BDBM35254 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3-b][1,5]benzodiazepine::CHEMBL715::Olansek::US8802672, Olanzapine::Zyprexa::olanzapine

SMILES CN1CCN(CC1)C1=Nc2ccccc2Nc2sc(C)cc12

InChI Key InChIKey=KVWDHTXUZHCGIO-UHFFFAOYSA-N

Data  182 KI  19 IC50  1 Kd  1 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 203 hits for monomerid = 35254   

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

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataIC50: 229nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataIC50: 100nMAssay Description:Antagonist activity against 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as reduction in [35S]-GTPgammaS binding incu...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
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataIC50: 182nMAssay Description:Inhibition of human Potassium channel HERG expressed in mammalian cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(4) dopamine receptor(Human)
Hoechst Marion Roussel

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataIC50: 173nMAssay Description:Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Rat)
Hoechst Marion Roussel

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataIC50: 158nMAssay Description:Binding affinity towards Dopamine receptor D2 was determined in rat striatal homogenate using [3H]- spiperone as radioligandMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataIC50: 9nMAssay Description:Inhibitory concentration against human 5-HT2A receptor in BEK cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Indiana University School of Medicine

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataIC50: 10nMAssay Description:Displacement of [3H]raclopride from D2 receptor in human corpus striatum after 30 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2C(Human)
Indiana University School of Medicine

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataIC50: 71nMAssay Description:Displacement of [3H]mesulergine from 5-HT2C receptor in human frontal cortex after 30 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataIC50: 7nMAssay Description:Displacement of [3H]ketanserin from 5-HT2A receptor in human frontal cortex after 30 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H1 receptor(Rat)
The Johns Hopkins University School of Medicine

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataIC50: 13nMAssay Description:Displacement of [3H]mepyramine from H1R in rat brainMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataIC50: 231nMAssay Description:Inhibition of human ERG channelMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataIC50: 181nMAssay Description:Inhibition of human ERG potassium channelMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataIC50: 182nMAssay 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
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataIC50: 182nMAssay 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
TargetHistamine H1 receptor(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKd:  0.0870nMAssay Description:Binding affinity to human histamine H1 receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBile salt export pump(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataIC50: 5.46E+4nMAssay 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 DepthDetails Article
PubMed
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
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
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
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
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
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
TargetBile salt export pump(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
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
TargetMuscarinic acetylcholine receptor M1(Human)
Sumitomo Dainippon Pharma.

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataEC50: >1.00E+5nMAssay Description:Agonist activity at muscarinic M1 receptor (unknown origin) expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H1 receptor(Rat)
The Johns Hopkins University School of Medicine

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  0.300nMAssay Description:Half-maximal inhibition of [3H]7-OH-DPAT binding to Histamine H1 receptor in rat tissue homogenateMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  0.420nMAssay Description:Binding affinity to human 5HT2A receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H1 receptor(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  1.20nMAssay Description:Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  1.60nMAssay Description:Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  1.90nMAssay Description:Binding affinity for human 5-hydroxytryptamine 2A receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  1.90nMAssay Description:Binding affinity towards human serotonin 5-hydroxytryptamine 2A receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  1.90nMAssay Description:Displacement of [3H]-ketanserin from human human 5-HT2A receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistone H1.0(Human)
Intra-Cellular Therapies

US Patent
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  2nMAssay Description:Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetHistamine H1 receptor(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  2nMAssay Description:Inhibition of histamine H1 receptor (unknown origin)More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Indiana University School of Medicine

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  2.10nMAssay Description:Binding affinity towards human D2 dopamine receptor.More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetMuscarinic acetylcholine receptor M1(Human)
Sumitomo Dainippon Pharma.

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  2.10nMAssay Description:Binding affinity towards human M1 receptor.More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  2.30nMAssay Description:Inhibition of [125I]R91150 binding to human 5-hydroxytryptamine 2A receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  2.5nMAssay Description:Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.More data for this Ligand-Target Pair
In DepthDetails
US Patent

Target5-hydroxytryptamine receptor 2A(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  2.5nMAssay Description:Displacement of [125]DOI from human recombinant full length 5HT2A receptor expressed in HEK293E cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H1 receptor(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  2.80nMAssay Description:Binding affinity to human cloned histamine H1 receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2C(Human)
Indiana University School of Medicine

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  2.80nMAssay Description:Binding affinity towards human 5-hydroxytryptamine 2C receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  3.30nMAssay Description:Displacement of [3H]Ketanserin from human 5-HT2A receptor by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  3.30nMAssay Description:Binding affinity to human cloned 5HT2A receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H1 receptor(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  3.5nMAssay Description:Binding affinity towards human histamine H1 receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  4nMAssay Description:Compounds were evaluated the inhibition of [3H] nisoxetine binding to MDCK-Net6 cells, stably transfected with the human norepinephrine transporter (...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  4nMAssay Description:Binding affinity towards human 5-HT2A receptor in BEK cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  4nMAssay Description:Binding affinity to 5HT2A receptor (unknown origin)More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Rat)
Università

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  4nMAssay Description:Inhibition of [3H]ketanserin binding to rat 5-hydroxytryptamine 2A receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Rat)
Università

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  4nMAssay Description:Displacement of [3H]ketanserin from 5HT2A receptor in CRL:CD(SD)BR-COBS rat cortex by scintillation spectrometryMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Rat)
Università

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  4nMAssay Description:Displacement of [3H]ketanserin from 5HT2A receptor in CRL:CD(SD)BR-COBS rat cortex by scintillation spectrometryMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Rat)
Università

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  4nMAssay Description:In vitro binding affinity towards 5-hydroxytryptamine 2A receptor in rat tissue homogenate using [3H]ketanserin as radioligandMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Rat)
Università

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  4nMAssay Description:Half-maximal inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenateMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Target5-hydroxytryptamine receptor 2A(Human)
Fudan University

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  4nMAssay Description:Displacement of [3H]ketanserin from 5-HT2A receptor in human frontal cortex after 30 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetD(2) dopamine receptor(Human)
Indiana University School of Medicine

Curated by ChEMBL
LigandPNGBDBM35254(CHEMBL715 | 2-methyl-4-(4-methylpiperazin-1-yl)-10...)
Affinity DataKi:  4nMAssay Description:Displacement of [3H]-raclopride from human D2LR expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
Displayed 1 to 50 (of 203 total ) | Next | Last >>