BDBM50031299 6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamine::6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamine(lamotrigine)::6-(2,3-dichlorophenyl)-1,2,4-triazine-3,5-diamine::BW-430C::CHEMBL741::LAMOTRIGINE::Lamictal::Lamictal cd

SMILES Nc1nnc(c(N)n1)-c1cccc(Cl)c1Cl

InChI Key InChIKey=PYZRQGJRPPTADH-UHFFFAOYSA-N

Data  2 KI  26 IC50

PDB links: 1 PDB ID matches this monomer.

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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 28 hits for monomerid = 50031299   

TargetDihydrofolate reductase(Escherichia coli)
Georgia Institute Of Technology

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataKi:  1.52E+4nMAssay Description:Inhibition of Escherichia coli DHFR assessed as NADP formation by quadratic Morrison plot analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 4 subunit alpha(Homo sapiens (Human))
Purdue Pharma

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataKi:  1.70E+4nMAssay Description:Affinity for inactive human SkM1 sodium channel expressed in HEK293 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 2 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50:  1.70E+4nMAssay Description:Inhibition of human Nav1.2 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 3 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50:  1.70E+4nMAssay Description:Inhibition of human Nav1.3 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50:  1.70E+4nMAssay Description:Inhibition of human Nav1.7 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assayMore data for this Ligand-Target Pair
TargetSodium channel protein type 10 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50:  9.80E+4nMAssay Description:Inhibition of human Nav1.8 expressed in HEK293 cells assessed as reduction in blue fluorescent signal by VSP-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent L-type calcium channel subunit alpha-1C(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50:  1.58E+6nMAssay Description:Inhibition of long-lasting type calcium current (hICa) in Chinese Hamster Ovary (CHO) cells expressing hCav1.2 measured using IonWorks Quattro automa...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50:  3.98E+4nMAssay Description:Inhibition of fast sodium current (INa) in HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platformMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50:  3.98E+5nMAssay Description:Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG measured using I...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50:  2.51E+5nMAssay Description:Inhibition of rapid delayed inward rectifying potassium current (IKr) measured using manual patch clamp assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50:  1.00E+5nMAssay Description:Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells transfected with human Nav1.5 measured using IonWorks Quattro automat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50:  2.51E+5nMAssay Description:Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) cells stable expressing hERG measured using IonW...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent L-type calcium channel subunit alpha-1C(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50:  1.26E+6nMAssay Description:Inhibition of long-lasting type calcium current (ICaL) in HEK293 cells (alpha1C/beta2a/alpha2delta1) cells measured using IonWorks Barracuda automat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 10 subunit alpha(Rattus norvegicus (Rat))
Abbott Laboratories

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50:  2.50E+4nMAssay Description:Blockade of Nav1.8 channel in rat dorsal root ganglion neurons assessed as inhibition of TTX-R current by whole cell patch clamp techniqueMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 10 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50:  9.60E+4nMAssay Description:Inhibition of human recombinant Nav1.8 channel expressed in HEK293 cells by whole cell voltage clamp techniqueMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 2 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50:  1.00E+4nMAssay Description:Inhibition of human recombinant Nav1.2 channel expressed in HEK293 cells by whole cell voltage clamp techniqueMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50:  6.20E+4nMAssay Description:Inhibition of human recombinant Nav1.5 channel expressed in HEK293 cells by whole cell voltage clamp techniqueMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 2 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of human Nav1.2 channel expressed in HEK cells by patch-clamp electrophysiology methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSigma non-opioid intracellular receptor 1(RAT)
Pharmacia & Upjohn

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of [3H]pentazocine binding to Opioid receptor sigma 1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 1/2/3 subunit alpha(Rattus norvegicus)
Pharmacia & Upjohn

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of [3H]saxitoxin binding to rat brain sodium channelMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 2 subunit alpha(Rattus norvegicus)
Johnson & Johnson Pharmaceutical Research & Development

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50:  3.50E+4nMAssay Description:Inhibition of rat Nav1.2 channel expressed in chinese hamster CHL1610 cells at preconditioning pulse of -67 mV after 2 to 3 mins by whole-cell patch-...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50:  2.29E+5nMAssay Description:Inhibition of human ERG channel in HEK293 cells by voltage-clamp methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 1/2/3 subunit alpha(Rattus norvegicus)
Pharmacia & Upjohn

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50:  3.10E+4nMAssay Description:Concentration required to inhibit [3H]BTX binding to Sodium channel of rat brainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBile salt export pump(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
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 DepthDetails ArticlePubMed
TargetSodium channel protein type 1/2/3 subunit alpha(Rattus norvegicus)
Pharmacia & Upjohn

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50:  1.14E+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 DepthDetails ArticlePubMed
TargetDihydrofolate reductase(Escherichia coli)
Georgia Institute Of Technology

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50:  3.49E+5nMAssay Description:Inhibition of Escherichia coli DHFR assessed as NADP formationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 1/2/3 subunit alpha(Rattus norvegicus)
Pharmacia & Upjohn

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50:  1.86E+5nMAssay Description:Inhibition of [3H]batrachotoxin binding to rat brain sodium channelMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily E/KQT member 1(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM50031299(6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamin...)
Affinity DataIC50:  1.58E+5nMAssay Description:Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells expressing hKvLQT1/hminK measured using Ion...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed