memantine [Ligand Id: 4253] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL807 (D-145, DRG-0267, Memantine, Namenda, NSC-757843) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Acetylcholinesterase in Electrophorus electricus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4078] [UniProtKB: O42275] | ||||||||
| ChEMBL | Inhibition of electric eel AChE by modified Ellman's method | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2010) 53: 3611-3617 [PMID:20361801] |
| acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303] | ||||||||
| ChEMBL | Inhibition of recombinant human AChE expressed in HEK293 cells by Ellman's method | B | 8.31 | pIC50 | 4.9 | nM | IC50 | Bioorg Med Chem (2021) 46: 116355-116355 [PMID:34391122] |
| Cholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5763] [UniProtKB: P81908] | ||||||||
| ChEMBL | Inhibition of equine serum BChE by modified Ellman's method | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2010) 53: 3611-3617 [PMID:20361801] |
| 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 | Binding affinity to NMDA receptor (unknown origin) | B | 5.92 | pKi | 1200 | nM | Ki | Medchemcomm (2010) 1: 87-102 |
| ChEMBL | The compound was tested for its ability to block PCP N-methyl-D-aspartate glutamate receptor at the PCP (phencyclidine) binding site in postmortem human frontal cortex. | B | 6.27 | pKi | 540 | nM | Ki | J Med Chem (1998) 41: 393-400 [PMID:9464369] |
| ChEMBL | Binding affinity to NMDAR (unknown origin) | B | 6.27 | pKi | 540 | nM | Ki | Eur J Med Chem (2020) 194: 112242-112242 [PMID:32248004] |
| GluN2D/GluN3B/GluN1/GluN2A/GluN2B/GluN2C/GluN3A in Rat [GtoPdb: 459, 461, 455, 456, 457, 458, 460] [UniProtKB: Q62645, Q8VHN2, P35439, Q00959, Q00960, Q00961, Q9R1M7] | ||||||||
| GtoPdb | - | - | 6.15 | pKi | 700 | nM | Ki | J Med Chem (1999) 42: 1481-500 [PMID:10229619] |
| 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] | ||||||||
| GtoPdb | - | - | 6.15 | pKi | 700 | nM | Ki | J Med Chem (1999) 42: 1481-500 [PMID:10229619] |
| ChEMBL | Inhibition of NMDA receptor in rat cerebellar granule neurons assessed as glutamate-induced intracellular calcium increase | B | 4.26 | pIC50 | 55400 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 6156-6160 [PMID:18947998] |
| ChEMBL | Antagonist activity at NMDA receptor in rat cerebellar granule neurons assessed as inhibition of glutamate-induced increase in intracellular calcium level by fluorometric assay | F | 4.26 | pIC50 | 55000 | nM | IC50 | Bioorg Med Chem (2010) 18: 46-57 [PMID:19954985] |
| ChEMBL | Antagonist activity at NMDA receptor in cerebellar granule neurons assessed as inhibition of glutamate-induced increase in intracellular calcium concentration by fluorometric assay | F | 4.26 | pIC50 | 55000 | nM | IC50 | Bioorg Med Chem (2008) 16: 9925-9936 [PMID:18954995] |
| ChEMBL | Antagonist activity at NMDAR in embryonic cultures of rat cortical neuron assessed as inhibition of NMDA-induced calcium influx preincubated for 10 mins followed by NMDA addition by Fluo-4/AM dye based fluorescence assay | B | 4.52 | pIC50 | 30000 | nM | IC50 | Eur J Med Chem (2020) 194: 112242-112242 [PMID:32248004] |
| ChEMBL | Antagonist activity at NMDA receptor in rat CGN cells assessed as increase in intracellular calcium level incubated for 30 mins in presence of Fura-2AM followed by NMDA/glycine stimulation by fluorescence spectrometer analysis | B | 5.82 | pIC50 | 1500 | nM | IC50 | Eur J Med Chem (2019) 180: 613-626 [PMID:31351393] |
| ChEMBL | Antagonist activity at NMDA receptor in rat cerebellar granule neurons assessed as inhibition of NMDA-induced increase in intracellular calcium level by fluorometric assay | F | 5.82 | pIC50 | 1500 | nM | IC50 | Bioorg Med Chem (2010) 18: 46-57 [PMID:19954985] |
| ChEMBL | Antagonist activity at NMDA receptor in cerebellar granule neurons assessed as inhibition of NMDA-induced increase in intracellular calcium concentration by fluorometric assay | F | 5.82 | pIC50 | 1500 | nM | IC50 | Bioorg Med Chem (2008) 16: 9925-9936 [PMID:18954995] |
| ChEMBL | Inhibition of NMDA receptor in rat cerebellar granule neurons assessed as NMDA-induced intracellular calcium increase | B | 5.82 | pIC50 | 1500 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 6156-6160 [PMID:18947998] |
| ChEMBL | Antagonist activity against NMDA receptor in rat cerebellar granule neurons assessed as inhibition of NMDA -induced increase in intracellular calcium level by Fura-2 AM dye based fluorimetry | F | 5.82 | pIC50 | 1500 | nM | IC50 | Bioorg Med Chem (2009) 17: 3198-3206 [PMID:19251424] |
| ChEMBL | Displacement of [3H]MK-801 from NMDA receptor in Wistar rat brain membranes by scintillation counting analysis | B | 5.96 | pIC50 | 1090 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4131-4135 [PMID:26296478] |
| GluN1/GluN2A/Glutamate NMDA receptor; GRIN1/GRIN2A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907604] [GtoPdb: 455, 456] [UniProtKB: Q05586, Q12879] | ||||||||
| ChEMBL | Inhibition of human GluN1-1a/NR2A receptor expressed in transgenic mouse fibroblast cells assessed as inhibition of L-glutamate-induced excitotoxicity by measuring LDH activity by cell based assay | B | 5.17 | pIC50 | 6700 | nM | IC50 | Bioorg Med Chem (2021) 46: 116355-116355 [PMID:34391122] |
| ChEMBL | Inhibition of dexamethasone-induced human NR1-1a/NR2A receptor-mediated excitotoxicity in (S)-glutamate/glycine-stimulated mouse L12-G10 cells assessed as LDH release after 30 mins | B | 5.25 | pIC50 | 5600 | nM | IC50 | J Med Chem (2010) 53: 3611-3617 [PMID:20361801] |
| ChEMBL | Inhibition of human NR1-1a/NR2A expressed in mouse L12-G10 cells assessed as inhibition of glutamate-induced excitotoxicity incubated for 16 hrs by LDH release assay | B | 5.36 | pIC50 | 4400 | nM | IC50 | J Med Chem (2015) 58: 6710-6715 [PMID:26278660] |
| ChEMBL | Antagonist activity at NR1/NR2A receptor (unknown origin) expressed in Xenopus laevis oocytes assessed as inhibition of glutamate/glycine-induced current at pH 7.6 at -40mV holding potential by two-electrode voltage-clamp electrophysiology | B | 5.36 | pIC50 | 4360 | nM | IC50 | Bioorg Med Chem (2014) 22: 1983-1992 [PMID:24630693] |
| ChEMBL | Antagonist activity at recombinant NR1/NR2A receptor expressed in Xenopus laevis oocytes | F | 6.04 | pIC50 | 911 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 4729-4732 [PMID:17624774] |
| ChEMBL | Antagonist activity at recombinant GluN1/GluN2A receptor (unknown origin) expressed in Xenopus laevis oocytes assessed as inhibition of glycine/glutamate-induced inward current at -70mV by two-electrode voltage clamp assay | B | 9.02 | pIC50 | 0.95 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3901-3904 [PMID:23692871] |
| GluN1/GluN2B/Glutamate NMDA receptor; GRIN1/GRIN2B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907603] [GtoPdb: 455, 457] [UniProtKB: Q05586, Q13224] | ||||||||
| ChEMBL | Inhibition of recombinant GluN1/GluN2B receptor (unknown origin) expressed in HEK293 cells by patch-clamp method | B | 6 | pKi | 1000 | nM | Ki | Eur J Med Chem (2019) 180: 613-626 [PMID:31351393] |
| ChEMBL | Inhibition of NMDA NR1/NR2B receptor expressed in xenopus oocytes assessed as inhibition of NMDA and glycine-induced current response by two-electrode voltage clamp assay | B | 5.02 | pIC50 | 9520 | nM | IC50 | J Med Chem (2008) 51: 4381-4384 [PMID:18605718] |
| ChEMBL | Inhibition of dexamethasone-induced human NR1-1a/NR2B receptor-mediated excitotoxicity in (S)-glutamate/glycine-stimulated mouse L13-E6 cells assessed as LDH release after 30 mins | B | 5.26 | pIC50 | 5500 | nM | IC50 | J Med Chem (2010) 53: 3611-3617 [PMID:20361801] |
| ChEMBL | Inhibition of human NR1-1a/NR2B expressed in mouse L13-E6 cells assessed as inhibition of glutamate-induced excitotoxicity incubated for 16 hrs by LDH release assay | B | 5.28 | pIC50 | 5200 | nM | IC50 | J Med Chem (2015) 58: 6710-6715 [PMID:26278660] |
| ChEMBL | Antagonist activity at recombinant NR1/NR2B receptor expressed in Xenopus laevis oocytes | F | 5.99 | pIC50 | 1020 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 4729-4732 [PMID:17624774] |
| GluN2B/Glutamate [NMDA] receptor subunit epsilon 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL311] [GtoPdb: 457] [UniProtKB: Q00960] | ||||||||
| ChEMBL | Displacement of [3H]Ifenprodil from NMDAR-2B in Sprague-Dawley rat frontal cortex homogenates after 2 hrs by liquid scintillation counting | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (2012) 55: 9708-9721 [PMID:23033965] |
| GluN2C/Glutamate [NMDA] receptor subunit epsilon 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL401] [GtoPdb: 458] [UniProtKB: Q00961] | ||||||||
| GtoPdb | - | - | 6.15 | pKi | 700 | nM | Ki | J Med Chem (1999) 42: 1481-500 [PMID:10229619] |
| ChEMBL | Compound with the N-methyl-D-aspartate glutamate receptor blocking activity | B | 6.15 | pKi | 700 | nM | Ki | J Med Chem (1999) 42: 1481-1500 [PMID:10229619] |
| nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α6 subunit/Nicotinic acetylcholine receptor alpha6/alpha3/beta4 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3137276] [GtoPdb: 464, 474, 467] [UniProtKB: P04757, P12392, P43143] | ||||||||
| ChEMBL | Inhibition of human GluN1-1a/NR2B receptor expressed in transgenic mouse fibroblast cells assessed as inhibition of L-glutamate-induced excitotoxicity by measuring LDH activity by cell based assay | B | 5.22 | pIC50 | 6000 | nM | IC50 | Bioorg Med Chem (2021) 46: 116355-116355 [PMID:34391122] |
| Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245] | ||||||||
| ChEMBL | Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy | B | 4.57 | pIC50 | 27200 | nM | IC50 | J Med Chem (2008) 51: 5932-5942 [PMID:18788725] |
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]
