BindingDB PrimarySearch

BDBM50017662 2-(Diethylamino)-2',6'-acetoxylidide::2-(Diethylamino)-N-(2,6-dimethylphenyl)acetamide::CHEMBL79::Dalcaine::LIDOCAINE::Lignocaine::N-(2,6-dimethylphenyl)-N(2),N(2)-diethylglycinamide::Octocaine::SAMPL3, G5

SMILES: CCN(CC)CC(=O)Nc1c(C)cccc1C

InChI Key: InChIKey=NNJVILVZKWQKPM-UHFFFAOYSA-N

Data: 21 IC50 1 ITC

PDB links: 2 PDB IDs match this monomer.

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 21 hits for monomerid = 50017662
Target/Host (Institution)	Ligand	Target/Host Links	Ligand Links	Trg + Lig Links	Ki nM	ΔG° kcal/mole	IC50 nM	Kd nM	EC50/IC50 nM	k_off s^-1	k_on M^-1s^-1	pH	Temp °C
Potassium voltage-gated channel subfamily H member 2 (Homo sapiens (Human))	BDBM50017662 (2-(Diethylamino)-2',6'-acetoxylidide \| 2-(Diethyla...) Show SMILES CCN(CC)CC(=O)Nc1c(C)cccc1C Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL DrugBank KEGG MMDB PC cid PC sid PDB UniChem Patents Similars	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
TCG Lifesciences Ltd. Curated by ChEMBL					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 SMILES CCN(CC)CC(=O)Nc1c(C)cccc1C Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL DrugBank KEGG MMDB PC cid PC sid PDB UniChem Patents Similars	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
University of Ljubljana Curated by ChEMBL					More data for this Ligand-Target Pair
Voltage-gated L-type calcium channel alpha-1C subunit (Oryctolagus cuniculus)	BDBM50017662 (2-(Diethylamino)-2',6'-acetoxylidide \| 2-(Diethyla...) Show SMILES CCN(CC)CC(=O)Nc1c(C)cccc1C Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet	Purchase CHEMBL DrugBank KEGG MMDB PC cid PC sid PDB UniChem Patents Similars	PubMed	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
Ortho Pharmaceutical Corporation Curated by ChEMBL					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 SMILES CCN(CC)CC(=O)Nc1c(C)cccc1C Show InChI	UniProtKB/SwissProt GoogleScholar AffyNet	Purchase CHEMBL DrugBank KEGG MMDB PC cid PC sid PDB UniChem Patents Similars	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
Pfizer Inc. Curated by ChEMBL					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 SMILES CCN(CC)CC(=O)Nc1c(C)cccc1C Show InChI	PDB MMDB KEGG UniProtKB/SwissProt B.MOAD GoogleScholar AffyNet	Purchase CHEMBL DrugBank KEGG MMDB PC cid PC sid PDB UniChem Patents Similars	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
Cardiome Pharma Corporation Curated by ChEMBL					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 SMILES CCN(CC)CC(=O)Nc1c(C)cccc1C Show InChI	PDB KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL DrugBank KEGG MMDB PC cid PC sid PDB UniChem Patents Similars	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
Cardiome Pharma Corporation Curated by ChEMBL					More data for this Ligand-Target Pair
Voltage-gated potassium channel subunit Kv1.5 (Homo sapiens (Human))	BDBM50017662 (2-(Diethylamino)-2',6'-acetoxylidide \| 2-(Diethyla...) Show SMILES CCN(CC)CC(=O)Nc1c(C)cccc1C Show InChI	PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet	Purchase CHEMBL DrugBank KEGG MMDB PC cid PC sid PDB UniChem Patents Similars	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
Cardiome Pharma Corporation Curated by ChEMBL					More data for this Ligand-Target Pair
Sodium channel protein type I I alpha subunit (Homo sapiens (Human))	BDBM50017662 (2-(Diethylamino)-2',6'-acetoxylidide \| 2-(Diethyla...) Show SMILES CCN(CC)CC(=O)Nc1c(C)cccc1C Show InChI	PDB KEGG UniProtKB/SwissProt antibodypedia antibodypedia antibodypedia GoogleScholar AffyNet	Purchase CHEMBL DrugBank KEGG MMDB PC cid PC sid PDB UniChem Patents Similars	PubMed	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
TBA Curated by ChEMBL					More data for this Ligand-Target Pair
Twik-RElated Potassium (K+) channel 1 (TREK1) (Homo sapiens (Human))	BDBM50017662 (2-(Diethylamino)-2',6'-acetoxylidide \| 2-(Diethyla...) Show SMILES CCN(CC)CC(=O)Nc1c(C)cccc1C Show InChI	PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet	Purchase CHEMBL DrugBank KEGG MMDB PC cid PC sid PDB UniChem Patents Similars	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
Pfizer Inc. Curated by ChEMBL					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 SMILES CCN(CC)CC(=O)Nc1c(C)cccc1C Show InChI	Reactome pathway KEGG UniProtKB/SwissProt DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL DrugBank KEGG MMDB PC cid PC sid PDB UniChem Patents Similars	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
University of California Curated by ChEMBL					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 SMILES CCN(CC)CC(=O)Nc1c(C)cccc1C Show InChI	PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL B.MOAD DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL DrugBank KEGG MMDB PC cid PC sid PDB UniChem Patents Similars	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
Universit£ di Pisa Curated by ChEMBL					More data for this Ligand-Target Pair
Sodium channel protein type I I alpha subunit (Rattus norvegicus)	BDBM50017662 (2-(Diethylamino)-2',6'-acetoxylidide \| 2-(Diethyla...) Show SMILES CCN(CC)CC(=O)Nc1c(C)cccc1C Show InChI	PDB UniProtKB/SwissProt GoogleScholar AffyNet	Purchase CHEMBL DrugBank KEGG MMDB PC cid PC sid PDB UniChem Patents Similars	PubMed	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
Institut Henri Beaufour Curated by ChEMBL					More data for this Ligand-Target Pair
Bile salt export pump (BSEP) (Homo sapiens (Human))	BDBM50017662 (2-(Diethylamino)-2',6'-acetoxylidide \| 2-(Diethyla...) Show SMILES CCN(CC)CC(=O)Nc1c(C)cccc1C Show InChI	PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet	Purchase CHEMBL DrugBank KEGG MMDB PC cid PC sid PDB UniChem Patents Similars	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
Amgen Inc. Curated by ChEMBL					More data for this Ligand-Target Pair
Canalicular multispecific organic anion transporter 2 (Homo sapiens (Human))	BDBM50017662 (2-(Diethylamino)-2',6'-acetoxylidide \| 2-(Diethyla...) Show SMILES CCN(CC)CC(=O)Nc1c(C)cccc1C Show InChI	Reactome pathway KEGG UniProtKB/SwissProt DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL DrugBank KEGG MMDB PC cid PC sid PDB UniChem Patents Similars	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) BindingDB Entry DOI: 10.7270/Q2JM2D2D
Amgen Inc Curated by ChEMBL					More data for this Ligand-Target Pair
Multidrug resistance-associated protein 4 (Homo sapiens (Human))	BDBM50017662 (2-(Diethylamino)-2',6'-acetoxylidide \| 2-(Diethyla...) Show SMILES CCN(CC)CC(=O)Nc1c(C)cccc1C Show InChI	Reactome pathway KEGG UniProtKB/SwissProt DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL DrugBank KEGG MMDB PC cid PC sid PDB UniChem Patents Similars	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) BindingDB Entry DOI: 10.7270/Q2JM2D2D
Amgen Inc Curated by ChEMBL					More data for this Ligand-Target Pair
Canalicular multispecific organic anion transporter 1 (Homo sapiens (Human))	BDBM50017662 (2-(Diethylamino)-2',6'-acetoxylidide \| 2-(Diethyla...) Show SMILES CCN(CC)CC(=O)Nc1c(C)cccc1C Show InChI	UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet	Purchase CHEMBL DrugBank KEGG MMDB PC cid PC sid PDB UniChem Patents Similars	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) BindingDB Entry DOI: 10.7270/Q2JM2D2D
Amgen Inc Curated by ChEMBL					More data for this Ligand-Target Pair
Bile salt export pump (Homo sapiens (Human))	BDBM50017662 (2-(Diethylamino)-2',6'-acetoxylidide \| 2-(Diethyla...) Show SMILES CCN(CC)CC(=O)Nc1c(C)cccc1C Show InChI	PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet	Purchase CHEMBL DrugBank KEGG MMDB PC cid PC sid PDB UniChem Patents Similars	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) BindingDB Entry DOI: 10.7270/Q2JM2D2D
Amgen Inc Curated by ChEMBL					More data for this Ligand-Target Pair
Potassium channel protein TASK-1 (Homo sapiens (Human))	BDBM50017662 (2-(Diethylamino)-2',6'-acetoxylidide \| 2-(Diethyla...) Show SMILES CCN(CC)CC(=O)Nc1c(C)cccc1C Show InChI	PDB KEGG UniProtKB/SwissProt DrugBank antibodypedia GoogleScholar AffyNet	Purchase CHEMBL DrugBank KEGG MMDB PC cid PC sid PDB UniChem Patents Similars	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
Universidad de Talca Curated by ChEMBL					More data for this Ligand-Target Pair
Sodium channel alpha subunit (Homo sapiens (Human))	BDBM50017662 (2-(Diethylamino)-2',6'-acetoxylidide \| 2-(Diethyla...) Show SMILES CCN(CC)CC(=O)Nc1c(C)cccc1C Show InChI	PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet	Purchase CHEMBL DrugBank KEGG MMDB PC cid PC sid PDB UniChem Patents 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
University of Ljubljana Curated by ChEMBL					More data for this Ligand-Target Pair
Sodium channel alpha subunit (Homo sapiens (Human))	BDBM50017662 (2-(Diethylamino)-2',6'-acetoxylidide \| 2-(Diethyla...) Show SMILES CCN(CC)CC(=O)Nc1c(C)cccc1C Show InChI	PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet	Purchase CHEMBL DrugBank KEGG MMDB PC cid PC sid PDB UniChem Patents 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
University of Ljubljana Curated by ChEMBL					More data for this Ligand-Target Pair
Twik-RElated Potassium (K+) channel 1 (TREK1) (Homo sapiens (Human))	BDBM50017662 (2-(Diethylamino)-2',6'-acetoxylidide \| 2-(Diethyla...) Show SMILES CCN(CC)CC(=O)Nc1c(C)cccc1C Show InChI	PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet	Purchase CHEMBL DrugBank KEGG MMDB PC cid PC sid PDB UniChem Patents Similars	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) BindingDB Entry DOI: 10.7270/Q2319XSS
Universit£ Clermont Auvergne Curated by ChEMBL					More data for this Ligand-Target Pair

Activity Spreadsheet -- ITC Data from BindingDB

Found 1 hit for monomerid = 50017662
Cell (A)	Syringe (B)	Cell Links	Syringe Links	Cell + Syr Links	ΔG° kcal/mole	-TΔS° kcal/mole	ΔH° kcal/mole	log K	pH	Temp °C
BDBM197280	BDBM50017662	PC cid PC sid	CHEBI DrugBank KEGG MMDB PC cid PC sid PDB		-6.07	n/a	n/a	4.41	7.40	24.9
University of California San Diego	BDBM50017662	PC cid PC sid	CHEBI DrugBank KEGG MMDB PC cid PC sid PDB		J Comput Aided Mol Des 26: 475-87 (2012)