NBQX [Ligand Id: 4264] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL222519 (NBQX) |
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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: 459, 461, 455, 456, 457, 458, 460] [UniProtKB: O15399, O60391, Q05586, Q12879, Q13224, Q14957, Q8TCU5] | ||||||||
| 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: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7] | ||||||||
| 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: 444, 445, 446, 447] [UniProtKB: P42261, P42262, P42263, P48058] | ||||||||
| 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: 444, 445, 447, 446] [UniProtKB: P23818, P23819, Q9Z2W8, Q9Z2W9] | ||||||||
| 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: 444, 445, 446, 447] [UniProtKB: P19490, P19491, P19492, P19493] | ||||||||
| 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: 450, 451, 452, 453, 454] [UniProtKB: P39086, Q13002, Q13003, Q16099, Q16478] | ||||||||
| 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: 450, 451, 452, 453, 454] [UniProtKB: P22756, P42260, P42264, Q01812, Q63273] | ||||||||
| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
