Compile Data Set for Download or QSAR
Report error Found 3519 Enz. Inhib. hit(s) with Target = 'Histamine H1 receptor'
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50341447(4-[(4-Chlorophenyl)methyl]-2-({(2R)-1-[4-(4-{[3-(h...)
Affinity DataKd:  0.794nMAssay Description:Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular cal...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/3/2011
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50418269(CHEMBL1767165)
Affinity DataKd:  1.26nMAssay Description:Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular cal...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/3/2011
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50418270(CHEMBL1767166)
Affinity DataKd:  3.98nMAssay Description:Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular cal...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/3/2011
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50341448(4-(4-Chloro-benzyl)-2-(1-methyl-azepan-4-yl)-2H-ph...)
Affinity DataKd:  0.200nMAssay Description:Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular cal...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/3/2011
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50418271(CHEMBL1767167)
Affinity DataKd:  1.26nMAssay Description:Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular cal...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/3/2011
Entry Details Article
PubMed
TargetHistamine H1 receptor(Guinea pig)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM50343841(3-(1H-Imidazol-4-yl)propyl2-cyclohexylethylcarbama...)
Affinity DataKd:  1.10E+5nMAssay Description:Antagonist activity at histamine H1 receptor in guinea-pig ileumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2011
Entry Details Article
PubMed
TargetHistamine H1 receptor(Guinea pig)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM50343845((Z)-3-(1H-Imidazol-4-yl)propylpent-2-enylcarbamate...)
Affinity DataKd:  7.94E+4nMAssay Description:Antagonist activity at histamine H1 receptor in guinea-pig ileumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2011
Entry Details Article
PubMed
TargetHistamine H1 receptor(Guinea pig)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM50343848((E/Z)-3-(1H-Imidazol-4-yl)propylbut-2-enylcarbamat...)
Affinity DataKd:  6.92E+4nMAssay Description:Antagonist activity at histamine H1 receptor in guinea-pig ileumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2011
Entry Details Article
PubMed
TargetHistamine H1 receptor(Guinea pig)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM50343847(3-(1H-Imidazol-4-yl)propyl2-cyclohexylpropylcarbam...)
Affinity DataKd:  1.07E+4nMAssay Description:Antagonist activity at histamine H1 receptor in guinea-pig ileumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2011
Entry Details Article
PubMed
TargetHistamine H1 receptor(Guinea pig)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM50343849(3-(1H-Imidazol-4-yl)propylbut-3-enylcarbamate hydr...)
Affinity DataKd: >1.00E+5nMAssay Description:Antagonist activity at histamine H1 receptor in guinea-pig ileumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2011
Entry Details Article
PubMed
TargetHistamine H1 receptor(Guinea pig)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM50343846(3-(1H-Imidazol-4-yl)propyl2-cyclohexylbutylcarbama...)
Affinity DataKd: >3.02E+3nMAssay Description:Antagonist activity at histamine H1 receptor in guinea-pig ileumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2011
Entry Details Article
PubMed
TargetHistamine H1 receptor(Guinea pig)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM50343843(3-(1H-Imidazol-4-yl)propyl2-cyclohexenylethylcarba...)
Affinity DataKd:  4.68E+4nMAssay Description:Antagonist activity at histamine H1 receptor in guinea-pig ileumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2011
Entry Details Article
PubMed
TargetHistamine H1 receptor(Guinea pig)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM50031686(6-[3-(4-Benzhydrylidene-piperidin-1-yl)-propoxy]-4...)
Affinity DataKd:  6nMAssay Description:Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H1 receptor(Guinea pig)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM50017376(1-(4-tert-butylphenyl)-4-(4-(hydroxydiphenylmethyl...)
Affinity DataKd:  35nMAssay Description:Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H1 receptor(Guinea pig)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM50031679(7-[3-(4-Benzhydrylidene-piperidin-1-yl)-propoxy]-2...)
Affinity DataKd:  5.90nMAssay Description:dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50127603(C-[2-(1H-Imidazol-4-yl)-cyclopropyl]-methylamine |...)
Affinity DataEC50: >0.000100nMAssay Description:Inhibition of human Histamine H1 receptor using [3H]pyrilamineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50127602(C-[2-(1H-Imidazol-4-yl)-cyclopropyl]-methylamine |...)
Affinity DataEC50: >0.000100nMAssay Description:Inhibition of human Histamine H1 receptor using [3H]pyrilamineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50127609(C-[2-(1H-Imidazol-4-yl)-cyclopropyl]-methylamine |...)
Affinity DataEC50: >0.000100nMAssay Description:Inhibition of human Histamine H1 receptor using [3H]pyrilamineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50127608(2-[2-(1H-Imidazol-4-yl)-cyclopropyl]-ethylamine | ...)
Affinity DataEC50: >0.000100nMAssay Description:Inhibition of human Histamine H1 receptor using [3H]pyrilamineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50127610((1S,2S)-2-(2-aminoethyl)-1-(1H-imidazol-4-yl)cyclo...)
Affinity DataEC50: >0.000100nMAssay Description:Inhibition of human Histamine H1 receptor using [3H]pyrilamineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50127606(2-(1H-Imidazol-4-yl)-cyclopropylamine | CHEMBL2940...)
Affinity DataEC50: >0.000100nMAssay Description:Inhibition of human Histamine H1 receptor using [3H]pyrilamineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50127607(VUF-5296 | 2-(1H-Imidazol-4-yl)-cyclopropylamine |...)
Affinity DataEC50: >0.000100nMAssay Description:Inhibition of human Histamine H1 receptor using [3H]pyrilamineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50127601(2-(1H-Imidazol-4-yl)-cyclopropylamine | CHEMBL5938...)
Affinity DataEC50: >0.000100nMAssay Description:Inhibition of human Histamine H1 receptor using [3H]pyrilamineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50127604(C-[2-(1H-Imidazol-4-yl)-cyclopropyl]-methylamine |...)
Affinity DataEC50: >0.000100nMAssay Description:Inhibition of human Histamine H1 receptor using [3H]pyrilamineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50413500(UR-PI287 | CHEMBL471724)
Affinity DataEC50:  2.57E+3nMAssay Description:Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation coun...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/21/2013
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50413508(CHEMBL474448)
Affinity DataEC50:  1.70E+3nMAssay Description:Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation coun...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/21/2013
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50413499(UR-PI295 | CHEMBL465170)
Affinity DataEC50:  2.19E+3nMAssay Description:Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation coun...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/21/2013
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50413498(UR-PI294 | CHEMBL475621)
Affinity DataEC50:  3.47E+3nMAssay Description:Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation coun...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/21/2013
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50413497(UR-PI288 | CHEMBL443896)
Affinity DataEC50:  1.29E+4nMAssay Description:Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation coun...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/21/2013
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM7966([3H]histamine | 2-(1H-imidazol-4-yl)ethan-1-amine ...)
Affinity DataEC50:  191nMAssay Description:Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation coun...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/21/2013
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM7966([3H]histamine | 2-(1H-imidazol-4-yl)ethan-1-amine ...)
Affinity DataEC50:  13nMAssay Description:Inhibition of human Histamine H1 receptor using [3H]pyrilamineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50127605(VUF-5297 | (1S,2S)-2-(1H-Imidazol-4-yl)-cyclopropy...)
Affinity DataEC50:  864nMAssay Description:Inhibition of human Histamine H1 receptor using [3H]pyrilamineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50194208((1S,2R)-trans-2-[2-(4-chlorobenzylamino)ethyl]-1-(...)
Affinity DataEC50: >1.00E+4nMAssay Description:Agonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM7966([3H]histamine | 2-(1H-imidazol-4-yl)ethan-1-amine ...)
Affinity DataEC50:  45nMAssay Description:Agonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50194202((1S,2R)-trans-2-[2-(cyclohexylmethylamino)ethyl]-1...)
Affinity DataEC50: >1.00E+4nMAssay Description:Agonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50194205((1R,2S)-trans-2-[2-(4-chlorobenzylamino)ethyl]-1-(...)
Affinity DataEC50: >1.00E+4nMAssay Description:Agonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50261729(6-chloro-3-(4-(3-(2-chloro-4-fluorophenyl)-1,2,4-o...)
Affinity DataEC50: >5.00E+4nMAssay Description:Agonist activity at histamine H1 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50121205(CHEBI:18295 | Histamine)
Affinity DataEC50:  190nMAssay Description:Agonist activity at human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 or RGS9 assessed as increase in 32Pi level incubate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/31/2017
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50319285(5-fluoro-4-methyl-2-(2-methyl-4-(3-((4aR,7aR)-tetr...)
Affinity DataEC50: >1.00E+4nMAssay Description:Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in human SK-N-MC cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2010
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50319300(N-(2-(1H-imidazol-4-yl)ethyl)-3-(4-(5-fluoro-4-met...)
Affinity DataEC50: >1.00E+4nMAssay Description:Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in human SK-N-MC cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2010
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50319302(5-(3-(4-(5-fluoro-4-methyl-1H-benzo[d]imidazol-2-y...)
Affinity DataEC50: >1.00E+4nMAssay Description:Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in human SK-N-MC cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2010
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50175517((R)-2-Benzyloxycarbonylamino-3-[4-(10,11-dihydro-5...)
Affinity DataKd:  410nMAssay Description:Dissociation constant against histamine H1 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2012
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50017721(5-(1-methylpiperidylidene-4)-5H-dibenzo(a,d)cyclop...)
Affinity DataKd:  5.40E+3nMAssay Description:Dissociation constant against histamine H1 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2012
Entry Details Article
PubMed
TargetHistamine H1 receptor(Guinea pig)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM22879((1R)-1-(4-tert-butylphenyl)-4-[4-(hydroxydiphenylm...)
Affinity DataKd:  380nMAssay Description:Inhibition of specific binding of [3H]mepyramine to Histamine 1 receptors in guinea-pigMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/22/2013
Entry Details Article

TargetHistamine H1 receptor(Guinea pig)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM50421337(CHEMBL432527)
Affinity DataKd:  214nMAssay Description:Inhibition of specific binding of [3H]mepyramine to Histamine 1 receptors in guinea-pigMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/22/2013
Entry Details Article

TargetHistamine H1 receptor(Guinea pig)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM50017376(1-(4-tert-butylphenyl)-4-(4-(hydroxydiphenylmethyl...)
Affinity DataKd:  302nMAssay Description:Inhibition of specific binding of [3H]mepyramine to Histamine 1 receptors in guinea-pigMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/22/2013
Entry Details Article

TargetHistamine H1 receptor(Guinea pig)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM50419324(CHEMBL1910384)
Affinity DataKd:  8.51nMAssay Description:Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetHistamine H1 receptor(Guinea pig)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM50419322(CHEMBL1910386)
Affinity DataKd:  3.80nMAssay Description:Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetHistamine H1 receptor(Guinea pig)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM50419323(CHEMBL1910385)
Affinity DataKd:  12.6nMAssay Description:Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetHistamine H1 receptor(Guinea pig)
Jagiellonian University Medical College

Curated by ChEMBL
LigandPNGBDBM50017674(Hydramine | Benylin | Silphen | (2-Benzhydryloxy-e...)
Affinity DataKd:  11.8nMAssay Description:Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
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