BDBM50020712 10,11-dihydro-5-(gamma-dimethylaminopropylidene)-5H-dibenzo(a,d)cycloheptene::10,11-dihydro-N,N-dimethyl-5H-dibenzo(a,d)heptalene-Delta(5),gamma-propylamine::3-(10,11-dihydro-5H-dibenzo(a,d)cyclohepten-5-ylidene)-N,N-dimethyl-1-propanamine::3-(10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-ylidene)-N,N-dimethylpropan-1-amine::3-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)-N,N-dimethylpropan-1-amine::5-(3-dimethylaminopropylidene)-10,11-dihydro-5H-dibenzo(a,d)cycloheptatriene::5-(3-dimethylaminopropylidene)-10,11-dihydro-5H-dibenzo(a,d)cycloheptene::5-(gamma-dimethylaminopropylidene)-5H-dibenzo[a,d][1,4]cycloheptadiene::AMITRIPTYLINE::Amitriptylin::CHEMBL629::US20240189287, Compound Amitriptyline

SMILES [#6]-[#7](-[#6])-[#6]-[#6]\[#6]=[#6]-1/c2ccccc2-[#6]-[#6]-c2ccccc-12

InChI Key InChIKey=AGLIFTAZEUCEAB-UHFFFAOYSA-N

Data  81 KI  40 IC50  5 Kd  1 EC50

  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 127 hits for monomerid = 50020712   

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Queen'S University At Kingston

US Patent
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 1.00E+3nMpH: 7.4 T: 2°CAssay Description:Approximately 5-20 μg of purified GST-RET proteins were incubated with 1 mM ATP in 20 μL kinase buffer (10 mM Tris-HCl, 5 mM MgCl2, pH 7.4)...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetTransporter(Rat)
TBA

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 2.50E+3nMAssay Description:Inhibition of the NE [3H]norepinephrine uptake by rat brain slices In vitroMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 8.50E+3nMAssay Description:In vitro inhibition of [14C]5-HT transporter uptake by rat brain slicesMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHigh affinity nerve growth factor receptor(Human)
Southmead Hospital

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataEC50:  8.60E+4nMAssay Description:Antagonist activity at full length glycosylated human TrkA expressed in HEKN3S cells cells assessed as reduction in NGF-induced ERK 42/44 phosphoryla...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHigh affinity nerve growth factor receptor(Human)
Southmead Hospital

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 6.00E+4nMAssay Description:Displacement of [125I]NGF from full length human TrkA expressed in HEKN3S cells cells by gamma counting based radioligand competition assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHigh affinity nerve growth factor receptor(Human)
Southmead Hospital

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataKd:  2.20E+6nMAssay Description:Binding affinity to F303 residue of human recombinant TrkAIg2-NMR construct expressed in Escherichia coli by 1H-15N HSQC NMR spectroscopyMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHigh affinity nerve growth factor receptor(Human)
Southmead Hospital

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataKd:  2.10E+6nMAssay Description:Binding affinity to C345 residue of human recombinant TrkAIg2-NMR construct expressed in Escherichia coli by 1H-15N HSQC NMR spectroscopyMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHigh affinity nerve growth factor receptor(Human)
Southmead Hospital

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataKd:  2.10E+6nMAssay Description:Binding affinity to V305 residue of human recombinant TrkAIg2-NMR construct expressed in Escherichia coli by 1H-15N HSQC NMR spectroscopyMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHigh affinity nerve growth factor receptor(Human)
Southmead Hospital

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataKd:  1.80E+6nMAssay Description:Binding affinity to T292 residue of human recombinant TrkAIg2-NMR construct expressed in Escherichia coli by 1H-15N HSQC NMR spectroscopyMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetVoltage-dependent L-type calcium channel subunit alpha-1C(Rat)
Jagiellonian University

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 2.32E+4nMAssay Description:Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytesMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 7 subunit alpha(Human)
University of Oxford

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of Na channel (species unknown)More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 1.16E+4nMAssay Description:Inhibition of voltage-gated L-type Ca channel (species unknown)More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 3.28E+3nMAssay Description:Inhibition of hERG K channelMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetAlbumin(Rat)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataKd:  1.34E+5nMAssay Description:Binding affinity to Wistar rat serum albuminMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetVoltage-dependent L-type calcium channel subunit alpha-1C(Rat)
Jagiellonian University

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 3.75E+3nMAssay Description:Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytesMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human Potassium channel HERG expressed in mammalian cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H1 receptor(Rat)
Universidad De Valencia

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 0.0200nMAssay Description:Compound tested for its inhibitory activity against Histamine H1 receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetAlpha-1A adrenergic receptor(Rat)
Universidad De Valencia

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 0.0200nMAssay Description:Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H2 receptor(Guinea pig)
Universidad De Valencia

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 660nMAssay Description:Inhibitory activity against brain adenylate cyclase Histamine H2 receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 1.00E+4nMAssay Description:K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 9 subunit alpha(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 7.00E+3nMAssay Description:Inhibition of recombinant human NaV1.7 alpha subunit expressed in HEK293 cells at -90 mV holding potential by patch clamp electrophysiological assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 5 subunit alpha(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 1.60E+3nMAssay Description:Inhibition of human NaV1.5 alpha subunit expressed in CHOK1 cells at -90 mV holding potential by patch clamp electrophysiological assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 9 subunit alpha(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 1.00E+3nMAssay Description:Inhibition of recombinant human NaV1.7 alpha subunit expressed in HEK293 cells at -65 mV holding potential by patch clamp electrophysiological assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 2 subunit alpha(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 3.10E+3nMAssay Description:Inhibition of human NaV1.2 alpha subunit expressed in CHOK1 cells at -65 mV holding potential by patch clamp electrophysiological assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 1.00E+4nMAssay 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 DepthDetails Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open stateMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSolute carrier family 22 member 1(Human)
Uppsala University

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 1.69E+4nMAssay Description:Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopyMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human ERG in MCF7 cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibitory concentration against potassium channel HERGMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human ERG expressed in CHO cells by whole cell patch clamp techniqueMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBile salt export pump(Human)
Amgen

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
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 DepthDetails Article
PubMed
TargetBile salt export pump(Human)
Amgen

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
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 Article
PubMed
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
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 DepthDetails Article
PubMed
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
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 DepthDetails Article
PubMed
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
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 DepthDetails Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 3.29E+3nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 9.60E+3nMAssay Description:Inhibition of [3H]-dofetilide binding to human ERG expressed in HEK293 cell membranes measured after 1 hr by liquid scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 9.60E+3nMAssay Description:Inhibition of [3H]-dofetilide binding to human ERG expressed in HEK293 cell membranes measured after 1 hr by liquid scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 3.00E+3nMAssay Description:Inhibition of human ERG expressed in CHO cells at -80 mV holding potential by whole-cell patch clamp assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 3.00E+3nMAssay Description:Inhibition of human ERG expressed in CHO cells at -80 mV holding potential by whole-cell patch clamp assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetVoltage-dependent N-type calcium channel subunit alpha-1B(Human)
The University of Queensland

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 1.20E+4nMAssay Description:Inhibition of endogenous human CaV2.2 in human SH-SY5Y cells in presence of nifedipine by Calcium 4 dye based calcium influx fluorescence-imaging ass...More data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 3.20E+3nMAssay Description:Inhibition of human ERG at -90 mV holding potentialMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 1.81E+3nMAssay Description:Inhibition of hERG expressed in HEK293 cells by automated patch clamp assayMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 2.58E+3nMAssay Description:Cardiotoxicity potential of BNS808 and BNS822 on the hERG potassium channels was evaluated using the automated patch clamp method (SyncroPatch 384PE)...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetPoly [ADP-ribose] polymerase 1(Human)
Niper Guwahati

Curated by ChEMBL
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataIC50: 1.65E+3nMAssay Description:Inhibition of human N-terminal His6-tagged PARP1 CD (662 to 1011 residues) expressed in Escherichia coli BL21 incubated for 60 mins by chemiluminesce...More data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetHistamine H1 receptor(Guinea pig)
Emory University

Curated by PDSP Ki Database
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataKi:  0.170nMMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetHistamine H1 receptor(Human)
Mayo Foundation

Curated by PDSP Ki Database
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataKi:  0.670nMMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H1 receptor(Human)
Mayo Foundation

Curated by PDSP Ki Database
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataKi:  0.950nMMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H1 receptor(Human)
Mayo Foundation

Curated by PDSP Ki Database
LigandPNGBDBM50020712(CHEMBL629 | Amitriptylin | 10,11-dihydro-N,N-dimet...)
Affinity DataKi:  1.12nMAssay Description:Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
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