Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL299155 (Kynurenic Acid, Transtorine) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 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]