memantine [Ligand Id: 4253] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL807 (Memantine, D-145, Namenda, DRG-0267)
  • Acetylcholinesterase in Electrophorus electricus [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
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  • GluN2B/Glutamate [NMDA] receptor subunit epsilon 2 in Rat [ChEMBL: CHEMBL311] [GtoPdb: 457] [UniProtKB: Q00960]
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  • GluN2C/Glutamate [NMDA] receptor subunit epsilon 3 in Rat [ChEMBL: CHEMBL401] [GtoPdb: 458] [UniProtKB: Q00961]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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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]
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]
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 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 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 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 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 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 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]
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 28:

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