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  169 KI  15 IC50  1 Kd  12 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 197 hits for monomerid = 22914   

TargetHistamine H4 receptor(Human)
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataEC50:  79.4nMAssay Description:Inverse agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by l...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H3 receptor(Human)
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataEC50:  39.8nMAssay Description:Inverse agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by l...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H3 receptor(Human)
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataEC50:  98nMAssay Description:Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding b...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H4 receptor(Human)
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataEC50:  110nMAssay Description:Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[3...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H3 receptor(Human)
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataIC50: 16nMAssay Description:Antagonist activity at human H3 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H4 receptor(Human)
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataIC50: 680nMAssay Description:Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H4 receptor(Human)
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataEC50:  417nMAssay Description:Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H3 receptor(Mouse)
Tsukuba Research Institute

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataEC50:  11nMAssay Description:Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCytochrome P450 3A4(Human)
Jadavpur University

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataIC50: 6.10E+3nMAssay Description:Inhibition of CYP3A4More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H4 receptor(Human)
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataIC50: 667nMAssay Description:Antagonist activity at histamine H4 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H3 receptor(Human)
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataIC50: 518nMAssay Description:Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H4 receptor(Human)
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataIC50: 977nMAssay Description:Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H3 receptor(Guinea pig)
De Novo Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKd:  1.26nMAssay Description:Displacement of [3H]Nalpha-methylhistamine from histamine H3 receptors in homogenates of rat cerebral cortexMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H3 receptor(Human)
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataEC50:  97.7nMAssay Description:Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-sta...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H4 receptor(Human)
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataEC50:  110nMAssay Description:Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H3 receptor(Human)
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataIC50: 120nMAssay Description:Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 h...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H3 receptor(Human)
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataIC50: 140nMAssay Description:Inverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H4 receptor(Human)
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataIC50: 19nMAssay Description:Antagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calciu...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H3 receptor(Human)
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataIC50: 1.03E+3nMAssay Description:Inhibition of human H3R expressed in methylhistamine-induced human H3-bla U2OS cells incubated for 30 mins by beta-lactamase complementation technolo...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H3 receptor(Human)
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataIC50: 20nMAssay Description:Inverse agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells assessed as reduction in histamine-induced inhibition of forsko...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H4 receptor(Human)
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataEC50:  120nMAssay Description:Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H4 receptor(Human)
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataIC50: 490nMAssay Description:Inverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H4 receptor(Mouse)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataEC50:  302nMAssay Description:Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H4 receptor(Mouse)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataEC50:  28nMAssay Description:Antagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCholesterol 24-hydroxylase(Human)
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataIC50: 430nMAssay Description:Inhibition of CH24H expressing human 293-F cells for 15 minutes using [14C] cholesterol as substrate and measured after 5 hrs by trypan blue staining...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H3 receptor(Human)
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataIC50: 140nMAssay Description:Histamine-3 membranes were prepared from recombinant CHO-k1 cells expressing human histamine-3 receptor or rat histamine-3 receptor. Radioligand (RS)...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetHistamine H3 receptor(Human)
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataIC50: 296nMAssay Description:Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of imetit-stimulation ERK1/2 phosphorylation by E...More data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetHistamine H3 receptor(Human)
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataEC50:  34nMAssay Description:Inverse agonist activity at recombinant human histamine H3 receptor expressed in CHO-K1 cells preincubated for 10 mins followed by [35S]GTPgammaS add...More data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetHistamine H3 receptor(Rat)
Gliatech

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  1.5nMAssay Description:Antagonistic activity was evaluated against histamine H3 receptor using [3H]- N-alpha-methylhistamine as radioligand in experiment 2More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
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 Article
PubMed
TargetHistamine H3 receptor(Guinea pig)
De Novo Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
In DepthDetails Article
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(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 Article
PubMed
TargetHistamine H3 receptor(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 Article
PubMed
TargetHistamine H3 receptor(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 Article
PubMed
TargetHistamine H3 receptor(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 Article
PubMed
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 Article
PubMed
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 Article
PubMed
TargetHistamine H3 receptor(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 Article
PubMed
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 Article
PubMed
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 Article
PubMed
TargetHistamine H3 receptor(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 Article
PubMed
TargetHistamine H3 receptor(Guinea pig)
De Novo Pharmaceuticals

Curated by ChEMBL
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

TargetHistamine H3 receptor(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 Article
PubMed
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(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 on Synaptosomes of rat cerebral cortex.More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistamine H3 receptor(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 synaptosome...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
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