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Found 1087 with Last Name = 'kraus' and Initial = 'm'
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM50246967(CHEMBL4080228 | US10570121, Example 81)
Affinity DataKi: <0.100nMAssay Description:Binding affinity to EZH2 (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  0.300nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Freie UniversitäT Berlin

Curated by ChEMBL
LigandPNGBDBM27213(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)
Affinity DataKi:  0.490nMAssay Description:In vitro binding affinity against rat histamine H3 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Freie UniversitäT Berlin

Curated by ChEMBL
LigandPNGBDBM27213(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)
Affinity DataKi:  0.490nMAssay 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 DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361648(CHEMBL1940246)
Affinity DataKi:  0.600nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361649(CHEMBL1938415)
Affinity DataKi:  0.600nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Freie UniversitäT Berlin

Curated by ChEMBL
LigandPNGBDBM22541(Clobenpropit | N''-[(4-chlorophenyl)methyl]{[3-(1H...)
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 DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Freie UniversitäT Berlin

Curated by ChEMBL
LigandPNGBDBM22541(Clobenpropit | N''-[(4-chlorophenyl)methyl]{[3-(1H...)
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 DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361642(CHEMBL1940251)
Affinity DataKi:  0.700nMAssay Description:Inhibition of recombinant human His-tagged PDK1 catalytic domain using Ac-Sox-PKTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIAD-NH2 as substrate by fluorescence...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Freie UniversitäT Berlin

Curated by ChEMBL
LigandPNGBDBM50092853(1-{4-[3-(1H-Imidazol-4-yl)-propoxy]-phenyl}-propan...)
Affinity DataKi:  0.740nMAssay 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 DepthDetails ArticlePubMed
TargetHistamine H3 receptor(GUINEA PIG)
TBA

Curated by ChEMBL
LigandPNGBDBM50283867(CHEMBL98165 | N-Cyclohexylmethyl-N'-[3-(1H-imidazo...)
Affinity DataKi:  0.740nMAssay Description:Antagonistic activity for Histamine H3 receptor binding in guinea pigMore data for this Ligand-Target Pair
In DepthDetails Article
TargetHistamine H3 receptor(GUINEA PIG)
TBA

Curated by ChEMBL
LigandPNGBDBM50283867(CHEMBL98165 | N-Cyclohexylmethyl-N'-[3-(1H-imidazo...)
Affinity DataKi:  0.794nMAssay 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(Rattus norvegicus (rat))
Freie UniversitäT Berlin

Curated by ChEMBL
LigandPNGBDBM50091386(1-{4-[3-(1H-Imidazol-4-yl)-propoxy]-phenyl}-ethano...)
Affinity DataKi:  0.800nMAssay 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 DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Freie UniversitäT Berlin

Curated by ChEMBL
LigandPNGBDBM50092841(CHEMBL128690 | Cyclobutyl-{4-[3-(1H-imidazol-4-yl)...)
Affinity DataKi:  0.890nMAssay 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 DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361641(CHEMBL1940247)
Affinity DataKi:  0.900nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM50193709(CHEMBL3911017)
Affinity DataKi:  1nMAssay Description:Inhibition of wild type EZH2 (unknown origin)More data for this Ligand-Target Pair
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361652(CHEMBL1940250)
Affinity DataKi:  1nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Freie UniversitäT Berlin

Curated by ChEMBL
LigandPNGBDBM50092846(1-{2-Fluoro-4-[3-(1H-imidazol-4-yl)-propoxy]-pheny...)
Affinity DataKi:  1.10nMAssay 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 DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Freie UniversitäT Berlin

Curated by ChEMBL
LigandPNGBDBM50092848(1-{4-[3-(1H-Imidazol-4-yl)-propoxy]-2-methyl-pheny...)
Affinity DataKi:  1.20nMAssay 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 DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361650(CHEMBL1940248)
Affinity DataKi:  1.30nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361643(CHEMBL1940252)
Affinity DataKi:  1.40nMAssay Description:Inhibition of recombinant human His-tagged PDK1 catalytic domain using Ac-Sox-PKTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIAD-NH2 as substrate by fluorescence...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361644(CHEMBL1940253)
Affinity DataKi:  1.40nMAssay Description:Inhibition of recombinant human His-tagged PDK1 catalytic domain using Ac-Sox-PKTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIAD-NH2 as substrate by fluorescence...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(GUINEA PIG)
TBA

Curated by ChEMBL
LigandPNGBDBM50283869(CHEMBL99830 | N-[3-(1H-Imidazol-4-yl)-propyl]-N'-(...)
Affinity DataKi:  1.58nMAssay 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(GUINEA PIG)
TBA

Curated by ChEMBL
LigandPNGBDBM50283869(CHEMBL99830 | N-[3-(1H-Imidazol-4-yl)-propyl]-N'-(...)
Affinity DataKi:  1.60nMAssay Description:Antagonistic activity for Histamine H3 receptor binding in guinea pigMore data for this Ligand-Target Pair
In DepthDetails Article
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Freie UniversitäT Berlin

Curated by ChEMBL
LigandPNGBDBM50092845(1-{4-[3-(1H-Imidazol-4-yl)-propoxy]-phenyl}-butan-...)
Affinity DataKi:  1.90nMAssay 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 DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361653(CHEMBL1940245)
Affinity DataKi:  2nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM50562994(CHEMBL4740532)
Affinity DataKi:  2nMAssay Description:Inhibition of wild type EZH2 (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Freie UniversitäT Berlin

Curated by ChEMBL
LigandPNGBDBM50092844(4-[3-(4-Methoxy-phenoxy)-propyl]-1H-imidazole; com...)
Affinity DataKi:  2.20nMAssay 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 DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Freie UniversitäT Berlin

Curated by ChEMBL
LigandPNGBDBM50067472(4-[3-(4-Ethynyl-phenoxy)-propyl]-1H-imidazole | 4-...)
Affinity DataKi:  2.30nMAssay 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 DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Freie UniversitäT Berlin

Curated by ChEMBL
LigandPNGBDBM50067472(4-[3-(4-Ethynyl-phenoxy)-propyl]-1H-imidazole | 4-...)
Affinity DataKi:  2.30nMAssay 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 DepthDetails ArticlePubMed
TargetSubstance-K receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50277511(3-[(3aR,4R,5S,7aS)-5-{(1R)-1-[3,5-Bis(trifluoromet...)
Affinity DataKi:  2.40nMAssay Description:Binding affinity to human NK2 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeuromedin-K receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50277511(3-[(3aR,4R,5S,7aS)-5-{(1R)-1-[3,5-Bis(trifluoromet...)
Affinity DataKi:  2.40nMAssay Description:Binding affinity to human NK3 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Freie UniversitäT Berlin

Curated by ChEMBL
LigandPNGBDBM50092843(1-{4-[3-(1H-Imidazol-4-yl)-propoxy]-phenyl}-hexan-...)
Affinity DataKi:  2.5nMAssay 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 DepthDetails ArticlePubMed
Target3-phosphoinositide-dependent protein kinase 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361651(CHEMBL1940249)
Affinity DataKi:  2.5nMAssay Description:Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Freie UniversitäT Berlin

Curated by ChEMBL
LigandPNGBDBM50092838(1-{4-[3-(1H-Imidazol-4-yl)-propoxy]-phenyl}-pentan...)
Affinity DataKi:  2.60nMAssay 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 DepthDetails ArticlePubMed
TargetNeuronal acetylcholine receptor subunit alpha-7(Rattus norvegicus (Rat))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50377050(CHEMBL403858 | PH-709829)
Affinity DataKi:  2.90nMAssay Description:Displacement of [3H]MLA from alpha-7 nACh receptor in rat brainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM50193709(CHEMBL3911017)
Affinity DataKi:  3nMAssay Description:Inhibition of wild type EZH2 Y641N mutant (unknown origin)More data for this Ligand-Target Pair
TargetHistamine H3 receptor(GUINEA PIG)
TBA

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(Rattus norvegicus (rat))
Freie UniversitäT Berlin

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  4nMAssay 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 DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Freie UniversitäT Berlin

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  4nMAssay Description:In vitro binding affinity against rat histamine H3 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Freie UniversitäT Berlin

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataKi:  4nMAssay 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 DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Freie UniversitäT Berlin

Curated by ChEMBL
LigandPNGBDBM50092856(1-{4-[3-(1H-Imidazol-4-yl)-propoxy]-3-methyl-pheny...)
Affinity DataKi:  4.80nMAssay 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 DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Freie UniversitäT Berlin

Curated by ChEMBL
LigandPNGBDBM50092850(1-{4-[3-(1H-Imidazol-4-yl)-propoxy]-phenyl}-2-meth...)
Affinity DataKi:  4.80nMAssay 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 DepthDetails ArticlePubMed
TargetHistamine H3 receptor(GUINEA PIG)
TBA

Curated by ChEMBL
LigandPNGBDBM50283874(CHEMBL317325 | N-Cyclohexyl-N'-[4-(1H-imidazol-4-y...)
Affinity DataKi:  5nMAssay Description:Antagonistic activity for Histamine H3 receptor binding in guinea pigMore data for this Ligand-Target Pair
In DepthDetails Article
TargetHistamine H3 receptor(GUINEA PIG)
TBA

Curated by ChEMBL
LigandPNGBDBM50283874(CHEMBL317325 | N-Cyclohexyl-N'-[4-(1H-imidazol-4-y...)
Affinity DataKi:  5.01nMAssay 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(Rattus norvegicus (rat))
Freie UniversitäT Berlin

Curated by ChEMBL
LigandPNGBDBM50092834(1-{4-[3-(1H-Imidazol-4-yl)-propoxy]-phenyl}-2-phen...)
Affinity DataKi:  5.90nMAssay 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 DepthDetails ArticlePubMed
TargetNeuronal acetylcholine receptor subunit alpha-7(Rattus norvegicus (Rat))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50377049(CHEMBL258031)
Affinity DataKi:  6.20nMAssay Description:Displacement of [3H]MLA from alpha-7 nACh receptor in rat brainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(GUINEA PIG)
TBA

Curated by ChEMBL
LigandPNGBDBM50283871(CHEMBL329275 | N-(tert-Butoxy-carbonyl)-N'-cyclohe...)
Affinity DataKi:  6.31nMAssay Description:Antagonistic activity for Histamine H3 receptor on electrically evoked guinea-pig ileum contractionMore data for this Ligand-Target Pair
In DepthDetails Article
TargetNitric oxide synthase, brain(Rattus norvegicus (rat))
University Of California

Curated by ChEMBL
LigandPNGBDBM50328814((+/-)-6-((4-(2-(3-fluorophenethylamino)ethoxy)pyrr...)
Affinity DataKi:  7nMAssay Description:Inhibition of rat nNOS expressed in Escherichia coli using L-arginine as substrate assessed as formation of nitric oxide by hemoglobin capture assayMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-7(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50190786((R)-N-(quinuclidin-3-yl)furo[2,3-c]pyridine-5-carb...)
Affinity DataKi:  7nMAssay Description:Displacement of [3H]MLA from alpha-7 nACh receptor in human IMR32 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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