L-glutamic acid [Ligand Id: 1369] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL575060 (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) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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] |
| 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] |
| 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 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]
