receptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879] [GtoPdb: 295] [UniProtKB: P35400] | ||||||||
| ChEMBL | Agonist activity at rat mGluR7 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay | F | 4 | pEC50 | >100000 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 2523-2526 [PMID:25958247] |
| 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 | 5.02 | pKi | 9500 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| GtoPdb | - | - | 5.7 | pIC50 | - | - | - |
Brain Res Mol Brain Res (1998) 53: 88-97 [PMID:9473604]; Brain Res Mol Brain Res (1999) 67: 201-10 [PMID:10216218] |
| ChEMBL | Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8 | B | 8.24 | pIC50 | 5.7 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 349-351 [PMID:15603952] |
| GtoPdb | - | - | 5.6 | pEC50 | - | - | - | Eur J Pharmacol (1999) 375: 277-94 [PMID:10443583] |
| mGlu8 receptor/Metabotropic glutamate receptor 8 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4626] [GtoPdb: 296] [UniProtKB: P47743] | ||||||||
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouse | B | 7.66 | pEC50 | 22 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| mGlu8 receptor/Metabotropic glutamate receptor 8 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2718] [GtoPdb: 296] [UniProtKB: P70579] | ||||||||
| ChEMBL | Displacement of [3H]LY341495 from rat mGluR8 expressed in BHK cells | B | 5.47 | pKi | 3400 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 196-199 [PMID:16213710] |
| ChEMBL | Displacement of [3H]LY341495 from rat recombinant mGluR8 expressed in BHK cells by SPA assay | B | 5.47 | pKi | 3400 | nM | Ki | Bioorg Med Chem (2007) 15: 3161-3170 [PMID:17350267] |
| ChEMBL | Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay | F | 4.67 | pEC50 | 21470 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 2523-2526 [PMID:25958247] |
| ChEMBL | Agonist activity at rat mGlu8 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay | F | 4.85 | pEC50 | 14010 | nM | EC50 | J Med Chem (2016) 59: 914-924 [PMID:26814576] |
| ChEMBL | Agonist activity in rat at Metabotropic glutamate receptor 8 expressed in HEK293 cells | F | 5.1 | pEC50 | 8000 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 1569-1572 [PMID:11412983] |
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]
