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  180 KI  19 IC50  1 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 19 hits for monomerid = 35254   

TargetD(2) dopamine receptor(Homo sapiens (Human))
Merck Sharp And Dohme Research Laboratories

Curated by ChEMBL
LigandPNGBDBM35254(2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3...)
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 ArticlePubMedDrugBank

Target5-hydroxytryptamine receptor 2C(Homo sapiens (Human))
Merck Sharp And Dohme Research Laboratories

Curated by ChEMBL
LigandPNGBDBM35254(2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3...)
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 ArticlePubMedDrugBank

TargetHistamine H1 receptor(RAT)
Universit£

Curated by ChEMBL
LigandPNGBDBM35254(2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3...)
Affinity DataIC50:  13nMAssay Description:Displacement of [3H]mepyramine from H1R in rat brainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Universita Di Siena

Curated by ChEMBL
LigandPNGBDBM35254(2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3...)
Affinity DataIC50:  231nMAssay Description:Inhibition of human ERG channelMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Universita Di Siena

Curated by ChEMBL
LigandPNGBDBM35254(2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3...)
Affinity DataIC50:  181nMAssay Description:Inhibition of human ERG potassium channelMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Universita Di Siena

Curated by ChEMBL
LigandPNGBDBM35254(2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3...)
Affinity DataIC50:  182nMAssay Description:Inhibitory concentration against potassium channel HERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Universita Di Siena

Curated by ChEMBL
LigandPNGBDBM35254(2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3...)
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 ArticlePubMed
TargetBile salt export pump(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM35254(2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3...)
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 ArticlePubMed
TargetATP-binding cassette sub-family C member 2(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM35254(2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3...)
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 ArticlePubMed
TargetATP-binding cassette sub-family C member 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM35254(2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3...)
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 ArticlePubMed
TargetATP-binding cassette sub-family C member 4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM35254(2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3...)
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 ArticlePubMed
TargetBile salt export pump(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM35254(2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3...)
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
Target5-hydroxytryptamine receptor 2A(Homo sapiens (Human))
Sumitomo Dainippon Pharma.

Curated by ChEMBL
LigandPNGBDBM35254(2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3...)
Affinity DataIC50:  9nMAssay Description:Inhibitory concentration against human 5-HT2A receptor in BEK cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(2) dopamine receptor(Rattus norvegicus (rat))
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM35254(2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3...)
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 ArticlePubMed
TargetD(4) dopamine receptor(Homo sapiens (Human))
Solvay Pharma

Curated by ChEMBL
LigandPNGBDBM35254(2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3...)
Affinity DataIC50:  173nMAssay Description:Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Universita Di Siena

Curated by ChEMBL
LigandPNGBDBM35254(2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3...)
Affinity DataIC50:  182nMAssay Description:Inhibition of human Potassium channel HERG expressed in mammalian cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target5-hydroxytryptamine receptor 2A(Homo sapiens (Human))
Sumitomo Dainippon Pharma.

Curated by ChEMBL
LigandPNGBDBM35254(2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3...)
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 ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Universita Di Siena

Curated by ChEMBL
LigandPNGBDBM35254(2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3...)
Affinity DataIC50:  229nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target5-hydroxytryptamine receptor 2A(Homo sapiens (Human))
Sumitomo Dainippon Pharma.

Curated by ChEMBL
LigandPNGBDBM35254(2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3...)
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 ArticlePubMed