memantine [Ligand Id: 4253] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL807 (D-145, DRG-0267, Memantina, Memantine, 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 AChE (unknown origin) | B | 6.11 | pIC50 | 780 | nM | IC50 | Eur J Med Chem (2023) 259: 115670-115670 [PMID:37515920] |
| 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/GluN2A/Glutamate NMDA receptor; Grin1/Grin2a in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096680] [GtoPdb: 455, 456] [UniProtKB: P35439, Q00959] | ||||||||
| ChEMBL | Inhibition of NMDA/glycine-activated rat GluN1/Glu2A expressed in xenopus laevis oocytes at -75 mV holding potential by voltage clamp method | B | 5.58 | pIC50 | 2660 | nM | IC50 | Eur J Med Chem (2023) 261: 115803-115803 [PMID:37734258] |
| ChEMBL | Inhibition of eGFP-tagged rat GluN1-1a/GluN2A transfected in human tsA201 cells assessed as inhibition glutamate-induced current measured at -65 mV holding potential applied for 10 secs by whole-cell patch-clamp method | B | 6 | pIC50 | 1000 | nM | IC50 | Eur J Med Chem (2022) 236: 114354-114354 [PMID:35453065] |
| 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] |
| GluN1/GluN2B/Glutamate NMDA receptor; Grin1/Grin2b in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096666] [GtoPdb: 455, 457] [UniProtKB: P35439, Q00960] | ||||||||
| ChEMBL | Inhibition of NMDA/glycine-activated rat GluN1/Glu2B expressed in xenopus laevis oocytes at -75 mV holding potential by voltage clamp method | B | 5.25 | pIC50 | 5570 | nM | IC50 | Eur J Med Chem (2023) 261: 115803-115803 [PMID:37734258] |
| GluN1/Glutamate receptor ionotropic, NMDA 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL330] [GtoPdb: 455] [UniProtKB: P35439] | ||||||||
| ChEMBL | Protective Effects of Compounds on Primary Cerebellum Granule Cells of Rats: Isolated primary cerebellum granule cells of infant rats were inoculated in 96-well plates with 1.2×105/well by using 10% FBS+25 mM KCl+2 mM Glutamine+1% of double-antibody BME medium. After 24 hours, cytarabine with a final concentration of 10 iM was added to inhibit the proliferation of neurogliocyte cells. After the day 4, glucose with the final concentration of 5 mM was added every four days to complement energy metabolism and water evaporation of cells. The materials were placed in a cell incubator (37° C., 5% CO2) to be cultured for 10 days. A 200 iM of glutamate was used to induce the excitotoxic injury of the primary cerebellum granule cells, with test groups of normal control group, glutamate group, pretreatment groups with different memantine nitrate compounds, and pretreatment control group with memantine. In the testing groups, the compounds of NM-001, NM-002, NM-003, NM-004, NM-005, NM-008, NM-009, NM-011, NM-012 and memantine were respectively added. After pre-protection for 2 h, 200 iM of glutamate was added to induce cell damage for 24 h, and then MTT was added to culture for 4 h. The supernatant fraction was sucked, and 150 iL of DMSO was added to each well for dissolving. After blending with shaking, the light absorption values under 570 nm wavelength was measured with a microplate reader, and the viability of cells was calculated. Cell viability (%)=absorbance of different groups/absorbance of the normal control group×100%. | B | 5.57 | pEC50 | 2720 | nM | EC50 | US-10214478-B2. Amantadine nitrate compounds with neural protective effect, and preparation and medical use thereof (2019) |
| GluN2B/Glutamate receptor ionotropic, NMDA 2B 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 receptor ionotropic, NMDA 2C 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 36:
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]
