Found 21 hits of ic50 for drug = Alphacaine Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kJ/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
Sodium channel protein type 4 subunit alpha
(Homo sapiens (Human)) | BDBM50017662
(2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethyla...)Show InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) | PDB
UniProtKB/SwissProt
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Similars
| Article PubMed
| n/a | n/a | 2.00E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Ljubljana
Curated by ChEMBL
| Assay Description Modulation of human Nav1.4 in open-inactivated state assessed as inhibition of inward current after 4 mins by whole-cell electrophysiology |
Eur J Med Chem 74: 23-30 (2014)
Article DOI: 10.1016/j.ejmech.2013.12.034 BindingDB Entry DOI: 10.7270/Q2V69NJW |
More data for this Ligand-Target Pair | |
Sodium channel protein type 3 subunit alpha
(Homo sapiens (Human)) | BDBM50017662
(2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethyla...)Show InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) | PDB
UniProtKB/SwissProt
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Similars
| Article PubMed
| n/a | n/a | 1.05E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Ljubljana
Curated by ChEMBL
| Assay Description Modulation of human Nav1.3 in open-inactivated state assessed as inhibition of inward current after 4 mins by whole-cell electrophysiology |
Eur J Med Chem 74: 23-30 (2014)
Article DOI: 10.1016/j.ejmech.2013.12.034 BindingDB Entry DOI: 10.7270/Q2V69NJW |
More data for this Ligand-Target Pair | |
Sodium channel protein type 9 subunit alpha
(Homo sapiens (Human)) | BDBM50017662
(2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethyla...)Show InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) | PDB
KEGG
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| DrugBank Article PubMed
| n/a | n/a | 2.90E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Ljubljana
Curated by ChEMBL
| Assay Description Modulation of human Nav1.7 in open-inactivated state assessed as inhibition of inward current after 4 mins by whole-cell electrophysiology |
Eur J Med Chem 74: 23-30 (2014)
Article DOI: 10.1016/j.ejmech.2013.12.034 BindingDB Entry DOI: 10.7270/Q2V69NJW |
More data for this Ligand-Target Pair | |
Sodium channel protein type 1/2/3 subunit alpha
(Rattus norvegicus) | BDBM50017662
(2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethyla...)Show InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) | PDB
UniProtKB/SwissProt
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| n/a | n/a | 5.60E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Institut Henri Beaufour
Curated by ChEMBL
| Assay Description Concentration required to inhibit [3H]BTX binding to Sodium channel of rat brain |
Bioorg Med Chem Lett 14: 3521-3 (2004)
BindingDB Entry DOI: 10.7270/Q2474D2N |
More data for this Ligand-Target Pair | |
Potassium channel subfamily K member 18
(Homo sapiens (Human)) | BDBM50017662
(2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethyla...)Show InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) | UniProtKB/SwissProt
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| Article PubMed
| n/a | n/a | >1.00E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Inc.
Curated by ChEMBL
| Assay Description Channel blocking activity at human TRESK channel |
Bioorg Med Chem Lett 26: 4919-4924 (2016)
Article DOI: 10.1016/j.bmcl.2016.09.020 BindingDB Entry DOI: 10.7270/Q2T72KDN |
More data for this Ligand-Target Pair | |
Sodium channel protein type 5 subunit alpha
(Homo sapiens (Human)) | BDBM50017662
(2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethyla...)Show InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) | PDB
KEGG
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| DrugBank Article PubMed
| n/a | n/a | 1.08E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
Cardiome Pharma Corporation
Curated by ChEMBL
| Assay Description Inhibition of human heart sodium channel Nav1.5 by patch-clamp method |
J Med Chem 50: 2818-41 (2007)
Article DOI: 10.1021/jm0604528 BindingDB Entry DOI: 10.7270/Q29Z95QZ |
More data for this Ligand-Target Pair | |
ATP-binding cassette sub-family C member 2
(Homo sapiens (Human)) | BDBM50017662
(2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethyla...)Show InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) | PDB
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| Article PubMed
| n/a | n/a | >1.33E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
Amgen Inc
Curated by ChEMBL
| Assay Description Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and... |
Toxicol Sci 136: 216-41 (2013)
Article DOI: 10.1093/toxsci/kft176 BindingDB Entry DOI: 10.7270/Q2JM2D2D |
More data for this Ligand-Target Pair | |
ATP-binding cassette sub-family C member 4
(Homo sapiens (Human)) | BDBM50017662
(2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethyla...)Show InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) | PDB
Reactome pathway KEGG
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| Article PubMed
| n/a | n/a | >1.33E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
Amgen Inc
Curated by ChEMBL
| Assay Description Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and... |
Toxicol Sci 136: 216-41 (2013)
Article DOI: 10.1093/toxsci/kft176 BindingDB Entry DOI: 10.7270/Q2JM2D2D |
More data for this Ligand-Target Pair | |
ATP-binding cassette sub-family C member 3
(Homo sapiens (Human)) | BDBM50017662
(2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethyla...)Show InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) | PDB
Reactome pathway KEGG
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| Article PubMed
| n/a | n/a | >1.33E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
Amgen Inc
Curated by ChEMBL
| Assay Description Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ... |
Toxicol Sci 136: 216-41 (2013)
Article DOI: 10.1093/toxsci/kft176 BindingDB Entry DOI: 10.7270/Q2JM2D2D |
More data for this Ligand-Target Pair | |
Bile salt export pump
(Homo sapiens (Human)) | BDBM50017662
(2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethyla...)Show InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) | PDB
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| Article PubMed
| n/a | n/a | >1.33E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
Amgen Inc
Curated by ChEMBL
| Assay Description Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to ... |
Toxicol Sci 136: 216-41 (2013)
Article DOI: 10.1093/toxsci/kft176 BindingDB Entry DOI: 10.7270/Q2JM2D2D |
More data for this Ligand-Target Pair | |
Bile salt export pump
(Homo sapiens (Human)) | BDBM50017662
(2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethyla...)Show InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) | PDB
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| Article PubMed
| n/a | n/a | >1.35E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
Amgen Inc.
Curated by ChEMBL
| Assay Description Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate t... |
Toxicol Sci 118: 485-500 (2010)
Article DOI: 10.1093/toxsci/kfq269 BindingDB Entry DOI: 10.7270/Q26Q20JN |
More data for this Ligand-Target Pair | |
Potassium channel subfamily K member 2
(Homo sapiens (Human)) | BDBM50017662
(2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethyla...)Show InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) | PDB
UniProtKB/SwissProt
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| Article PubMed
| n/a | n/a | 1.80E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Inc.
Curated by ChEMBL
| Assay Description Inhibition of human TREK-1 expressed in HEK293 cells by patch-clamp technique |
J Med Chem 56: 593-624 (2013)
Article DOI: 10.1021/jm3011433 BindingDB Entry DOI: 10.7270/Q23B61GZ |
More data for this Ligand-Target Pair | |
Potassium channel subfamily K member 2
(Homo sapiens (Human)) | BDBM50017662
(2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethyla...)Show InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) | PDB
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| Article PubMed
| n/a | n/a | 2.07E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
Universit£ Clermont Auvergne
Curated by ChEMBL
| Assay Description Inhibition of of human TREK1 expressed in HEK293 cells assessed as reduction in channel currents |
J Med Chem 59: 5149-57 (2016)
Article DOI: 10.1021/acs.jmedchem.5b00671 BindingDB Entry DOI: 10.7270/Q2319XSS |
More data for this Ligand-Target Pair | |
Potassium channel subfamily K member 3
(Homo sapiens (Human)) | BDBM50017662
(2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethyla...)Show InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) | PDB
KEGG
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| Article PubMed
| n/a | n/a | 2.22E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
Universidad de Talca
Curated by ChEMBL
| Assay Description Inhibition of human TASK1 expressed in Xenopus oocytes by whole cell voltage clamp assay |
J Med Chem 62: 10044-10058 (2019)
Article DOI: 10.1021/acs.jmedchem.9b00248 BindingDB Entry DOI: 10.7270/Q2TT4V7B |
More data for this Ligand-Target Pair | |
Sodium channel protein type 1/2/3 subunit alpha
(Homo sapiens (Human)) | BDBM50017662
(2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethyla...)Show InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) | PDB
KEGG
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| n/a | n/a | 2.40E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
Curated by ChEMBL
| Assay Description Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea... |
J Med Chem 28: 381-8 (1985)
BindingDB Entry DOI: 10.7270/Q2Z321T8 |
More data for this Ligand-Target Pair | |
Potassium voltage-gated channel subfamily H member 2
(Homo sapiens (Human)) | BDBM50017662
(2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethyla...)Show InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt UniProtKB/TrEMBL
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Patents
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| Article PubMed
| n/a | n/a | 2.63E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
TCG Lifesciences Ltd.
Curated by ChEMBL
| Assay Description Inhibition of human ERG |
Eur J Med Chem 46: 618-30 (2011)
Article DOI: 10.1016/j.ejmech.2010.11.042 BindingDB Entry DOI: 10.7270/Q2WQ052W |
More data for this Ligand-Target Pair | |
Potassium voltage-gated channel subfamily H member 2
(Homo sapiens (Human)) | BDBM50017662
(2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethyla...)Show InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) | PDB MMDB
Reactome pathway KEGG
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Patents
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| Article PubMed
| n/a | n/a | 2.63E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
Universit£ di Pisa
Curated by ChEMBL
| Assay Description Inhibition of human ERG channel in HEK293 cells by voltage-clamp method |
Eur J Med Chem 43: 2479-88 (2008)
Article DOI: 10.1016/j.ejmech.2007.12.025 BindingDB Entry DOI: 10.7270/Q2542PTB |
More data for this Ligand-Target Pair | |
Multidrug and toxin extrusion protein 1
(Homo sapiens (Human)) | BDBM50017662
(2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethyla...)Show InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) | Reactome pathway KEGG
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| Article PubMed
| n/a | n/a | >5.00E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
University of California
Curated by ChEMBL
| Assay Description Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay |
J Med Chem 56: 781-95 (2013)
Article DOI: 10.1021/jm301302s BindingDB Entry DOI: 10.7270/Q2F76DWZ |
More data for this Ligand-Target Pair | |
Voltage-dependent L-type calcium channel subunit alpha-1C
(Oryctolagus cuniculus) | BDBM50017662
(2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethyla...)Show InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) | PDB MMDB
Reactome pathway KEGG
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| n/a | n/a | >1.00E+6 | n/a | n/a | n/a | n/a | n/a | n/a |
Ortho Pharmaceutical Corporation
Curated by ChEMBL
| Assay Description Inhibition of [3H]nitrendipine binding to calcium channels in Rabbit cardiac muscle. |
J Med Chem 31: 2221-7 (1988)
BindingDB Entry DOI: 10.7270/Q2T72J19 |
More data for this Ligand-Target Pair | |
Potassium voltage-gated channel subfamily D member 2
(Rattus norvegicus) | BDBM50017662
(2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethyla...)Show InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) | PDB MMDB
KEGG
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| Article PubMed
| n/a | n/a | 1.21E+6 | n/a | n/a | n/a | n/a | n/a | n/a |
Cardiome Pharma Corporation
Curated by ChEMBL
| Assay Description Inhibition of rat potassium channel Kv4.2 by patch-clamp method |
J Med Chem 50: 2818-41 (2007)
Article DOI: 10.1021/jm0604528 BindingDB Entry DOI: 10.7270/Q29Z95QZ |
More data for this Ligand-Target Pair | |
Potassium voltage-gated channel subfamily A member 5
(Homo sapiens (Human)) | BDBM50017662
(2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethyla...)Show InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) | PDB
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| Article PubMed
| n/a | n/a | 2.19E+6 | n/a | n/a | n/a | n/a | n/a | n/a |
Cardiome Pharma Corporation
Curated by ChEMBL
| Assay Description Inhibition of human potassium channel Kv1.5 by patch-clamp method |
J Med Chem 50: 2818-41 (2007)
Article DOI: 10.1021/jm0604528 BindingDB Entry DOI: 10.7270/Q29Z95QZ |
More data for this Ligand-Target Pair | |