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 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]
