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Lidocaine (CID 3676) - Compound BioActivity Data
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BioActivity Outcomes:
Active(21)
 
 
Inactive(1269)
 
 
Inconclusive(54)
 
 
Unspecified(436)
 
 
Top Targets:
7TM GPCR Srx(48)
 
 
 
 
7TM GPCR Srsx(37)
 
 
 
p450(28)
 
 
 
 
Tryp SPc(17)
 
 
 
Na trans asso..(15)
 
 
 
BioAssay Types:
Confirmatory(596)
 
 
 
 
Screening(538)
 
 
 
Literature(407)
 
 
 
 
 
Summary(24)
 
 
 
BioActivity Types:
Potency(500)
 
 
 
 
IC50(192)
 
 
 
 
EC50(11)
 
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 1385    Data Row: 1780   Total Pages: 36   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103169867]
EC50 0.017Negative inotropic activity against potassium-induced contraction in guinea pig left atrium assessed as decrease in developed tension [AID491141, Type: Literature]
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2
[SID103169867]
EC50 0.017Negative inotropic activity in guinea pig left atria assessed as decrease of 1 Hz current-induced developed tension [AID655940, Type: Literature]
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3
[SID103169867]
EC50 0.017Negative inotropic activity assessed as decrease in developed tension in isolated guinea pig left atrium [AID275639, Type: Literature]
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4
[SID103169867]
Relative effect on exacerbation of ventricular tachycardia in dogs; Exacerbation of VT present [AID60332, Type: Literature]
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5
[SID103169867]
Relative effect on slowing of ventricular tachycardia in dogs;slowing of VT present [AID60348, Type: Literature]
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6
[SID103169867]
Inhibition of yeast prion protein Sup35 infection of PSI yeast spheroplast cells at 200 uM [AID497664, Type: Literature]
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7
[SID855682]
qHTS Assay for Spectroscopic Profiling in 4-MU Spectral Region [AID589, Type: other]
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8
[SID855682]
qHTS Assay for Spectroscopic Profiling in A350 Spectral Region [AID590, Type: other]
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9
[SID855682]
Aqueous Solubility from MLSMR Stock Solutions [AID1996, Type: other]
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10
[SID11110520]
NINDS Anticonvulsant Data (Qualitative) [AID423, Type: other]
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11
[SID11110520]
NINDS Anticonvulsant Data (Quantitative) [AID424, Type: other]
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12
[SID103169867]
Sodium channel alpha subunit blocker [AID742738, Type: other]Sodium channel protein type 1 subunit alpha [gi:12644229]
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13
[SID103169867]
Sodium channel alpha subunit blocker [AID742738, Type: other]Sodium channel protein type 2 subunit alpha [gi:25014053]
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14
[SID103169867]
Sodium channel alpha subunit blocker [AID742738, Type: other]Sodium channel protein type 3 subunit alpha [gi:25014054]
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15
[SID103169867]
Sodium channel alpha subunit blocker [AID742738, Type: other]Sodium channel protein type 8 subunit alpha [gi:34098756]
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16
[SID103169867]
Sodium channel alpha subunit blocker [AID742738, Type: other]Sodium channel protein type 10 subunit alpha [gi:205371821]
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17
[SID103169867]
Sodium channel alpha subunit blocker [AID742738, Type: other]Sodium channel protein type 5 subunit alpha [gi:215273881]
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18
[SID103169867]
Sodium channel alpha subunit blocker [AID742738, Type: other]Sodium channel protein type 11 subunit alpha [gi:124053649]
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19
[SID103169867]
Sodium channel alpha subunit blocker [AID742738, Type: other]Sodium channel protein type 4 subunit alpha [gi:292495096]
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20
[SID103169867]
Sodium channel alpha subunit blocker [AID742738, Type: other]Sodium channel protein type 7 subunit alpha [gi:296452902]
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21
[SID103169867]
Sodium channel alpha subunit blocker [AID742738, Type: other]Sodium channel protein type 9 subunit alpha [gi:327478559]
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22
[SID103169867]
IC50 56Concentration 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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23
[SID103169867]
IC50 56Concentration 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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24
[SID103169867]
IC50 56Concentration 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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25
[SID103169867]
IC50 97Inhibition of veratridine-induced guanidine flux in cardiac voltage-gated sodium channel (veratridine block vs. Na release) [AID217929, Type: Literature]
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26
[SID103169867]
IC50 108Inhibition of human heart sodium channel Nav1.5 by patch-clamp method [AID288782, Type: Literature]Sodium channel protein type 5 subunit alpha [gi:215273881]
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27
[SID103169867]
IC50 113Inhibition of [3H]BTX binding to cardiac voltage-gated sodium channel [AID217926, Type: Literature]
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28
[SID103169867]
IC50 180Activity at sodium channel assessed as blockade of sodium current [AID317688, Type: Literature]
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29
[SID103169867]
IC50 180Inhibition of human TREK-1 expressed in HEK293 cells by patch-clamp technique [AID726093, Type: Literature]Potassium channel subfamily K member 2 [gi:145559488]
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30
[SID103169867]
IC50 240Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex [AID205267, Type: Literature]
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31
[SID103169867]
IC50 240Displacement of [3H]-BTX-B from neuronal voltage-gated sodium channel in rat cerebral cortex synaptoneurosomes [AID450269, Type: Literature]
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32
[SID103169867]
IC50 263.027Inhibition of human ERG channel in HEK293 cells by voltage-clamp method [AID392051, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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33
[SID103169867]
IC50 263.027Inhibition of human ERG [AID576612, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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34
[SID103169867]
IC50 500Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay [AID721754, Type: Literature]Multidrug and toxin extrusion protein 1 [gi:74731723]
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35
[SID103169867]
IC50 740Reduction in amplitude of compound action potential in frog sciatic nerve by electrophysiology [AID716814, Type: Literature]
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36
[SID103169867]
IC50 1000Inhibition of [3H]nitrendipine binding to calcium channels in Rabbit cardiac muscle. [AID45634, Type: Literature]Voltage-dependent L-type calcium channel subunit alpha-1C [gi:116411]
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37
[SID103169867]
IC50 1210Inhibition of rat potassium channel Kv4.2 by patch-clamp method [AID288784, Type: Literature]Potassium voltage-gated channel subfamily D member 2 [gi:38257805]
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38
[SID103169867]
IC50 1410Antispasmodic activity in guinea pig ileum assessed as inhibition of histamine-induced contraction [AID317686, Type: Literature]
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39
[SID103169867]
IC50 1430Antispasmodic activity in guinea pig ileum assessed as inhibition of allergen-induced contraction [AID317687, Type: Literature]
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40
[SID103169867]
IC50 2188Inhibition of human potassium channel Kv1.5 by patch-clamp method [AID288783, Type: Literature]Potassium voltage-gated channel subfamily A member 5 [gi:146345443]
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41
[SID103169867]
DRUGMATRIX: CYP450, 2A6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) [AID625246, Type: other]Cytochrome P450 2A6 [gi:308153612]
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42
[SID103169867]
IC50 DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) [AID625161, Type: other]Delta-type opioid receptor [gi:311033488]
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43
[SID103169867]
IC50 DRUGMATRIX: Protease, Matrix Metalloprotease-9 (MMP-9) enzyme inhibition (substrate: Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2) [AID625178, Type: other]Matrix metalloproteinase-9 [gi:269849668]
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44
[SID103169867]
IC50 DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) [AID625205, Type: other]Beta-2 adrenergic receptor [gi:296439450]
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45
[SID103169867]
Inhibition of ASM in human H4 cells assessed as residual activity at 10 uM [AID311932, Type: Literature]Sphingomyelin phosphodiesterase [gi:224471897]
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46
[SID103169867]
IC50 DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2) [AID625229, Type: other]Thromboxane-A synthase [gi:254763392]
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47
[SID103169867]
IC50 DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) [AID625227, Type: other]Substance-K receptor [gi:229462950]
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48
[SID103169867]
Apparent permeability (Papp) from apical to basolateral side determined in MDR1-MDCKII cells [AID624622, Type: Literature]Multidrug resistance protein 1 [gi:238054374]
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49
[SID103169867]
Apparent permeability (Papp) from basolateral to apical side determined in MDR1-MDCKII cells [AID624623, Type: Literature]Multidrug resistance protein 1 [gi:238054374]
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50
[SID103169867]
Ratio of apparent permeability from basolateral to apical side over apical to basolateral side determined in MDR1-MDCKII cells [AID624626, Type: Literature]Multidrug resistance protein 1 [gi:238054374]
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