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lamotrigine (CID 3878) - Compound BioActivity Data
.
BioActivity Outcomes:
Active(50)
 
 
Inactive(1520)
 
 
Inconclusive(46)
 
 
Unspecified(303)
 
 
Top Targets:
7TM GPCR Srx(58)
 
 
 
 
Na trans asso..(46)
 
 
 
7TM GPCR Srsx(44)
 
 
 
p450(28)
 
 
 
 
alkPPc(20)
 
 
BioAssay Types:
Screening(707)
 
 
 
 
Confirmatory(697)
 
 
 
 
 
Literature(285)
 
 
 
 
 
Summary(25)
 
 
 
BioActivity Types:
Potency(555)
 
 
 
 
 
IC50(218)
 
 
 
 
 
EC50(20)
 
 
Ki(2)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 1365    Data Row: 1919   Total Pages: 39   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103199382]
IC50 2.6Displacement of [3H]BW202W92 from voltage-gated sodium channel in Wistar rat forebrain synaptosomes by liquid scintillation counting [AID352884, Type: Literature]
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2
[SID11113342]
Potency 6.3096qHTS Assay for Inhibitors and Substrates of Cytochrome P450 2D6 [AID891, Type: confirmatory]cytochrome P450 2D6 isoform 1 [Homo sapiens] [gi:40805836]
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3
[SID103199382]
IC50 8.1Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes [AID409601, Type: Literature]
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4
[SID103199382]
IC50 10Inhibition of human recombinant Nav1.2 channel expressed in HEK293 cells by whole cell voltage clamp technique [AID404535, Type: Literature]Sodium channel protein type 2 subunit alpha [gi:25014053]
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5
[SID103199382]
Ki 17Affinity for inactive human SkM1 sodium channel expressed in HEK293 cells [AID205290, Type: Literature]Sodium channel protein type 4 subunit alpha [gi:292495096]
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6
[SID90341162]
Potency 20.5962qHTS Assay for Small Molecule Inhibitors of Mitochondrial Division or Activators of Mitochondrial Fusion [AID485298, Type: confirmatory]
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7
[SID103199382]
IC50 21Inhibition of veratridine-induced guanidine flux in cardiac voltage-gated sodium channel (veratridine block vs. Na release) [AID217929, Type: Literature]
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8
[SID103199382]
IC50 25Blockade of Nav1.8 channel in rat dorsal root ganglion neurons assessed as inhibition of TTX-R current by whole cell patch clamp technique [AID404533, Type: Literature]Sodium channel protein type 10 subunit alpha [gi:56748617]
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9
[SID855818]
IC50 25.82A counter screen for small molecule screen for inhibitors of the PhoP regulon in Salmonella typhi [AID2384, Type: confirmatory]
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10
[SID103199382]
Ki 29.2Dissociation constant for binding to inactivated state of rat brain NaIIa (rNav1.2) -B2 cell line stably expressed in HEK293 Cells [AID244602, Type: Literature]
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11
[SID103199382]
IC50 31Concentration required to inhibit [3H]BTX binding to Sodium channel of rat brain [AID205273, Type: Literature]Sodium channel protein type 1 subunit alpha [gi:116447]
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12
[SID103199382]
IC50 31Concentration required to inhibit [3H]BTX binding to Sodium channel of rat brain [AID205273, Type: Literature]Sodium channel protein type 2 subunit alpha [gi:116448]
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13
[SID103199382]
IC50 31Concentration required to inhibit [3H]BTX binding to Sodium channel of rat brain [AID205273, Type: Literature]Sodium channel protein type 3 subunit alpha [gi:116449]
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14
[SID855818]
IC50 32.987A screen for inhibitors of the PhoP regulon in Salmonella Typhi using a modified counterscreen [AID1985, Type: confirmatory]
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15
[SID103199382]
IC50 35Inhibition of rat Nav1.2 channel expressed in chinese hamster CHL1610 cells at preconditioning pulse of -67 mV after 2 to 3 mins by whole-cell patch-clamp technique [AID471864, Type: Literature]Sodium channel protein type 2 subunit alpha [gi:116448]
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16
[SID855818]
IC50 60.49A Counter Screen to identiry small molecule screen for inhibitors of the PhoP regulon in Salmonella Typhimurium [AID2401, Type: confirmatory]
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17
[SID855818]
IC50 65.34A small molecule screen for inhibitors of the PhoP regulon in Salmonella typhi [AID1850, Type: confirmatory]
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18
[SID855818]
IC50 66.35A screen for inhibitors of the PhoP regulon in Salmonella Typhimurium using a modified counterscreen. [AID1981, Type: confirmatory]
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19
[SID855818]
IC50 150A small molecule screen for inhibitors of the PhoP regulon in Salmonella Typhimurium [AID1863, Type: confirmatory]
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20
[SID103199382]
FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase [AID588216, Type: Literature]
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21
[SID103199382]
FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase [AID588217, Type: Literature]
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22
[SID103199382]
FDA HLAED, liver enzyme composite activity [AID588214, Type: Literature]
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23
[SID103199382]
Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis [AID678721, Type: Literature]
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24
[SID48416154]
DSSTox (FDAMDD) FDA Maximum (Recommended) Daily Dose Database [AID1195, Type: other]
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25
[SID103199382]
Inhibition of native TTX-S sodium currents in acutely dissociated rat dorsal root ganglion (DRG) [AID253081, Type: Literature]
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26
[SID103199382]
Antiallodynic activity in Wistar albino rat chronic constriction injury-induced neuropathic pain model assessed as reversal of spontaneous pain response up to 2 hrs at 100 mg/kg, ip [AID603564, Type: Literature]
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27
[SID103199382]
Antiallodynic activity in Wistar albino rat chronic constriction injury-induced neuropathic pain model assessed as attenuation of mechanical allodynia after 0.5 hrs at 100 mg/kg, ip [AID603565, Type: Literature]
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28
[SID103199382]
Unbound drug concentration in Sprague-Dawley rat plasma administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method [AID604020, Type: Literature]
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29
[SID103199382]
Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins [AID678712, Type: Literature]Cytochrome P450 1A2 [gi:117144]
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30
[SID103199382]
Inhibition of AQP4 expressed in rat FRT cells assessed as transepithelial osmotic water permeability at 100 uM by dye dilution method [AID342469, Type: Literature]
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31
[SID103199382]
Inhibition of AQP4 in wild type mouse brain gilial cells assessed as osmotic water permeability at 10 to 100 uM after 15 mins by calcein quenching assay [AID342470, Type: Literature]Aquaporin-4 [gi:47117859]
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32
[SID103199382]
Inhibition of AQP4 in wild type mouse brain gilial cells assessed as reduction of osmotic equilibrium rate at 10 to 100 uM after 15 mins by calcein quenching assay relative to water permeability [AID342471, Type: Literature]Aquaporin-4 [gi:47117859]
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33
[SID103199382]
Inhibition of AQP4 in mouse erythrocytes assessed as inhibition of osmotic water permeability at 100 uM after 15 mins by stopped-flow light scattering method [AID342472, Type: Literature]Aquaporin-4 [gi:47117859]
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34
[SID103199382]
Sodium channel alpha subunit blocker [AID742738, Type: other]Sodium channel protein type 2 subunit alpha [gi:25014053]
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35
[SID103199382]
Sodium channel alpha subunit blocker [AID742738, Type: other]Sodium channel protein type 3 subunit alpha [gi:25014054]
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36
[SID103199382]
Sodium channel alpha subunit blocker [AID742738, Type: other]Sodium channel protein type 8 subunit alpha [gi:34098756]
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37
[SID103199382]
Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins [AID678713, Type: Literature]Cytochrome P450 2C9 [gi:6686268]
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38
[SID103199382]
Sodium channel alpha subunit blocker [AID742738, Type: other]Sodium channel protein type 1 subunit alpha [gi:12644229]
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39
[SID103199382]
Sodium channel alpha subunit blocker [AID742738, Type: other]Sodium channel protein type 4 subunit alpha [gi:292495096]
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40
[SID103199382]
Sodium channel alpha subunit blocker [AID742738, Type: other]Sodium channel protein type 7 subunit alpha [gi:296452902]
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41
[SID103199382]
Sodium channel alpha subunit blocker [AID742738, Type: other]Sodium channel protein type 9 subunit alpha [gi:327478559]
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42
[SID103199382]
Sodium channel alpha subunit blocker [AID742738, Type: other]Sodium channel protein type 10 subunit alpha [gi:205371821]
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43
[SID103199382]
Sodium channel alpha subunit blocker [AID742738, Type: other]Sodium channel protein type 5 subunit alpha [gi:215273881]
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44
[SID11113342]
Cytochrome panel assay with activity outcomes [AID1851_2, Type: other]cytochrome P450 2D6 isoform 2 [Homo sapiens] [gi:68509921]
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45
[SID103199382]
Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins [AID678714, Type: Literature]Cytochrome P450 2C19 [gi:60416369]
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46
[SID103199382]
Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins [AID678716, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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47
[SID103199382]
Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins [AID678717, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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48
[SID103199382]
Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins [AID678715, Type: Literature]Cytochrome P450 2D6 [gi:84028191]
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49
[SID103199382]
Sodium channel alpha subunit blocker [AID742738, Type: other]Sodium channel protein type 11 subunit alpha [gi:124053649]
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50
[SID56423136]
Fluorescence Polarization Cell-Free Homogeneous Primary HTS to Identify Inhibitors of the LANA Histone H2A/H2B Interaction [AID2629, Type: screening]LANA [Human herpesvirus 8] [gi:139472804]
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