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

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 12 hits for monomerid = 22914   

TargetHistamine H4 receptor(Homo sapiens (Human))
The R. W. Johnson Pharmaceutical Research Institute

Curated by PDSP Ki Database
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 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 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(Homo sapiens (Human))
Jagiellonian University Medical College

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 ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
The R. W. Johnson Pharmaceutical Research Institute

Curated by PDSP Ki Database
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 ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
The R. W. Johnson Pharmaceutical Research Institute

Curated by PDSP Ki Database
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 ArticlePubMed
TargetHistamine H3 receptor(Mus musculus)
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 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 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 ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
The R. W. Johnson Pharmaceutical Research Institute

Curated by PDSP Ki Database
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 ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
The R. W. Johnson Pharmaceutical Research Institute

Curated by PDSP Ki Database
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 ArticlePubMed
TargetHistamine H4 receptor(Mus musculus (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 ArticlePubMed
TargetHistamine H4 receptor(Mus musculus (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 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 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 ArticlePubMed