NBQX [Ligand Id: 4264] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL222519 (NBQX)
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  • GluN2C/Glutamate [NMDA] receptor subunit epsilon 3 in Rat [ChEMBL: CHEMBL401] [GtoPdb: 458] [UniProtKB: Q00961]
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  • GluN1/Glutamate (NMDA) receptor subunit zeta 1 in Rat [ChEMBL: CHEMBL330] [GtoPdb: 455] [UniProtKB: P35439]
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  • GluA1/Glutamate receptor ionotropic, AMPA 1 in Human [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261]
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  • GluA2/Glutamate receptor ionotropic, AMPA 2 in Human [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262]
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  • GluA3/Glutamate receptor ionotropic, AMPA 3 in Human [ChEMBL: CHEMBL3595] [GtoPdb: 446] [UniProtKB: P42263]
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  • GluA4/Glutamate receptor ionotropic, AMPA 4 in Human [ChEMBL: CHEMBL3190] [GtoPdb: 447] [UniProtKB: P48058]
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  • GluK1/Glutamate receptor ionotropic kainate 1 in Human [ChEMBL: CHEMBL1918] [GtoPdb: 450] [UniProtKB: P39086]
  • GluK1/Glutamate receptor ionotropic kainate 1 in Rat [ChEMBL: CHEMBL2919] [GtoPdb: 450] [UniProtKB: P22756]
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  • GluK2/Glutamate receptor ionotropic kainate 2 in Human [ChEMBL: CHEMBL3683] [GtoPdb: 451] [UniProtKB: Q13002]
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  • GluK3/Glutamate receptor ionotropic kainate 3 in Human [ChEMBL: CHEMBL3684] [GtoPdb: 452] [UniProtKB: Q13003]
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  • GluK5/Glutamate receptor ionotropic kainate 5 in Rat [ChEMBL: CHEMBL4041] [GtoPdb: 454] [UniProtKB: Q63273]
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  • mGlu6 receptor/Metabotropic glutamate receptor 6 in Human [ChEMBL: CHEMBL4573] [GtoPdb: 294] [UniProtKB: O15303]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GluN2D/GluN3B/GluN1/GluN2A/GluN2B/GluN2C/GluN3A/Glutamate [NMDA] receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094124] [GtoPdb: 459461455456457458460] [UniProtKB: O15399O60391Q05586Q12879Q13224Q14957Q8TCU5]
ChEMBL Tested for the affinity to the glycine site -NMDA receptor using [3H]Gly as radioligand. B 4 pIC50 >100000 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 77-80
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455456457458459461460] [UniProtKB: P35439Q00959Q00960Q00961Q62645Q8VHN2Q9R1M7]
ChEMBL The compound was tested for its ability to inhibit [3H]Glu binding to N-methyl-D-aspartate glutamate receptor from rat whole brain. B 4 pKi >100000 nM Ki J. Med. Chem. (1997) 40: 2053-2063 [PMID:9207947]
ChEMBL The compound was tested for its ability to inhibit [3H]Gly binding to N-methyl-D-aspartate glutamate receptor from rat whole brain. B 4 pKi >100000 nM Ki J. Med. Chem. (1997) 40: 2053-2063 [PMID:9207947]
ChEMBL Binding affinity of compound against NMDA receptor binding site in rat brain membrane using [3H]glutamate as radioligand B 4 pKi >100000 nM Ki J. Med. Chem. (1994) 37: 467-475 [PMID:8120865]
ChEMBL Binding affinity of compound against strychnine-insensitive glycine site on NMDA receptor in rat brain membrane using [3H]glycine as radioligand B 4 pKi >100000 nM Ki J. Med. Chem. (1994) 37: 467-475 [PMID:8120865]
ChEMBL Binding affinity towards NMDA receptor was determined in rat whole brain membrane using NMDA-sensitive [3H]Glu as radioligand B 4 pKi >100000 nM Ki J. Med. Chem. (1996) 39: 3971-3979 [PMID:8831762]
ChEMBL Binding affinity against glycine binding site of NMDA receptor using [3H]glycine B 4.48 pKi 33000 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 2441-2446
ChEMBL Inhibition of NMDA receptor glycine site from rat cortical membrane B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2010) 53: 5367-5382 [PMID:20356304]
ChEMBL Inhibition of NMDA receptor glutamate site from rat cortical membrane B 4.05 pIC50 >90000 nM IC50 J. Med. Chem. (2010) 53: 5367-5382 [PMID:20356304]
ChEMBL Binding affinity for N-methyl-D-aspartate glutamate receptor B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 2749-2754 [PMID:11133083]
ChEMBL Inhibition of [3H]CPP binding to rat N-methyl-D-aspartate glutamate receptor B 5 pIC50 >10000 nM IC50 J. Med. Chem. (1992) 35: 4720-4726 [PMID:1361582]
ChEMBL In vitro binding affinity towards NMDA glutamate receptor using [3H]5,7-dichlorokynurenate as ligand on rat cortical membrane preparations B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 127-132 [PMID:11206442]
ChEMBL Displacement of [3H]DCKA from N-methyl-D-aspartate glutamate receptor of rat cortical membrane B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 1133-1137 [PMID:10843235]
ChEMBL Inhibition of [3H]-(+)-MK-801 binding to NMDA receptor ion-channel complex of rat cortical memembranes B 6.7 pIC50 200 nM IC50 J. Med. Chem. (2001) 44: 3157-3165 [PMID:11543685]
GluN2C/Glutamate [NMDA] receptor subunit epsilon 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL401] [GtoPdb: 458] [UniProtKB: Q00961]
ChEMBL Ability to displace [3H]glycine from NMDA receptor B 4.48 pKi 33000 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 1101-1106
ChEMBL Compound was tested for binding affinity against glycine site of NMDA receptor using [3H]glycine as a radioligand. B 4.48 pKi 33000 nM Ki Bioorg. Med. Chem. Lett. (1996) 6: 2887-2892
GluN1/Glutamate (NMDA) receptor subunit zeta 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL330] [GtoPdb: 455] [UniProtKB: P35439]
ChEMBL Binding affinity towards glycine binding site on NMDA receptor was determined in rat whole brain membrane using strychnine-insensitive [3H]Gly as radioligand B 4 pKi >100000 nM Ki J. Med. Chem. (1996) 39: 3971-3979 [PMID:8831762]
ChEMBL Affinity for N-methyl-D-aspartate glutamate receptor 1 in rat brain synaptic membranes, using [3H]glycine as radioligand B 4 pIC50 >100000 nM IC50 J. Med. Chem. (1995) 38: 3720-3740 [PMID:7562904]
ChEMBL Affinity for N-methyl-D-aspartate glutamate receptor 1 in rat brain synaptic membranes, using [3H]glycine as radioligand B 4 pIC50 >100000 nM IC50 J. Med. Chem. (1995) 38: 3720-3740 [PMID:7562904]
GluA1/GluA2/GluA3/GluA4/Glutamate receptor ionotropic AMPA in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2096670] [GtoPdb: 444445446447] [UniProtKB: P42261P42262P42263P48058]
ChEMBL Displacement of [3H]AMPA from AMPA receptor B 7.15 pKi 70 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 1101-1106
ChEMBL In vitro binding affinity against AMPA receptor by [3H]AMPA displacement. B 7.15 pKi 70 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 2441-2446
ChEMBL Tested for the affinity to the Ionotropic glutamate receptor AMPA using [3H]-AMPA as radioligand B 6.7 pIC50 200 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 77-80
ChEMBL Binding affinity against AMPA receptor using [3H]- AMPA radioligand B 7.28 pIC50 52 nM IC50 Bioorg. Med. Chem. Lett. (1997) 7: 1437-1442
GluA1/GluA2/GluA4/GluA3/Glutamate receptor ionotropic, AMPA in Mouse (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2096617] [GtoPdb: 444445447446] [UniProtKB: P23818P23819Q9Z2W8Q9Z2W9]
ChEMBL Compound was tested for binding affinity against Ionotropic glutamate receptor AMPA using [3H]AMPA as a radioligand. B 7.15 pKi 70 nM Ki Bioorg. Med. Chem. Lett. (1996) 6: 2887-2892
ChEMBL Antagonist activity against AMPA receptor assessed as inhibition of SAMPA-induced depolarization of mouse cortex F 6.7 pIC50 200 nM IC50 J. Med. Chem. (2006) 49: 6015-6026 [PMID:17004715]
GluA1/GluA2/GluA3/GluA4/Glutamate receptor ionotropic, AMPA in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093871] [GtoPdb: 444445446447] [UniProtKB: P19490P19491P19492P19493]
ChEMBL Inhibitory concentration of compound for depolarization induced by 5 uM S-AMPA in mouse cortical wedge preparation B 6.7 pKi 200 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 2345-2349 [PMID:15081038]
ChEMBL Binding affinity towards ionotropic glutamate receptor (high-affinity) of rat cortical synaptic membranes by using [3H]AMPA as radioligand B 7.15 pKi 70 nM Ki J. Med. Chem. (2004) 47: 262-272 [PMID:14695840]
ChEMBL Binding affinity at ionotropic glutamate receptor AMPA in rat cortical membranes [3H]AMPA displacement. B 7.15 pKi 70 nM Ki J. Med. Chem. (2001) 44: 3157-3165 [PMID:11543685]
ChEMBL Compound was evaluated for inhibition of binding of [3H]AMPA to specific binding at Ionotropic glutamate receptor AMPA in rat cortical membrane B 7.15 pKi 70 nM Ki J. Med. Chem. (2000) 43: 3824-3826 [PMID:11052786]
ChEMBL Binding affinity for ionotropic glutamate receptor AMPA using [3H]AMPA as radioligand, bound to synaptic membranes prepared from rat cerebral cortex B 7.19 pKi 65 nM Ki Bioorg. Med. Chem. Lett. (2003) 13: 3521-3525 [PMID:14505662]
ChEMBL Binding affinity against AMPA receptor in rat brain membrane using [3H]-AMPA as radioligand B 7.22 pKi 60 nM Ki J. Med. Chem. (1994) 37: 467-475 [PMID:8120865]
ChEMBL Displacement binding affinity against Ionotropic glutamate receptor AMPA was determined B 7.22 pKi 60 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 1203-1205 [PMID:10866381]
ChEMBL The compound was tested for its ability to inhibit [3H]AMPA binding to Ionotropic glutamate receptor AMPA from rat whole brain B 7.22 pKi 60 nM Ki J. Med. Chem. (1997) 40: 2053-2063 [PMID:9207947]
ChEMBL Binding affinity towards Ionotropic glutamate receptor AMPA was determined in rat whole brain membrane using [3H]AMPA as radioligand B 7.22 pKi 60 nM Ki J. Med. Chem. (1996) 39: 3971-3979 [PMID:8831762]
ChEMBL Antagonistic activity against Ionotropic glutamate receptor AMPA induced LDH release in cultured rat cortical neurons after 24 hr 100 uM AMPA F 5.52 pIC50 3000 nM IC50 J. Med. Chem. (1995) 38: 3720-3740 [PMID:7562904]
ChEMBL Binding affinity towards AMPA receptor to rat neocortical membrane using [3H]AMPA as radioligand B 5.52 pIC50 3000 nM IC50 Bioorg. Med. Chem. Lett. (1994) 4: 371-376
ChEMBL Antagonist potency against functional AMPA receptor by kainate-induced Ca+2 in rat cerebellar granule neurons in primary culture F 5.62 pIC50 2400 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 1203-1205 [PMID:10866381]
ChEMBL Inhibition of Ca 2+ Influx in cultured rat cerebellar granule cells, mediated by ionotropic glutamate receptor AMPA F 5.62 pIC50 2400 nM IC50 J. Med. Chem. (2001) 44: 1710-1717 [PMID:11356106]
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 Antagonist activity on AMPA receptor expressed on rat motoneurons by its ability to reduce the fast component dorsal root evoked ventral root potential (fDR-VRP) F 6.67 pIC50 214 nM IC50 J. Med. Chem. (2005) 48: 7867-7881 [PMID:16302825]
ChEMBL Inhibitory activity against AMPA receptor currents in rat cortical cells stimulated with 50 uM kainic acid F 6.85 pIC50 140 nM IC50 J. Med. Chem. (1996) 39: 343-346 [PMID:8558499]
ChEMBL Displacement of [3H]AMPA from Ionotropic glutamate receptor AMPA of rat cortical membranes B 6.85 pIC50 140 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 1133-1137 [PMID:10843235]
ChEMBL Affinity towards Ionotropic glutamate receptor AMPA using [3H]AMPA as ligand on rat cortical membrane preparations B 6.85 pIC50 140 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 127-132 [PMID:11206442]
ChEMBL Binding affinity for Ionotropic glutamate receptor AMPA B 6.85 pIC50 140 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 2749-2754 [PMID:11133083]
ChEMBL Inhibition of Ionotropic glutamate receptor AMPA induced depolarization in rat cortical wedge by application of 10 uM of AMPA B 6.92 pIC50 120 nM IC50 J. Med. Chem. (1995) 38: 3720-3740 [PMID:7562904]
ChEMBL Tested for the inhibition of binding of [3H]AMPA radioligand to Ionotropic glutamate receptor AMPA to cortical membranes from rat brain B 7 pIC50 100 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 105-106
ChEMBL The compound was tested for its affinity against AMPA receptor in rats B 7 pIC50 100 nM IC50 J. Med. Chem. (1992) 35: 4720-4726 [PMID:1361582]
ChEMBL Inhibition of binding of [3H]AMPA to the binding sites of Ionotropic glutamate receptor AMPA in rat cortical membranes, at 32 uM conc. B 7.15 pIC50 70 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 443-446 [PMID:12565947]
ChEMBL Binding affinity was determined against ionotropic glutamate receptor AMPA in rat brain synaptic membranes using [3H]AMPA as radioligand B 7.28 pIC50 52 nM IC50 J. Med. Chem. (1995) 38: 3720-3740 [PMID:7562904]
ChEMBL Binding affinity in rat brain cortical membranes by the displacement of [3H]AMPA at Ionotropic glutamate receptor AMPA B 7.28 pIC50 52 nM IC50 J. Med. Chem. (1997) 40: 3679-3686 [PMID:9357535]
ChEMBL Inhibitory concentration required for antagonistic activity against AMPA receptor in rat neuronal cultures F 7.28 pIC50 52 nM IC50 Bioorg. Med. Chem. Lett. (1997) 7: 1979-1984
ChEMBL Binding affinity was determined against ionotropic glutamate receptor AMPA in rat brain synaptic membranes using [3H]AMPA as radioligand B 7.28 pIC50 52 nM IC50 J. Med. Chem. (1995) 38: 3720-3740 [PMID:7562904]
ChEMBL Antagonistic activity against Ionotropic glutamate receptor AMPA using kainate-evoked current in Xenopus oocytes injected with rat brain mRNA F 7.51 pIC50 31 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 2749-2754 [PMID:11133083]
ChEMBL Ability to block kainate-induced 45 [Ca2+] influx through functional assay of Ionotropic glutamate receptor AMPA activity in rat cerebellar granule cells. F 9.3 pIC50 0.5 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 177-181 [PMID:11206453]
GluA1/Glutamate receptor ionotropic, AMPA 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261]
ChEMBL Ability to displace binding of [3H]AMPA to recombinant human Ionotropic glutamate receptor AMPA 1 B 5.8 pKi 1600 nM Ki J. Med. Chem. (2002) 45: 4383-4386 [PMID:12238915]
ChEMBL Inhibition of glutamate-induced calcium influx in HEK293 cells expressing human GLUA1 F 5.22 pIC50 6000 nM IC50 J. Med. Chem. (2006) 49: 2579-2592 [PMID:16610801]
GluA2/Glutamate receptor ionotropic, AMPA 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262]
ChEMBL Ability to displace binding of [3H]AMPA to recombinant human Ionotropic glutamate receptor AMPA 2 B 6.59 pKi 260 nM Ki J. Med. Chem. (2002) 45: 4383-4386 [PMID:12238915]
ChEMBL Inhibition of [3H]-AMPA binding to human GluR2 receptors expressed in HEK 293 cells B 6.68 pKi 210 nM Ki J. Med. Chem. (2005) 48: 4200-4203 [PMID:15974569]
ChEMBL Inhibition of glutamate-induced calcium influx in HEK293 cells expressing human GLUA2 F 5.6 pIC50 2500 nM IC50 J. Med. Chem. (2006) 49: 2579-2592 [PMID:16610801]
ChEMBL Antagonist activity at human recombinant GLUA2-AMPA receptor expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay F 5.6 pIC50 2500 nM IC50 J. Med. Chem. (2007) 50: 1558-1570 [PMID:17348638]
GluA3/Glutamate receptor ionotropic, AMPA 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3595] [GtoPdb: 446] [UniProtKB: P42263]
ChEMBL Ability to displace binding of [3H]AMPA to recombinant human Ionotropic glutamate receptor AMPA 3 B 6.05 pKi 900 nM Ki J. Med. Chem. (2002) 45: 4383-4386 [PMID:12238915]
ChEMBL Inhibition of glutamate-induced calcium influx in HEK293 cells expressing human GLUA3 F 5.72 pIC50 1900 nM IC50 J. Med. Chem. (2006) 49: 2579-2592 [PMID:16610801]
GluA4/Glutamate receptor ionotropic, AMPA 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3190] [GtoPdb: 447] [UniProtKB: P48058]
ChEMBL Ability to displace binding of [3H]AMPA to recombinant human Ionotropic glutamate receptor AMPA 4 B 6.22 pKi 600 nM Ki J. Med. Chem. (2002) 45: 4383-4386 [PMID:12238915]
ChEMBL Inhibition of glutamate-induced calcium influx in HEK293 cells expressing human GLUA4 F 5.96 pIC50 1100 nM IC50 J. Med. Chem. (2006) 49: 2579-2592 [PMID:16610801]
GluK1/GluK2/GluK3/GluK4/GluK5/Glutamate receptor ionotropic kainate in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2109241] [GtoPdb: 450451452453454] [UniProtKB: P39086Q13002Q13003Q16099Q16478]
ChEMBL Ability to displace [3H]kainate from kainate receptor B 5.59 pKi 2600 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 1101-1106
ChEMBL Compound was tested for binding affinity against Ionotropic glutamate receptor kainate using [3H]kainate as a radioligand. B 5.59 pKi 2600 nM Ki Bioorg. Med. Chem. Lett. (1996) 6: 2887-2892
ChEMBL The compound was tested for binding affinity against Kainate binding site using [3H]kainate as radioligand. B 5.59 pKi 2600 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 2441-2446
ChEMBL Tested for the affinity for the Ionotropic glutamate receptor kainate using [3H]kainate as radioligand B 5.1 pIC50 8000 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 77-80
GluK1/GluK2/GluK3/GluK4/GluK5/Glutamate receptor ionotropic, kainate in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094119] [GtoPdb: 450451452453454] [UniProtKB: P22756P42260P42264Q01812Q63273]
ChEMBL Binding affinity against kainate receptor in rat brain membrane using [3H]kainate as radioligand B 5.39 pKi 4100 nM Ki J. Med. Chem. (1994) 37: 467-475 [PMID:8120865]
ChEMBL Binding affinity towards Ionotropic glutamate receptor kainate was determined in rat cortical membrane using [3H]KA as radioligand B 5.39 pKi 4100 nM Ki J. Med. Chem. (1996) 39: 3971-3979 [PMID:8831762]
ChEMBL Inhibition concentration towards high-affinity ionotropic glutamate receptor kainate of rat cortical membranes by using [3H]KA as radioligand B 5.15 pIC50 7000 nM IC50 J. Med. Chem. (2004) 47: 262-272 [PMID:14695840]
ChEMBL Compound was evaluated for inhibition of binding of [3H]KA to specific binding at Ka receptor in rat cortical membrane B 5.15 pIC50 7000 nM IC50 J. Med. Chem. (2000) 43: 3824-3826 [PMID:11052786]
ChEMBL Inhibition of [3H]KA binding to kainate receptor of rat brain membranes B 5.15 pIC50 7000 nM IC50 J. Med. Chem. (2001) 44: 3157-3165 [PMID:11543685]
ChEMBL Tested for the inhibition of binding of [3H]kainate radioligand to Ionotropic glutamate receptor kainate of cortical membranes from rat brain B 5.36 pIC50 4400 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 105-106
ChEMBL Antagonistic activity against Ionotropic glutamate receptor kainate induced LDH release in cultured cortical neurons in rat after 24 hr application of 500 uM of kainate F 5.7 pIC50 2000 nM IC50 J. Med. Chem. (1995) 38: 3720-3740 [PMID:7562904]
ChEMBL Inhibition concentration towards low-affinity Ionotropic glutamate receptor kainate of rat cortical membranes by using [3H]-KA as radioligand B 5.82 pIC50 1500 nM IC50 J. Med. Chem. (2004) 47: 262-272 [PMID:14695840]
ChEMBL Antagonistic activity against rat ionotropic glutamate receptor ionotropic kainate in xenopus oocytes F 7.05 pIC50 90 nM IC50 J. Med. Chem. (1996) 39: 197-206 [PMID:8568808]
ChEMBL Binding affinity for the ionotropic glutamate receptor kainate in rat brain synaptic membranes using [3H]kainate as radioligand B 7.1 pIC50 79 nM IC50 J. Med. Chem. (1995) 38: 3720-3740 [PMID:7562904]
ChEMBL Binding affinity for the ionotropic glutamate receptor kainate in rat brain synaptic membranes using [3H]kainate as radioligand B 7.1 pIC50 79 nM IC50 J. Med. Chem. (1995) 38: 3720-3740 [PMID:7562904]
ChEMBL Inhibitory activity against [3H]AMPA binding to rat cortical membranes B 7.22 pIC50 60 nM IC50 J. Med. Chem. (1996) 39: 197-206 [PMID:8568808]
ChEMBL Inhibitory activity against generation of currents by 50 uM kainate in Xenopus oocytes injected with rat brain mRNA F 7.51 pIC50 31 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 1133-1137 [PMID:10843235]
GluK1/Glutamate receptor ionotropic kainate 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1918] [GtoPdb: 450] [UniProtKB: P39086]
ChEMBL Inhibition of [3H]-KA binding to iontropic glutamate receptor 5 B 4.93 pKi 11730 nM Ki J. Med. Chem. (2005) 48: 4200-4203 [PMID:15974569]
ChEMBL Antagonist activity at human recombinant GLUK5/GLUK2 expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay F 4.3 pIC50 50000 nM IC50 J. Med. Chem. (2007) 50: 1558-1570 [PMID:17348638]
ChEMBL Inhibition of glutamate-induced calcium influx in HEK293 cells expressing human GLUK5 by FLIPR assay F 4.43 pIC50 37000 nM IC50 J. Med. Chem. (2006) 49: 2579-2592 [PMID:16610801]
ChEMBL Antagonist activity at human recombinant GLUK5 receptor expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay F 4.43 pIC50 37000 nM IC50 J. Med. Chem. (2007) 50: 1558-1570 [PMID:17348638]
GluK1/Glutamate receptor ionotropic kainate 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2919] [GtoPdb: 450] [UniProtKB: P22756]
ChEMBL Antagonism on GLUK5 containing kainate induced depolarization of isolated neonatal rat dorsal root C-fibers F 5.75 pKd 1780 nM Kd J. Med. Chem. (2005) 48: 7867-7881 [PMID:16302825]
GluK2/Glutamate receptor ionotropic kainate 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3683] [GtoPdb: 451] [UniProtKB: Q13002]
ChEMBL Ability to displace binding of [3H]KA to recombinant human KA receptor Ionotropic glutamate receptor ionotropic kainate 2 expressed in EK 293 cell membranes B 4 pKi >100000 nM Ki J. Med. Chem. (2002) 45: 4383-4386 [PMID:12238915]
ChEMBL Ability to displace binding of [3H]AMPA to recombinant human AMPA receptor Ionotropic glutamate receptor ionotropic kainate 2 B 4.88 pKi 13200 nM Ki J. Med. Chem. (2002) 45: 4383-4386 [PMID:12238915]
ChEMBL Inhibition of [3H]KA binding to iontropic glutamate receptor 6 B 4.88 pKi 13200 nM Ki J. Med. Chem. (2005) 48: 4200-4203 [PMID:15974569]
ChEMBL Inhibition of glutamate-induced calcium influx in HEK293 cells expressing human GLUK6 F 4.54 pIC50 29000 nM IC50 J. Med. Chem. (2006) 49: 2579-2592 [PMID:16610801]
ChEMBL Antagonist activity at human recombinant GLUK6 expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay F 4.54 pIC50 29000 nM IC50 J. Med. Chem. (2007) 50: 1558-1570 [PMID:17348638]
GluK3/Glutamate receptor ionotropic kainate 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3684] [GtoPdb: 452] [UniProtKB: Q13003]
ChEMBL Displacement of [3H]kainate from human GLUK7 receptor expressed in HEK293 cells B 4.74 pKi 18000 nM Ki J. Med. Chem. (2005) 48: 7867-7881 [PMID:16302825]
ChEMBL Displacement of [3H]kainate from human GLUK7 receptor expressed in HEK293 cells B 4.36 pIC50 44000 nM IC50 J. Med. Chem. (2005) 48: 7867-7881 [PMID:16302825]
GluK5/Glutamate receptor ionotropic kainate 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4041] [GtoPdb: 454] [UniProtKB: Q63273]
ChEMBL Antagonist activity against GLUK5-containing kainate receptor by inhibition of kainate-induced depolarization of neonatal rat dorsal root fibers F 5.75 pKd 1780 nM Kd J. Med. Chem. (2006) 49: 2579-2592 [PMID:16610801]
mGlu6 receptor/Metabotropic glutamate receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4573] [GtoPdb: 294] [UniProtKB: O15303]
ChEMBL Antagonist activity at human recombinant GluR6 expressed in HEK cells coexpressing aequorine assessed as inhibition of glutamate-induced Ca2+ influx at 10 uM by luminescence reporter assay F 4.13 pIC50 74000 nM IC50 Eur. J. Med. Chem. (2010) 45: 69-77 [PMID:19819046]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]