5,7-dichlorokynurenic acid [Ligand Id: 2361] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL50267 (5,7-Dichlorokynurenic Acid)
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  • GluN1/Glutamate (NMDA) receptor subunit zeta 1 in Rat [ChEMBL: CHEMBL330] [GtoPdb: 455] [UniProtKB: P35439]
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  • glycine receptor α2 subunit in Human [GtoPdb: 424] [UniProtKB: P23416]
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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 7.17 pIC50 68 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 Inhibitory concentration of compound for depolarization induced by 5 uM NMDA in mouse cortical wedge preparation B 5.33 pKi 4700 nM Ki Bioorg Med Chem Lett (2004) 14: 2345-2349 [PMID:15081038]
ChEMBL Ability to displace [3H]glycine from NMDA receptor in rat corticaln membranes B 7.05 pKi 90 nM Ki J Med Chem (2001) 44: 3157-3165 [PMID:11543685]
ChEMBL Displacement of [3H]glycine from NMDA receptor in rat cortical synaptical membrane B 7.1 pKi 80 nM Ki Eur J Med Chem (2012) 54: 470-482 [PMID:22704999]
ChEMBL Affinity for the glycine binding site of NMDA receptor by inhibition of [3H]5,7-dichlorokynurenic acid ([3H]DCKA) binding to rat brain synaptic membrane B 7.4 pKi 40 nM Ki J Med Chem (1994) 37: 3956-3968 [PMID:7966156]
ChEMBL Inhibition of [3H]-glutamate binding to N-methyl-D-aspartate glutamate receptor of rat cortical membranes B 4 pIC50 >100000 nM IC50 J Med Chem (1991) 34: 1243-1252 [PMID:1826744]
ChEMBL Binding activity against N-methyl-D-aspartate glutamate receptor in rat brain homogenate using [3H]CPP as the radioligand. B 4.43 pIC50 37000 nM IC50 J Med Chem (1990) 33: 3130-3132 [PMID:2147957]
ChEMBL Activity against rat cortical and hippocampal membrane N-methyl-D-aspartate glutamate receptor 1/2A/2B/2C/2D using [3H]CPP B 4.92 pIC50 12000 nM IC50 J Med Chem (1990) 33: 2944-2946 [PMID:2146391]
ChEMBL Tested for the ability to inhibit [3H]MK-801 binding to NMDA receptor of rat cortical membranes in the presence of glutamate (1 uM) B 6.07 pIC50 860 nM IC50 Bioorg Med Chem Lett (1993) 3: 81-84
ChEMBL Inhibition of [3H]glycine binding to glycine site of N-methyl-D-aspartate glutamate receptor in rat cortical membranes B 6.7 pIC50 200 nM IC50 J Med Chem (1991) 34: 1243-1252 [PMID:1826744]
ChEMBL Concentration required to inhibit 50% of the specific binding of [3H]glycine to NMDA receptor prepared from rat cerebral cortex and hippocampus B 6.7 pIC50 200 nM IC50 J Med Chem (1992) 35: 1942-1953 [PMID:1534583]
ChEMBL In vitro inhibition of [3H]glycine at NMDA receptor B 6.7 pIC50 200 nM IC50 J Med Chem (1994) 37: 4053-4067 [PMID:7990104]
ChEMBL Ability to compete with [3H]glycine for strychnine-insensitive binding sites on rat cortical and hippocampal membrane B 6.84 pIC50 143 nM IC50 J Med Chem (1992) 35: 1791-1799 [PMID:1534125]
ChEMBL Binding activity against N-methyl-D-aspartate glutamate receptor in rat brain homogenate using [3H]-glycine as the radioligand. B 7.1 pIC50 80 nM IC50 J Med Chem (1990) 33: 3130-3132 [PMID:2147957]
ChEMBL Activity against rat cortical and hippocampal membrane strychnine-insensitive N-methyl-D-aspartate glutamate receptor 1 using [3H]-gly B 7.1 pIC50 80 nM IC50 J Med Chem (1990) 33: 2944-2946 [PMID:2146391]
ChEMBL Affinity for the glycine binding site on rat N-methyl-D-aspartate glutamate receptor 1, determined by displacement of the glycine site antagonist [3H]L-689,560 from rat cortical membranes B 7.19 pIC50 64 nM IC50 J Med Chem (1997) 40: 4053-4068 [PMID:9406596]
ChEMBL Displacement of [3H]L-689,560 from NMDA receptor glycine site of rat brain membranes B 7.19 pIC50 64 nM IC50 Bioorg Med Chem Lett (1993) 3: 299-304
ChEMBL Tested for the binding affinity at glycine recognition site of the NMDA receptor in rat cortical membranes using radiolabeled [3H]- L-689 560 B 7.19 pIC50 64 nM IC50 Bioorg Med Chem Lett (1993) 3: 65-70
ChEMBL Binding affinity at the glycine binding site of the N-methyl-D-aspartate glutamate receptor in rat cortical membranes using [3H]dichlorokynurenate ([3H]DCKA) as radioligand B 7.34 pIC50 46 nM IC50 Bioorg Med Chem Lett (1994) 4: 2735-2740
GluN1/Glutamate (NMDA) receptor subunit zeta 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL330] [GtoPdb: 455] [UniProtKB: P35439]
ChEMBL Binding affinity towards N-methyl-D-aspartate glutamate receptor 1 (high affinity) of rat cortical synaptic membranes by using [3H]Gly as radioligand B 7.05 pKi 90 nM Ki J Med Chem (2004) 47: 262-272 [PMID:14695840]
ChEMBL Tested for the ability to displace [3H]glycine, by greater than 50%, from NMDA receptor of rat cortical membranes at a dose of 10 uM B 7.4 pKi 40 nM Ki Bioorg Med Chem Lett (1993) 3: 81-84
ChEMBL Ability to displace strychnine-insensitive [3H]glycine binding to rat cortical membranes. B 7.4 pKi 40 nM Ki J Med Chem (1992) 35: 3423-3425 [PMID:1326635]
ChEMBL Displacement of [3H]glycine from glycine site on the NMDA receptor. B 7.4 pKi 40 nM Ki J Med Chem (1992) 35: 3319-3324 [PMID:1382133]
ChEMBL Inhibition of [3H]-MK-801 binding to a N-methyl-D-aspartic acid(NMDA) receptor in glycine-sensitive rat cortical membranes. B 6.07 pIC50 860 nM IC50 J Med Chem (1992) 35: 3423-3425 [PMID:1326635]
ChEMBL Ability of compound to compete with [3H]glycine for the strychnine-insensitive NMDA receptor glycine binding sites on rat cortical and hippocampus B 6.85 pIC50 140 nM IC50 Bioorg Med Chem Lett (1991) 1: 455-460
ChEMBL Inhibition of specific binding of [3H]glycine to NMDA receptors, in rat cortical membranes at 32 uM conc. B 7.05 pIC50 90 nM IC50 Bioorg Med Chem Lett (2003) 13: 443-446 [PMID:12565947]
ChEMBL Functional antagonism at the N-methyl-D-aspartate glutamate receptor 1 was demonstarted by the ability to inhibit the binding of the channel-blocking agent [3H](+)-MK-801 B 6.48 pEC50 330 nM EC50 J Med Chem (1999) 42: 2478-2484 [PMID:10395489]
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 Tested for the affinity to the Ionotropic glutamate receptor AMPA using [3H]-AMPA as radioligand B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (1993) 3: 77-80
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 4.28 pKi 52000 nM Ki Bioorg Med Chem Lett (2004) 14: 2345-2349 [PMID:15081038]
ChEMBL Displacement of [3H]AMPA from Ionotropic glutamate receptor AMPA. B 5 pKi >10000 nM Ki J Med Chem (1992) 35: 3319-3324 [PMID:1382133]
ChEMBL Binding affinity for Ionotropic glutamate receptor AMPA was determined by the ability to displace [3H]AMPA in rat cortical membranes B 6.3 pKi 500 nM Ki Bioorg Med Chem Lett (1993) 3: 2801-2804
ChEMBL Inhibition of [3H]-AMPA binding to AMPA receptor of rat cortical membrane B 4.12 pIC50 75000 nM IC50 J Med Chem (1991) 34: 1243-1252 [PMID:1826744]
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 Tested for the affinity for the Ionotropic glutamate receptor kainate using [3H]kainate as radioligand B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (1993) 3: 77-80
glycine receptor α2 subunit in Human [GtoPdb: 424] [UniProtKB: P23416]
GtoPdb - - 3.7 pIC50 188000 nM IC50

ChEMBL data shown on this page come from version 32:

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]