BDBM50003659 5H-dibenzo[b,f]azepine-5-carboxamide::CARBAMAZEPINE::CARBATROL::CHEMBL108::DIBENZO[B,F]AZEPINE-5-CARBOXYLIC ACID AMIDE(CARBAMAZEPINE)::EPITOL::EQUETRO::G-32883::TEGRETOL::TEGRETOL-XR::TERIL::US9138393, Carbamazepine::US9144538, Carbamazepine

SMILES c1ccc2c(c1)C=Cc3ccccc3N2C(=O)N

InChI Key InChIKey=FFGPTBGBLSHEPO-UHFFFAOYSA-N

Data  10 KI  22 IC50  2 Kd  2 EC50

PDB links: 2 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 36 hits for monomerid = 50003659   

LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
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
TargetP2X purinoceptor 4(Human)
University of Bonn

Curated by ChEMBL
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataIC50: 1.00E+5nMAssay Description:Antagonist activity at human P2X4 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx preincubate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/25/2014
Entry Details Article
PubMed
TargetSodium channel protein type 1/2/3 subunit alpha(Rat)
University of Alabama

Curated by ChEMBL
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataIC50: 1.31E+5nMAssay Description:Displacement of [3H]batrachotoxin A 20alpha-benzoate (BTX-B) from rat cerebral cortex voltage-gated sodium channelMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/9/2019
Entry Details Article
PubMed
TargetSodium channel protein type 1/2/3 subunit alpha(Rat)
University of Alabama

Curated by ChEMBL
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataIC50: 1.67E+5nMAssay 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 1/2/3 subunit alpha(Rat)
University of Alabama

Curated by ChEMBL
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataIC50: 1.31E+5nMAssay Description:In vitro inhibition of [3H]-BTX-B binding to sodium channels in rat brain synapto-neurosomesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2018
Entry Details Article
PubMed
TargetBile salt export pump(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataIC50: 1.00E+6nMAssay Description:Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/28/2019
Entry Details Article
PubMed
TargetBile salt export pump(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
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
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
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
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
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
TargetSodium channel protein type 9 subunit alpha(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataIC50: 2.20E+4nMAssay Description:Blockade of human Nav1.7 channel expressed in HEK293 cells by FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetSodium channel protein type 1/2/3 subunit alpha(Rat)
University of Alabama

Curated by ChEMBL
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataIC50: 2.10E+5nMAssay Description:Displacement of [3H]BTX from voltage-gated sodium channel of rat cortical synaptosomesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2020
Entry Details Article
PubMed
TargetCytochrome P450 2B6(Human)
Amgen

Curated by ChEMBL
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataEC50:  1.45E+5nMAssay Description:Induction of CYP2B6 activity in human donor hepatocytes assessed as hydroxybupropion formation after 48 hrs by LC/MS methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetSodium channel protein type 1/2/3 subunit alpha(Rat)
University of Alabama

Curated by ChEMBL
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataIC50: 1.31E+5nMAssay Description:In vitro inhibition of Voltage-gated sodium channel by the displacement of [3H]batrachotoxin A 20-alpha-benzoate in rat brain cerebral cortex synapto...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2020
Entry Details Article
PubMed
TargetSodium channel protein type 1/2/3 subunit alpha(Rat)
University of Alabama

Curated by ChEMBL
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataIC50: 1.31E+5nMAssay Description:Inhibition of [3H]BTX-B binding to neurotoxin site 2 of sodium channel of rat cerebral cortex synaptoneurosomesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/21/2020
Entry Details Article
PubMed
TargetFrizzled-8(Mouse)
University of Oxford

Curated by ChEMBL
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataKd:  1.68E+4nMAssay Description:Binding affinity to immobilized mouse C-terminal Rhinovirus 3C cleavage site-fused 6xHis-tagged Frizzled-8 CRD (Q33 to G173 resideus) transfected wit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetSodium channel protein type 1 subunit alpha(Human)
Daiichi Sankyo Co.

Curated by ChEMBL
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataIC50: 1.00E+5nMAssay Description:Inhibition of human Nav1.1 at -60 mV holding potential 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
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataIC50: 4.68E+4nMAssay Description:Inhibition of human Nav1.5 at -60 mV holding potential 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)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataIC50: 9.13E+4nMAssay Description:Inhibition of human Nav1.7 at -60 mV holding potential by automated patch-clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetMajor prion protein(Human)
Institut F£R Molekularbiologie Und Biophysik

Curated by ChEMBL
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataEC50: >1.00E+4nMAssay Description:Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/29/2012
Entry Details Article
PubMed
TargetCytochrome P450 3A4(Human)
The Procter & Gamble

US Patent
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataIC50: 1.00E+4nMAssay Description:A commercially available P450-GLO Assay kit (Promega Corporation, Madison Wis.) is used to screen various compounds for CYP3A4A inhibition activity. ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/6/2016
Entry Details
Go to US Patent

TargetCytochrome P450 3A4(Human)
The Procter & Gamble

US Patent
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataIC50: 1.00E+4nMAssay Description:Cytochrome P450 is a large and diverse group of enzymes that catalyze the oxidation of organic substances. Some members of the CYP family contribute ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/13/2016
Entry Details
Go to US Patent

TargetBile salt export pump(Rat)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataIC50: 1.00E+6nMAssay Description:Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate up...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/8/2016
Entry Details Article
PubMed
TargetBile salt export pump(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataIC50: 1.00E+6nMAssay Description:Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptakeMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/8/2016
Entry Details Article
PubMed
TargetAlbumin(Rat)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataKd:  1.03E+5nMAssay Description:Binding affinity to Wistar rat serum albuminMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/5/2016
Entry Details Article
PubMed
TargetCytochrome P450 2J2(Human)
Tongji University

Curated by ChEMBL
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/3/2016
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataIC50: 1.05E+5nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
Target5-hydroxytryptamine receptor 2C(Rat)
Sri International

Curated by PDSP Ki Database
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataKi: >1.00E+4nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2012
Entry Details
PubMed
Target5-hydroxytryptamine receptor 2A(Rat)
Sri International

Curated by PDSP Ki Database
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataKi: >1.00E+4nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2012
Entry Details
PubMed
Target5-hydroxytryptamine receptor 1A(Human)
Sri International

Curated by PDSP Ki Database
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataKi: >1.00E+4nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2012
Entry Details
PubMed
TargetGlutamate receptor ionotropic, NMDA 1(Rat)
University of Colorado

Curated by PDSP Ki Database
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataKi: >1.00E+4nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/17/2012
Entry Details
PubMed
TargetD(2) dopamine receptor(Human)
Sri International

Curated by PDSP Ki Database
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataKi: >1.00E+4nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2012
Entry Details
PubMed
TargetD(1A) dopamine receptor(Human)
Sri International

Curated by PDSP Ki Database
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataKi: >1.00E+4nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2012
Entry Details
PubMed
Target5-hydroxytryptamine receptor 3A(Mouse)
Sri International

Curated by PDSP Ki Database
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataKi: >1.00E+4nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2012
Entry Details
PubMed
TargetHistamine H1 receptor(Human)
Mayo Foundation

Curated by PDSP Ki Database
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataKi: >1.00E+4nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/26/2011
Entry Details Article
PubMed
TargetSodium channel protein type 9 subunit alpha(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataKi:  3.27E+4nMAssay Description:Inhibition of Nav1.7 (unknown origin) by electrophysiological assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/9/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetSodium channel protein type 4 subunit alpha(Human)
Purdue Pharma

Curated by ChEMBL
LigandPNGBDBM50003659(5H-dibenzo[b,f]azepine-5-carboxamide | TEGRETOL | ...)
Affinity DataKi:  5.20E+4nMAssay Description:Affinity for inactive human SkM1 sodium channel expressed in HEK293 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMed