Memantine (CID 4054) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(24)
 
 
Inactive(134)
 
 
Inconclusive(41)
 
 
Unspecified(65)
 
 
Top Targets:
PBP1 iGluR NM..(8)
 
 
 
7TM GPCR Srx(4)
 
 
PIKKc TOR(4)
 
 
 
Esterase lipa..(4)
 
 
Geminin(4)
 
 
BioAssay Types:
Literature(136)
 
 
 
 
 
Confirmatory(87)
 
 
 
 
Screening(4)
 
 
BioActivity Types:
Potency(85)
 
 
 
 
IC50(22)
 
 
 
Ki(4)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 193    Data Row: 264   Total Pages: 6   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103211988]
Ki 0.54The 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. [AID156805, Type: Literature]
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2
[SID103211988]
Ki 0.7Compound with the N-methyl-D-aspartate glutamate receptor blocking activity [AID143463, Type: Literature]
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3
[SID103211988]
IC50 0.911Antagonist activity at recombinant NR1/NR2A receptor expressed in Xenopus laevis oocytes [AID292616, Type: Literature]Glutamate receptor ionotropic, NMDA 1 [gi:548377]
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4
[SID103211988]
IC50 1.02Antagonist activity at recombinant NR1/NR2B receptor expressed in Xenopus laevis oocytes [AID292617, Type: Literature]Glutamate receptor ionotropic, NMDA 1 [gi:548377]
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5
[SID103211988]
Ki 1.2Displacement of [3H]-(+)-MK801 from PCP binding site of NMDA receptor from pig brain cortex after 150 mins by scintillation counting [AID488105, Type: Literature]
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6
[SID103211988]
Ki 1.2Displacement of [3H]-(+)-MK-801 from NMDA receptor phencyclidine binding site in guinea pig brain cortex homogenates after 5 mins by scintillation counting [AID536042, Type: Literature]
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7
[SID103211988]
IC50 1.5Antagonist activity at NMDAR in rat cerebellar granule neurons assessed as inhibition of NMDA-induced calcium flux after 5 mins using FURA-2AM in presence of glycine [AID637740, Type: Literature]
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8
[SID103211988]
IC50 1.5Inhibition of NMDA receptor in rat cerebellar granule neurons assessed as NMDA-induced intracellular calcium increase [AID410126, Type: Literature]
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9
[SID103211988]
IC50 1.5Antagonist activity at NMDA receptor in cerebellar granule neurons assessed as inhibition of NMDA-induced increase in intracellular calcium concentration by fluorometric assay [AID388528, Type: Literature]
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10
[SID103211988]
IC50 1.5Antagonist 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 [AID416368, Type: Literature]
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11
[SID103211988]
IC50 1.5Antagonist activity at NMDA receptor in rat cerebellar granule neurons assessed as inhibition of NMDA-induced increase in intracellular calcium level by fluorometric assay [AID456467, Type: Literature]
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12
[SID103211988]
IC50 3.05Antagonist activity at NMDA receptor in ICR mouse synaptoneurosome assessed as inhibition of NMDA/Gly-mediated 45-calcium influx [AID305668, Type: Literature]
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13
[SID103211988]
IC50 5.5Inhibition 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 [AID480455, Type: Literature]Glutamate receptor ionotropic, NMDA 1 [gi:548377]
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14
[SID103211988]
IC50 5.6Inhibition 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 [AID480453, Type: Literature]Glutamate receptor ionotropic, NMDA 1 [gi:548377]
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15
[SID104171191]
Potency 6.7456Primary qHTS for delayed death inhibitors of the malarial parasite plastid, 96 hour incubation [AID504834, Type: confirmatory]
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16
[SID103211988]
IC50 9.52Inhibition 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 [AID341425, Type: Literature]
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17
[SID103211988]
IC50 13.75Antitrypanosomal activity against bloodstream form of Trypanosoma brucei 427 after 48 hrs by hemocytometer analysis [AID637741, Type: Literature]
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18
[SID103211988]
IC50 13.75Trypanocidal activity against Trypanosoma brucei 427 bloodstream form assessed as decrease in cell density after 48 hrs by hemocytometry [AID456470, Type: Literature]
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19
[SID103211988]
IC50 27.2Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy [AID386625, Type: Literature]Solute carrier family 22 member 1 [gi:313104181]
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20
[SID103211988]
 Inhibition of dexamethasone-induced human NR1-1a/NR2A receptor-mediated excitotoxicity in (S)-glutamate/glycine-stimulated mouse L12-G10 cells assessed as LDH release at 20 uM after 30 mins [AID480458, Type: Literature]Glutamate receptor ionotropic, NMDA 1 [gi:548377]
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21
[SID26751885]
 qHTS profiling for inhibitors of Plasmodium falciparum proliferation [AID504749_39, Type: Literature]
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22
[SID26751885]
 qHTS profiling for inhibitors of Plasmodium falciparum proliferation [AID504749_54, Type: Literature]
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23
[SID26751885]
 qHTS profiling for inhibitors of Plasmodium falciparum proliferation [AID504749_19, Type: Literature]
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24
[SID26751885]
 qHTS profiling for inhibitors of Plasmodium falciparum proliferation [AID504749_26, Type: Literature]
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25
[SID103211988]
IC50 10Inhibition of electric eel AChE by modified Ellman's method [AID480448, Type: Literature]Acetylcholinesterase [gi:14916521]
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26
[SID103211988]
IC50 10Inhibition of equine serum BChE by modified Ellman's method [AID480449, Type: Literature]Cholinesterase [gi:21362409]
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27
[SID103211988]
Km 34TP_TRANSPORTER: uptake (electrogenesis) in Xenopus laevis oocytes [AID679500, Type: other]
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28
[SID103211988]
IC50 55Antagonist activity at NMDA receptor in rat cerebellar granule neurons assessed as inhibition of glutamate-induced increase in intracellular calcium level by fluorometric assay [AID456466, Type: Literature]
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29
[SID103211988]
IC50 55Antagonist activity against glutamate receptor in rat cerebellar granule neurons assessed as inhibition of glutamate-induced increase in intracellular calcium level by Fura-2 AM dye based fluorimetry [AID416367, Type: Literature]
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30
[SID103211988]
IC50 55Antagonist activity at NMDA receptor in cerebellar granule neurons assessed as inhibition of glutamate-induced increase in intracellular calcium concentration by fluorometric assay [AID388526, Type: Literature]
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31
[SID103211988]
IC50 55Antagonist activity at NMDAR in rat cerebellar granule neurons assessed as inhibition of glutamate-induced calcium flux after 5 mins using FURA-2AM in presence of glycine [AID637739, Type: Literature]
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32
[SID103211988]
IC50 55.4Inhibition of NMDA receptor in rat cerebellar granule neurons assessed as glutamate-induced intracellular calcium increase [AID410125, Type: Literature]
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33
[SID103211988]
CC50 100Cytotoxicity against mouse L12-G10 cells by MTT assay [AID480463, Type: Literature]
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34
[SID103211988]
IC50 147Cytotoxicity in mouse FM3A cells after 48 hrs [AID292618, Type: Literature]
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35
[SID103211988]
 Cytotoxicity against mouse L12-G10 cells at 50 uM by MTT assay [AID480464, Type: Literature]
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36
[SID103211988]
 Displacement of [3H]MK-801 from NMDA receptor in ICR mouse synaptoneurosome at 100 uM [AID305670, Type: Literature]
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37
[SID103211988]
 Displacement of [3H]TCP from NMDA receptor in ICR mouse synaptoneurosome at 100 uM [AID305671, Type: Literature]
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38
[SID103211988]
 Inhibition of ASM in rat PC12 cells assessed as residual activity at 10 uM [AID311933, Type: Literature]
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39
[SID103211988]
 Dissociation constant, pKa of the compound [AID311934, Type: Literature]
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40
[SID103211988]
 Partition coefficient, log P of the compound [AID311935, Type: Literature]
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41
[SID104171191]
 qHTS profiling for inhibitors of Plasmodium falciparum proliferation [AID504749, Type: Literature]
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42
[SID26751885]
 qHTS profiling for inhibitors of Plasmodium falciparum proliferation [AID504749, Type: Literature]
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43
[SID103211988]
 Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset [AID588208, Type: Literature]
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44
[SID103211988]
 Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset [AID588209, Type: Literature]
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45
[SID103211988]
 Human drug-induced liver injury (DILI) modelling dataset from Ekins et al [AID588210, Type: Literature]
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46
[SID103211988]
 Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset [AID588220, Type: Literature]
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47
[SID103211988]
 Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia [AID625279, Type: Literature]
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48
[SID103211988]
 Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis [AID625280, Type: Literature]
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49
[SID103211988]
 Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis [AID625281, Type: Literature]
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50
[SID103211988]
 Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis [AID625282, Type: Literature]
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