kynurenic acid [Ligand Id: 2918] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL299155 (Kynurenic Acid, Transtorine)
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  • GluN1/Glutamate (NMDA) receptor subunit zeta 1 in Rat [ChEMBL: CHEMBL330] [GtoPdb: 455] [UniProtKB: P35439]
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  • GPR35/G-protein coupled receptor 35 in Human [ChEMBL: CHEMBL1293267] [GtoPdb: 102] [UniProtKB: Q9HC97]
  • GPR35 in Mouse [GtoPdb: 102] [UniProtKB: Q9ES90]
  • GPR35 in Rat [GtoPdb: 102] [UniProtKB: Q33BM1]
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  • GPR35 in Human [GtoPdb: 102] [UniProtKB: Q9HC97]
  • GPR35 in Mouse [GtoPdb: 102] [UniProtKB: Q9ES90]
  • GPR35/G protein-coupled receptor GPR35 in Rat [ChEMBL: CHEMBL2390812] [GtoPdb: 102] [UniProtKB: Q33BM1]
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  • nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Aryl hydrocarbon receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3201] [GtoPdb: 2951] [UniProtKB: P35869]
ChEMBL Activation of AHR (unknown origin) B 6.52 pEC50 300 nM EC50 J. Med. Chem. (2013) 56: 5182-5197 [PMID:23713606]
GluN2D/GluN3B/GluN1/GluN2A/GluN2B/GluN2C/GluN3A/Glutamate [NMDA] receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094124] [GtoPdb: 459461455456457458460] [UniProtKB: O15399O60391Q05586Q12879Q13224Q14957Q8TCU5]
ChEMBL Inhibition of NMDA receptor (unknown origin) B 4.82 pIC50 15000 nM IC50 J. Med. Chem. (2013) 56: 5182-5197 [PMID:23713606]
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455456457458459461460] [UniProtKB: P35439Q00959Q00960Q00961Q62645Q8VHN2Q9R1M7]
ChEMBL Activity against rat cortical and hippocampal membrane N-methyl-D-aspartate glutamate receptor 1/2A/2B/2C/2D using [3H]CPP B 4.12 pIC50 75000 nM IC50 J. Med. Chem. (1990) 33: 2944-2946 [PMID:2146391]
ChEMBL Binding activity against N-methyl-D-aspartate glutamate receptor in rat brain homogenate using [3H]CPP as the radioligand. B 4.15 pIC50 71000 nM IC50 J. Med. Chem. (1990) 33: 3130-3132 [PMID:2147957]
ChEMBL Inhibition of [3H]glycine binding to glycine site of N-methyl-D-aspartate glutamate receptor in rat cortical membranes B 4.39 pIC50 41000 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 4.39 pIC50 41000 nM IC50 J. Med. Chem. (1992) 35: 1942-1953 [PMID:1534583]
ChEMBL In vitro inhibition of [3H]glycine at NMDA receptor B 4.39 pIC50 41000 nM IC50 J. Med. Chem. (1994) 37: 4053-4067 [PMID:7990104]
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 4.4 pIC50 40250 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 81-84
ChEMBL Ability to compete with [3H]glycine for strychnine-insensitive binding sites on rat cortical and hippocampal membrane B 4.8 pIC50 16000 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 4.8 pIC50 16000 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 4.8 pIC50 16000 nM IC50 J. Med. Chem. (1990) 33: 2944-2946 [PMID:2146391]
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 4.86 pIC50 13800 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 65-70
GluN1/Glutamate (NMDA) receptor subunit zeta 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL330] [GtoPdb: 455] [UniProtKB: P35439]
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 5.27 pKi 5400 nM Ki Bioorg. Med. Chem. Lett. (1993) 3: 81-84
ChEMBL Ability to displace strychnine-insensitive [3H]glycine binding to rat cortical membranes. B 5.27 pKi 5400 nM Ki J. Med. Chem. (1992) 35: 3423-3425 [PMID:1326635]
ChEMBL Inhibition of [3H]-MK-801 binding to a N-methyl-D-aspartic acid(NMDA) receptor in glycine-sensitive rat cortical membranes. B 4.4 pIC50 40200 nM IC50 J. Med. Chem. (1992) 35: 3423-3425 [PMID:1326635]
GPR35/G-protein coupled receptor 35 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293267] [GtoPdb: 102] [UniProtKB: Q9HC97]
ChEMBL Antagonist activity at GPR35 (unknown origin) B 4.41 pIC50 39000 nM IC50 Bioorg Med Chem Lett (2017) 27: 612-615 [PMID:27989666]
ChEMBL Agonist activity at human GPR35 expressed in CHO cells assessed as increase in intracellular Ca2+ measured over 20 secs by Aequorin assay B 4.41 pEC50 39200 nM EC50 J. Med. Chem. (2013) 56: 7084-7099 [PMID:23888932]
GtoPdb - - 4.41 pEC50 - - - J Biol Chem (2006) 281: 22021-8 [PMID:16754668];
J Biomol Screen (2013) 18: 599-609 [PMID:23396314]
GPR35 in Mouse [GtoPdb: 102] [UniProtKB: Q9ES90]
GtoPdb - - 4.96 pEC50 - - - J Biol Chem (2006) 281: 22021-8 [PMID:16754668]
GPR35 in Rat [GtoPdb: 102] [UniProtKB: Q33BM1]
GtoPdb - - 5.15 pEC50 - - - J Biol Chem (2006) 281: 22021-8 [PMID:16754668]
GPR35 in Human [GtoPdb: 102] [UniProtKB: Q9HC97]
GtoPdb - - 4.41 pEC50 - - - J Biol Chem (2006) 281: 22021-8 [PMID:16754668];
J Biomol Screen (2013) 18: 599-609 [PMID:23396314]
GPR35 in Mouse [GtoPdb: 102] [UniProtKB: Q9ES90]
GtoPdb - - 4.96 pEC50 - - - J Biol Chem (2006) 281: 22021-8 [PMID:16754668]
GPR35/G protein-coupled receptor GPR35 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2390812] [GtoPdb: 102] [UniProtKB: Q33BM1]
ChEMBL Agonist activity at rat GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay B 4.18 pEC50 66000 nM EC50 J. Med. Chem. (2013) 56: 5182-5197 [PMID:23713606]
GtoPdb - - 5.15 pEC50 - - - J Biol Chem (2006) 281: 22021-8 [PMID:16754668]
nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544]
ChEMBL Inhibition of alpha7 nAChR (unknown origin) B 5.15 pIC50 7000 nM IC50 J. Med. Chem. (2013) 56: 5182-5197 [PMID:23713606]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]