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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| 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 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]
