BDBM22541 Clobenpropit::N''-[(4-chlorophenyl)methyl]{[3-(1H-imidazol-5-yl)propyl]sulfanyl}methanimidamide::VUF 9153::VUF-9153::VUF9153

SMILES NC(SCCCc1cnc[nH]1)=NCc1ccc(Cl)cc1

InChI Key InChIKey=UCAIEVHKDLMIFL-UHFFFAOYSA-N

Data  50 KI  2 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:
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 54 hits for monomerid = 22541   

TargetHistamine H3 receptor(Guinea pig)
De Novo Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKd:  0.158nMAssay Description:Displacement of [3H]Nalpha-methylhistamine from histamine H3 receptors in homogenates of rat cerebral cortexMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/25/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Mouse)
Tsukuba Research Institute

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataEC50:  1.70nMAssay 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 Depth
Date in BDB:
8/26/2010
Entry Details Article
PubMed
TargetHistamine H3 receptor(Mouse)
Tsukuba Research Institute

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataIC50: 1nMAssay Description:Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced i...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/13/2011
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Athersys

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataIC50: 1nMAssay Description:Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced i...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/13/2011
Entry Details Article
PubMed
TargetHistamine receptor H3(Dog)
Abbott Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.0800nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/13/2012
Entry Details Article
PubMed
TargetHrh3 protein(Rat)
Glaxo Research & Development

Curated by PDSP Ki Database
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.150nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rat)
TBA

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.180nMAssay 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 Depth
Date in BDB:
9/28/2012
Entry Details Article

TargetHrh3 protein(Rat)
Glaxo Research & Development

Curated by PDSP Ki Database
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.180nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/13/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rat)
TBA

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.180nMAssay 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 Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H3 receptor(Guinea pig)
De Novo Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.220nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/13/2012
Entry Details Article
PubMed
TargetHrh3 protein(Rat)
Glaxo Research & Development

Curated by PDSP Ki Database
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.25nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Athersys

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.339nM ΔG°:  -12.9kcal/molepH: 7.4 T: 2°CAssay Description:Ligand displacement assays were performed on CHO cells membranes expressing hH3R. Retained radioactivity was determined by liquid scintillation count...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/13/2008
Entry Details Article
PubMed
TargetHrh3 protein(Rat)
Glaxo Research & Development

Curated by PDSP Ki Database
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.350nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/13/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Athersys

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.360nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/13/2012
Entry Details Article
PubMed
TargetHrh3 protein(Rat)
Glaxo Research & Development

Curated by PDSP Ki Database
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.400nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2012
Entry Details
PubMed
TargetHrh3 protein(Rat)
Glaxo Research & Development

Curated by PDSP Ki Database
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.480nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/29/2011
Entry Details
PubMed
TargetHrh3 protein(Rat)
Glaxo Research & Development

Curated by PDSP Ki Database
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.5nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2012
Entry Details
PubMed
TargetHistamine H3 receptor(Human)
Athersys

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.580nMAssay 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 Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rat)
TBA

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.600nMAssay Description:In vitro antagonistic activity against Histamine H3 receptor on Synaptosomes of rat cerebral cortex.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rat)
TBA

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.600nMAssay Description:In vitro Histamine H3 receptor antagonist activity in an assay with K+-evoked depolarization-induced release of [3H]histamine from synaptosomes of ra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rat)
TBA

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.600nMAssay 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 Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Athersys

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.600nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/25/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rat)
TBA

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.600nMAssay 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 Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rat)
TBA

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.600nMAssay Description:In vitro inhibitory activity against Histamine H3 receptor for K+ evoked depolarization-induced release of [3H]histamine from synaptosomes of rat cer...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Athersys

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.600nMAssay Description:Antagonist potency against human H3 receptor in GTPgamma-S-AssayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H3 receptor(Mouse)
Tsukuba Research Institute

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.600nMAssay 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 Depth
Date in BDB:
8/26/2010
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rat)
TBA

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.600nMAssay 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 Depth
Date in BDB:
11/24/2012
Entry Details Article
PubMed
TargetHrh3 protein(Rat)
Glaxo Research & Development

Curated by PDSP Ki Database
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.600nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/29/2011
Entry Details
PubMed
TargetHistamine H3 receptor(Rat)
TBA

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.631nMAssay 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 Depth
Date in BDB:
5/19/2013
Entry Details Article

TargetHistamine H3 receptor(Human)
Athersys

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.780nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/13/2012
Entry Details Article
PubMed
TargetHrh3 protein(Rat)
Glaxo Research & Development

Curated by PDSP Ki Database
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  0.870nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/2/2012
Entry Details
PubMed
TargetHistamine H3 receptor(Rat)
TBA

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  1.40nMAssay Description:Binding affinity to rat Histamine H3 receptor in CHO-K1 cells using [125I]iodoproxyfan as radioligandMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Athersys

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  2.40nMAssay Description:Inhibition of [125I]iodoproxyfan binding to human histamine H3 receptor of CHO-K1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Athersys

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  2.40nMAssay Description:Displacement of [3H]iodoproxyfan from human histamine H3 receptor expressed in CHO-K1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/17/2010
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Athersys

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  2.40nMAssay Description:Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressing CHO cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Athersys

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  2.40nMAssay Description:Displacement of [125I]iodoproxyfan from human full-length histamine H3 receptor expressed in HEK293 cells after 60 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2011
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Athersys

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  2.82nMAssay Description:Displacement of [3H]histamine from human H3 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Athersys

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  3nMAssay Description:Ligand displacement assays were performed on The SK-N-MC/hH3R cell homogenates. Retained radioactivity was determined by liquid scintillation countin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/28/2008
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Athersys

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  3.16nMAssay Description:Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in human SK-N-MC cells by liquid scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/21/2013
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Athersys

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  3.80nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/2/2012
Entry Details
PubMed
TargetHistamine H4 receptor(Human)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  4.30nMAssay Description:Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/17/2010
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  4.30nMAssay Description:Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2011
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  5nMAssay Description:Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/16/2012
Entry Details Article
PubMed
Target5-hydroxytryptamine receptor 3A(Rat)
Abbott Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  7.41nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/13/2012
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  8nMAssay Description:Ligand displacement assays were performed on The SK-N-MC/hH4R cell homogenates. Retained radioactivity was determined by liquid scintillation countin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/28/2008
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  10nMAssay Description:Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  10nMAssay Description:Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/21/2013
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  12.8nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/25/2012
Entry Details Article
PubMed
TargetAlpha-2C adrenergic receptor(Human)
Abbott Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  15.8nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/13/2012
Entry Details Article
PubMed
TargetAlpha-2A adrenergic receptor(Human)
Abbott Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM22541(VUF 9153 | N''-[(4-chlorophenyl)methyl]{[3-(1H-imi...)
Affinity DataKi:  17.4nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/13/2012
Entry Details Article
PubMed
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