BDBM22914 CHEMBL260374::N-cyclohexyl-4-(1H-imidazol-5-yl)piperidine-1-carbothioamide::Thioperamide::US11622967, Compound Thioperamide

SMILES S=C(NC1CCCCC1)N1CCC(CC1)c1cnc[nH]1

InChI Key InChIKey=QKDDJDBFONZGBW-UHFFFAOYSA-N

Data  167 KI  14 IC50  1 Kd  11 EC50

PDB links: 1 PDB ID matches 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 193 hits for monomerid = 22914   

TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  1.5nMAssay Description:Antagonistic activity of the compound was evaluated against histamine H3 receptor using [3H]- N-alpha-methylhistamine as radioligand in experiment 2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHrh3 protein(RAT)
Gliatech

Curated by PDSP Ki Database
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  1.80nMMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetHrh3 protein(RAT)
Gliatech

Curated by PDSP Ki Database
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  1.99nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(GUINEA PIG)
UnitÉ

Curated by PDSP Ki Database
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
In DepthDetails ArticlePubMed
TargetHrh3 protein(RAT)
Gliatech

Curated by PDSP Ki Database
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
In DepthDetails PubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  2nMAssay Description:In vitro antagonistic activity against histamine H3 receptor on rat cerebral cortexMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  2nMAssay Description:Binding affinity against H3 receptor in rat cerebral cortex membranes was evaluated using [3H]N-methyl-histamine as radioligandMore data for this Ligand-Target Pair
In DepthDetails
TargetHrh3 protein(RAT)
Gliatech

Curated by PDSP Ki Database
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  2.10nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  2.10nMAssay Description:Displacement of [3H]-(R)alpha-MeHA from rat brain H3 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  2.70nMAssay Description:Inhibition of rat Histamine H3 receptor using [3H]-N-alpha-methyl histamineMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHrh3 protein(RAT)
Gliatech

Curated by PDSP Ki Database
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  3.21nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHrh3 protein(RAT)
Gliatech

Curated by PDSP Ki Database
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  3.63nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  3.63nMAssay Description:In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing rat histamine H3 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHrh3 protein(RAT)
Gliatech

Curated by PDSP Ki Database
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  3.98nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  3.98nMAssay Description:Binding affinity to rat cortical histamine H3 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  3.98nMAssay Description:In vitro antagonistic activity tested against Histamine H3 receptor on synaptosomes from rat cerebral cortexMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(GUINEA PIG)
UnitÉ

Curated by PDSP Ki Database
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  3.98nMAssay Description:Antagonistic activity for Histamine H3 receptor on electrically evoked guinea-pig ileum contractionMore data for this Ligand-Target Pair
In DepthDetails Article
TargetHrh3 protein(RAT)
Gliatech

Curated by PDSP Ki Database
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  3.98nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHrh3 protein(RAT)
Gliatech

Curated by PDSP Ki Database
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
In DepthDetails PubMed
TargetHrh3 protein(RAT)
Gliatech

Curated by PDSP Ki Database
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
In DepthDetails PubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  4nMAssay Description:In vitro antagonistic activity of the compound against Histamine H3 receptor on Synaptosomes of rat cerebral cortex.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  4nMAssay Description:Rat Histamine H3 receptor antagonism determined by [K+] - evoked depolarization-induced release of [3H]-histamine from rat cerebral cortex synaptosom...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  4nMAssay Description:In vitro antagonist potency at Histamine H3 receptor measured as K+-evoked [3H]-histamine release from synaptosomes of rat cerebral cortex.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  4nMAssay Description:In vitro Histamine H3 receptor antagonist activity in an assay with K+-evoked depolarization-induced release of [3H]-histamine from synaptosomes of r...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  4nMAssay Description:Effect at histamine H3 receptors (in vitro) on synaptosomes of rat cerebral cortex assayed by functional H3-receptor assay.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  4nMAssay Description:Histamine H3 receptor antagonist activity in an assay with K+ evoked depolarization-induced release of [3H]-histamine from rat synaptosomes.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  4nMAssay Description:In vitro inhibitory activity against Histamine H3 receptor for K+ evoked depolarization-induced release of [3H]-histamine from synaptosomes of rat ce...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  4nMAssay Description:In vitro inhibitory activity against against histamine H3 receptor using [3H]-Histamine as radioligand from rat cerebral cortex synaptosomesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  4nMAssay Description:In vitro binding affinity against rat histamine H3 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  4nMAssay Description:Effect on histamine H3 receptors in vitro, on synaptosomes of rat cerebral cortex for the release of [3H]histamineMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  4nMAssay Description:In vitro antagonistic activity against histamine H3-receptor in an assay with K+-evoked depolarisation-induced release of [3H]histamine of synaptosom...More data for this Ligand-Target Pair
In DepthDetails Article
TargetHrh3 protein(RAT)
Gliatech

Curated by PDSP Ki Database
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  4.20nMMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetHrh3 protein(RAT)
Gliatech

Curated by PDSP Ki Database
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  4.30nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  4.30nMAssay Description:In vitro antagonism of the histamine H3-receptor in the rat cerebral cortex.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  4.30nMAssay Description:Antagonistic activity of the compound was evaluated against histamine H3 receptor using [3H]- N-alpha-methylhistamine as radioligand in experiment 1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  4.30nMAssay Description:Histamine H3 receptor affinity of compound was determined in rat cortical membranes using the H3 selective agonist ligand, [3H]N-alpha-methylhistamin...More data for this Ligand-Target Pair
In DepthDetails Article
TargetHistamine H3 receptor(GUINEA PIG)
UnitÉ

Curated by PDSP Ki Database
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  4.57nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Mus musculus)
Tsukuba Research Institute

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  4.80nMAssay Description:Displacement of 3-([1,1,1-3H]methyl)-2-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone from mouse histamine H3 receptor expressed in HE...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHrh3 protein(RAT)
Gliatech

Curated by PDSP Ki Database
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  6.46nMMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  6.5nMAssay Description:Displacement of [125I]-iodoproxyfan from human striatal full length H3 receptor expressed in CHOK1 cells after 60 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  6.5nMAssay Description:Binding affinity of the compound to rat Histamine H3 receptor in CHO-K1 cells using [125I]-iodoproxyfan as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine receptor H3(Dog)
Abbott Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  6.76nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  7nMAssay Description:Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHrh3 protein(RAT)
Gliatech

Curated by PDSP Ki Database
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  7.08nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(GUINEA PIG)
UnitÉ

Curated by PDSP Ki Database
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  7.30nMAssay Description:Binding affinity against H3 receptor in guinea pig brain using [3H]-N-alpha-methyl histamine as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(GUINEA PIG)
UnitÉ

Curated by PDSP Ki Database
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  7.30nMAssay Description:Inhibition of N-alpha-methylhistamine binding to histamine H3 receptor of guinea pig brain membranesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHrh3 protein(RAT)
Gliatech

Curated by PDSP Ki Database
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  7.5nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHrh3 protein(RAT)
Gliatech

Curated by PDSP Ki Database
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  10.2nMMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  14nMAssay Description:Antagonist potency against human H3 receptor in GTPgamma[S]-AssayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  14nMAssay Description:Antagonist potency against human histamine H3 receptor expressed in CHO cells was determined by GTPgamma-S-assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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