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  23 IC50  1 ITC

PDB links: 3 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 23 hits for monomerid = 50017662   

TargetSodium channel protein type 1/2/3 subunit alpha(Rat)
Institut Henri Beaufour

Curated by ChEMBL
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 5.60E+4nMAssay Description:Concentration required to inhibit [3H]BTX binding to Sodium channel of rat brainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/24/2018
Entry Details Article
PubMed
TargetSodium channel protein type 9 subunit alpha(Human)
Daiichi Sankyo Co.

Curated by ChEMBL
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 1.60E+4nMAssay Description:Inhibition of human Nav1.7 in inactivated condition by automated patch-clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMed
TargetSodium channel protein type 5 subunit alpha(Human)
Daiichi Sankyo Co.

Curated by ChEMBL
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of human Nav1.5 in inactivated condition by automated patch-clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMed
TargetSodium channel protein type 9 subunit alpha(Human)
Daiichi Sankyo Co.

Curated by ChEMBL
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 2.90E+4nMAssay Description:Modulation of human Nav1.7 in open-inactivated state assessed as inhibition of inward current after 4 mins by whole-cell electrophysiologyMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2020
Entry Details Article
PubMed
TargetSodium channel protein type 3 subunit alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 1.05E+4nMAssay Description:Modulation of human Nav1.3 in open-inactivated state assessed as inhibition of inward current after 4 mins by whole-cell electrophysiologyMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2020
Entry Details Article
PubMed
TargetSodium channel protein type 4 subunit alpha(Human)
University of Ljubljana

Curated by ChEMBL
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 2.00E+3nMAssay Description:Modulation of human Nav1.4 in open-inactivated state assessed as inhibition of inward current after 4 mins by whole-cell electrophysiologyMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2020
Entry Details Article
PubMed
TargetPotassium channel subfamily K member 3(Human)
Universidad De Talca

Curated by ChEMBL
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 2.22E+5nMAssay Description:Inhibition of human TASK1 expressed in Xenopus oocytes by whole cell voltage clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMed
TargetBile salt export pump(Human)
Amgen

Curated by ChEMBL
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 1.33E+5nMAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/3/2019
Entry Details Article
PubMed
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 1.33E+5nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/3/2019
Entry Details Article
PubMed
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 1.33E+5nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/3/2019
Entry Details Article
PubMed
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 1.33E+5nMAssay Description:Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/3/2019
Entry Details Article
PubMed
TargetBile salt export pump(Human)
Amgen

Curated by ChEMBL
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 1.35E+5nMAssay Description:Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate t...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2019
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 2.63E+5nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 2.63E+5nMAssay Description:Inhibition of human ERG channel in HEK293 cells by voltage-clamp methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/21/2013
Entry Details Article
PubMed
TargetMultidrug and toxin extrusion protein 1(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 5.00E+5nMAssay Description:Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetPotassium channel subfamily K member 2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 1.80E+5nMAssay Description:Inhibition of human TREK-1 expressed in HEK293 cells by patch-clamp techniqueMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 2.40E+5nMAssay Description:Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2018
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily A member 5(Human)
Cardiome Pharma

Curated by ChEMBL
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 2.19E+6nMAssay Description:Inhibition of human potassium channel Kv1.5 by patch-clamp methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/10/2012
Entry Details Article
PubMed
TargetSodium channel protein type 5 subunit alpha(Human)
Daiichi Sankyo Co.

Curated by ChEMBL
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 1.08E+5nMAssay Description:Inhibition of human heart sodium channel Nav1.5 by patch-clamp methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/10/2012
Entry Details Article
PubMed
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 1.21E+6nMAssay Description:Inhibition of rat potassium channel Kv4.2 by patch-clamp methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/10/2012
Entry Details Article
PubMed
TargetPotassium channel subfamily K member 18(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 1.00E+5nMAssay Description:Channel blocking activity at human TRESK channelMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/14/2018
Entry Details Article
PubMed
TargetVoltage-dependent L-type calcium channel subunit alpha-1C(Rabbit)
Ortho Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 1.00E+6nMAssay Description:Inhibition of [3H]nitrendipine binding to calcium channels in Rabbit cardiac muscle.More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/16/2012
Entry Details Article
PubMed
TargetPotassium channel subfamily K member 2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
Affinity DataIC50: 2.07E+5nMAssay Description:Inhibition of of human TREK1 expressed in HEK293 cells assessed as reduction in channel currentsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/22/2017
Entry Details Article
PubMed

Activity Spreadsheet -- ITC Data from BindingDB

Found 1 hit for monomerid = 50017662   

HostPNGBDBM197280(SAMPL3, H1)
University of California San Diego

GuestPNGBDBM50017662(CHEMBL79 | N-(2,6-dimethylphenyl)-N(2),N(2)-diethy...)
ITC DataΔG°: -6.07kcal/mole logk: 2.60E+4
pH: 7.4 T: 24.85°C