Compile Data Set for Download or QSAR
Report error Found 8631 Enz. Inhib. hit(s) with Target = 'Histamine H3 receptor'
TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50127609(C-[2-(1H-Imidazol-4-yl)-cyclopropyl]-methylamine |...)
Affinity DataEC50: >0.000100nMAssay Description:Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50127602(C-[2-(1H-Imidazol-4-yl)-cyclopropyl]-methylamine |...)
Affinity DataEC50: >0.000100nMAssay Description:Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50127606(2-(1H-Imidazol-4-yl)-cyclopropylamine | CHEMBL2940...)
Affinity DataEC50: >0.000100nMAssay Description:Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50127603(C-[2-(1H-Imidazol-4-yl)-cyclopropyl]-methylamine |...)
Affinity DataEC50: >0.000100nMAssay Description:Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rhesus macaque)
Sanofi

US Patent
LigandPNGBDBM108297(US8604046, 77)
Affinity DataKi:  0.00800nMAssay Description:The compounds of this invention have been demonstrated to displace [3H]- methylhistamine radioligand binding to mammalian cell membranes expressing r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/5/2014
Entry Details
US Patent

TargetHistamine H3 receptor(Rat)
Abbvie

US Patent
LigandPNGBDBM50434335(CHEMBL2386729 | US9181275, 3)
Affinity DataKi:  0.0200nM ΔG°:  -61.1kJ/moleT: 2°CAssay Description:To determine the effectiveness of representative compounds of this invention as histamine-3 receptor ligands (H3 receptor ligands), the following tes...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/29/2016
Entry Details
US Patent

TargetHistamine H3 receptor(Rat)
Abbvie

US Patent
LigandPNGBDBM50434335(CHEMBL2386729 | US9181275, 3)
Affinity DataKi:  0.0200nMAssay Description:Binding affinity to histamine H3 receptor in rat cortical membranesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rat)
Abbvie

US Patent
LigandPNGBDBM50434337(CHEMBL2386727 | US9181275, 1)
Affinity DataKi:  0.0300nMAssay Description:Binding affinity to histamine H3 receptor in rat cortical membranesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rhesus macaque)
Sanofi

US Patent
LigandPNGBDBM108281(US8604046, 61)
Affinity DataKi:  0.0300nMAssay Description:The compounds of this invention have been demonstrated to displace [3H]- methylhistamine radioligand binding to mammalian cell membranes expressing r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/5/2014
Entry Details
US Patent

TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50138119(CHEMBL3753475)
Affinity DataKi:  0.0300nMAssay Description:Binding affinity to recombinant human H3 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/30/2017
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50246381(2-(4-(1-cyclobutylpiperidin-4-yloxy)phenyl)-3,8-di...)
Affinity DataKi:  0.0313nMAssay Description:Displacement of [125I]Iodoproxyfan from human recombinant histamine H3 receptor by Competitive binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rat)
Abbvie

US Patent
LigandPNGBDBM50434337(CHEMBL2386727 | US9181275, 1)
Affinity DataKi:  0.0320nM ΔG°:  -59.9kJ/moleT: 2°CAssay Description:To determine the effectiveness of representative compounds of this invention as histamine-3 receptor ligands (H3 receptor ligands), the following tes...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/29/2016
Entry Details
US Patent

TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50150945(CHEBI:81390 | Immepip)
Affinity DataEC50:  0.0398nMAssay Description:Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/28/2020
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rhesus macaque)
Sanofi

US Patent
LigandPNGBDBM108294(US8604046, 74)
Affinity DataKi:  0.0400nMAssay Description:The compounds of this invention have been demonstrated to displace [3H]- methylhistamine radioligand binding to mammalian cell membranes expressing r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/5/2014
Entry Details
US Patent

TargetHistamine H3 receptor(Rhesus macaque)
Sanofi

US Patent
LigandPNGBDBM108315(US8604046, 95)
Affinity DataKi:  0.0400nMAssay Description:The compounds of this invention have been demonstrated to displace [3H]- methylhistamine radioligand binding to mammalian cell membranes expressing r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/5/2014
Entry Details
US Patent

TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50277100(4-(3-Piperidin-1-yl-propoxy)-benzoic acid 2-{4-[3-...)
Affinity DataKi:  0.0420nMAssay Description:Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressed in CHO/HEK293 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/22/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50492784(CHEMBL2413837)
Affinity DataKi:  0.0450nMAssay Description:Displacement of [125I]iodoproxyfan from histamine H3 receptor (unknown origin) expressed in CHO cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2020
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rat)
Abbvie

US Patent
LigandPNGBDBM50374104(CHEMBL255962)
Affinity DataKi:  0.0500nMAssay Description:Displacement of N-[3H]methylhistamine from histamine H3 receptor in rat cortexMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rat)
Abbvie

US Patent
LigandPNGBDBM50434336(CHEMBL2386728 | US9181275, 2)
Affinity DataKi:  0.0500nM ΔG°:  -58.8kJ/moleT: 2°CAssay Description:To determine the effectiveness of representative compounds of this invention as histamine-3 receptor ligands (H3 receptor ligands), the following tes...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/29/2016
Entry Details
US Patent

TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50319536((R)-2-(4-methylpiperidin-1-yl)-6-(2-(2-methylpyrro...)
Affinity DataKi:  0.0500nMAssay Description:Displacement of [3H]N-alpha-methylhistamine from human cloned histamine H3 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2010
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rat)
Abbvie

US Patent
LigandPNGBDBM50434336(CHEMBL2386728 | US9181275, 2)
Affinity DataKi:  0.0500nMAssay Description:Binding affinity to histamine H3 receptor in rat cortical membranesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50319536((R)-2-(4-methylpiperidin-1-yl)-6-(2-(2-methylpyrro...)
Affinity DataKi:  0.0500nMAssay Description:Displacement of [125I]Iodoproxyfan from human recombinant histamine H3 receptor by Competitive binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rat)
Abbvie

US Patent
LigandPNGBDBM50374100(CHEMBL270011)
Affinity DataKi:  0.0500nMAssay Description:Displacement of N-[3H]methylhistamine from histamine H3 receptor in rat cortexMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50174619({2-[2-((R)-2-Methyl-pyrrolidin-1-yl)-ethyl]-benzof...)
Affinity DataKi:  0.0500nMAssay Description:In vitro binding affinity for human histamine H3 receptor using [3H]N-alpha-methylhistamineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50472544(Iodoproxyfan)
Affinity DataEC50:  0.0501nMAssay Description:Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/28/2020
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50492781(CHEMBL2413835)
Affinity DataKi:  0.0570nMAssay Description:Displacement of [125I]iodoproxyfan from histamine H3 receptor (unknown origin) expressed in CHO cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2020
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rhesus macaque)
Sanofi

US Patent
LigandPNGBDBM108295(US8604046, 75)
Affinity DataKi:  0.0600nMAssay Description:The compounds of this invention have been demonstrated to displace [3H]- methylhistamine radioligand binding to mammalian cell membranes expressing r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/5/2014
Entry Details
US Patent

TargetHistamine H3 receptor(Rhesus macaque)
Sanofi

US Patent
LigandPNGBDBM108284(US8604046, 64)
Affinity DataKi:  0.0600nMAssay Description:The compounds of this invention have been demonstrated to displace [3H]- methylhistamine radioligand binding to mammalian cell membranes expressing r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/5/2014
Entry Details
US Patent

TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50159110(1-(3-(4-(piperidin-1-ylmethyl)phenoxy)propyl)piper...)
Affinity DataKi:  0.0603nMAssay Description:Binding affinity in Nluc-hH3R assessed in HEK293 cells by NanoBRET binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50246382(8-chloro-2-(4-(1-cyclobutylpiperidin-4-yloxy)pheny...)
Affinity DataKi:  0.0625nMAssay Description:Displacement of [125I]Iodoproxyfan from human recombinant histamine H3 receptor by Competitive binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50278495(4-chloro-1-(4-(3-(piperidin-1-yl)propoxy)benzyl)pi...)
Affinity DataKi:  0.0680nMAssay Description:Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressed in HEL293 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50246290(2-(4-(1-cyclobutylpiperidin-4-yloxy)phenyl)-3-meth...)
Affinity DataKi:  0.0688nMAssay Description:Displacement of [125I]Iodoproxyfan from human recombinant histamine H3 receptor by Competitive binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rhesus macaque)
Sanofi

US Patent
LigandPNGBDBM108282(US8604046, 62)
Affinity DataKi:  0.0700nMAssay Description:The compounds of this invention have been demonstrated to displace [3H]- methylhistamine radioligand binding to mammalian cell membranes expressing r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/5/2014
Entry Details
US Patent

TargetHistamine H3 receptor(Rat)
Abbvie

US Patent
LigandPNGBDBM50232355((3aR,6aR)-2-(cyclopropylmethyl)-6-(4-(2-(pyrrolidi...)
Affinity DataKi:  0.0700nMAssay Description:Displacement of N-[3H]methylhistamine from histamine H3 receptor in rat cortexMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rat)
Abbvie

US Patent
LigandPNGBDBM50232355((3aR,6aR)-2-(cyclopropylmethyl)-6-(4-(2-(pyrrolidi...)
Affinity DataKi:  0.0700nMAssay Description:Displacement of N-[3H]methylhistamine from histamine H3 receptor in rat cortex membraneMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50246434(2-(4-(1-cyclobutylpiperidin-4-yloxy)phenyl)-8-fluo...)
Affinity DataKi:  0.0781nMAssay Description:Displacement of [125I]Iodoproxyfan from human recombinant histamine H3 receptor by Competitive binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50174627({2-[2-((R)-2-Methyl-pyrrolidin-1-yl)-ethyl]-benzof...)
Affinity DataKi:  0.0800nMAssay Description:In vitro binding affinity for human histamine H3 receptor using [3H]N-alpha-methylhistamineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50405121(CHEMBL1490875 | CHEBI:64151)
Affinity DataEC50:  0.0800nMAssay Description:Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rat)
Abbvie

US Patent
LigandPNGBDBM50319536((R)-2-(4-methylpiperidin-1-yl)-6-(2-(2-methylpyrro...)
Affinity DataKi:  0.0800nMAssay Description:Displacement of [3H]N-alpha-methylhistamine from rat cloned histamine H3 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2010
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rat)
Abbvie

US Patent
LigandPNGBDBM50074627(4-[2-(5,5-Dimethyl-hex-1-ynyl)-cyclopropyl]-1H-imi...)
Affinity DataKi:  0.0800nMAssay 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 Depth
Date in BDB:
12/3/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50405121(CHEMBL1490875 | CHEBI:64151)
Affinity DataEC50:  0.0800nMAssay Description:Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rhesus macaque)
Sanofi

US Patent
LigandPNGBDBM108310(US8604046, 90)
Affinity DataKi:  0.0800nMAssay Description:The compounds of this invention have been demonstrated to displace [3H]- methylhistamine radioligand binding to mammalian cell membranes expressing r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/5/2014
Entry Details
US Patent

TargetHistamine H3 receptor(Rat)
Abbvie

US Patent
LigandPNGBDBM50374110(CHEMBL401954)
Affinity DataKi:  0.0800nMAssay Description:Displacement of N-[3H]methylhistamine from histamine H3 receptor in rat cortexMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50158590(1-(3-{2-[2-((R)-2-Methyl-pyrrolidin-1-yl)-ethyl]-b...)
Affinity DataKi:  0.0800nMAssay Description:In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing human histamine H3 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/3/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Guinea pig)
The James Black Foundation

Curated by ChEMBL
LigandPNGBDBM50215536(CHEBI:73337 | (R)-Alpha-Methylhistamine | CHEMBL26...)
Affinity DataKi:  0.0851nMAssay Description:Binding affinity towards histamine H3 receptor using [3H](R)-alpha-methylhistamine as radioligand in guinea pig cortical homogenatesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/16/2018
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50110291((7-Chloro-quinolin-4-yl)-[4-(3-piperidin-1-yl-prop...)
Affinity DataKi:  0.0860nMAssay Description:Affinity for displacement of [125I]iodoproxyfan from human histamine H3 receptors stably expressed in CHO cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H3 receptor(Rhesus macaque)
Sanofi

US Patent
LigandPNGBDBM108328(US8604046, 108)
Affinity DataKi:  0.0900nMAssay Description:The compounds of this invention have been demonstrated to displace [3H]- methylhistamine radioligand binding to mammalian cell membranes expressing r...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/5/2014
Entry Details
US Patent

TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50158588((3,5-Difluoro-phenyl)-{2-[2-((R)-2-methyl-pyrrolid...)
Affinity DataKi:  0.0900nMAssay Description:In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing human histamine H3 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/3/2012
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50110288([4-(3-Piperidin-1-yl-propoxy)-phenyl]-quinolin-4-y...)
Affinity DataKi:  0.0910nMAssay Description:Affinity for displacement of [125I]iodoproxyfan from human histamine H3 receptors stably expressed in CHO cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50278350(CHEMBL513193 | CHEMBL2203701 | 4-fluoro-1-(4-(3-(p...)
Affinity DataKi:  0.0933nMAssay Description:Displacement of [3H]N-alpha-methylhistamine from recombinant human histamine H3 receptor expressed in HEK293 cells after 90 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2015
Entry Details Article
PubMed
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