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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| 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: 459, 461, 455, 456, 457, 458, 460] [UniProtKB: O15399, O60391, Q05586, Q12879, Q13224, Q14957, Q8TCU5] | ||||||||
| 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: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7] | ||||||||
| 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 | F | 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 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]
