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TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50356884(CHEMBL1915540)
Affinity DataIC50:  0.650nMAssay Description:Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50315348((R)-8-chloro-4-(3-(methylamino)pyrrolidin-1-yl)ben...)
Affinity DataIC50:  1nMAssay Description:Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50356884(CHEMBL1915540)
Affinity DataIC50:  1.30nMAssay Description:Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50538677(CHEMBL4635634)
Affinity DataIC50:  1.70nMAssay Description:Inverse agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskol...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50315348((R)-8-chloro-4-(3-(methylamino)pyrrolidin-1-yl)ben...)
Affinity DataIC50:  3nMAssay Description:Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity ass...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50315349((S)-8-chloro-4-(3-(methylamino)pyrrolidin-1-yl)ben...)
Affinity DataIC50:  4nMAssay Description:Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity ass...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50356884(CHEMBL1915540)
Affinity DataIC50:  4.90nMAssay Description:Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataIC50:  5.30nMAssay Description:Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50415489(CHEMBL591969)
Affinity DataIC50:  10nMAssay Description:Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294419(US9586959, Compound 98)
Affinity DataIC50:  11nMpH: 7.5 T: 2°CAssay Description:In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofac...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataIC50:  13nMAssay Description:Antagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-ind...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50315349((S)-8-chloro-4-(3-(methylamino)pyrrolidin-1-yl)ben...)
Affinity DataIC50:  13nMAssay Description:Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50538677(CHEMBL4635634)
Affinity DataIC50:  15nMAssay Description:Inverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294378(US9586959, Compound 31)
Affinity DataIC50:  16nMpH: 7.5 T: 2°CAssay Description:In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofac...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50315314(8-chloro-4-(4-methylpiperazin-1-yl)benzofuro[3,2-d...)
Affinity DataIC50:  19nMAssay Description:Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataIC50:  19nMAssay Description:Antagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calciu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294427(US9586959, Compound disclosed in WO 2010030785, Ex...)
Affinity DataIC50:  22nMAssay Description:Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta sc...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294427(US9586959, Compound disclosed in WO 2010030785, Ex...)
Affinity DataIC50:  22nMpH: 7.5 T: 2°CAssay Description:In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofac...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294407(US9586959, Compound 69 | US9586959, Compound 95)
Affinity DataIC50:  27nMAssay Description:Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta sc...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294407(US9586959, Compound 69 | US9586959, Compound 95)
Affinity DataIC50:  28nMAssay Description:Antagonist activity at recombinant human histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced st...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294418(US9586959, Compound 96)
Affinity DataIC50:  28nMpH: 7.5 T: 2°CAssay Description:In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofac...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294418(US9586959, Compound 96)
Affinity DataIC50:  28nMAssay Description:Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta sc...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataIC50:  29nMAssay Description:Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta sc...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataIC50:  30nMAssay Description:Antagonist activity at H4R in human eosinophils assessed as inhibition of imetit-induced shape change by GAFS assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294373(US9586959, Compound 104 | US9586959, Compound 24 |...)
Affinity DataIC50:  30nMpH: 7.5 T: 2°CAssay Description:In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofac...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50315333((R)-N-methyl-1-(8-(trifluoromethyl)benzofuro[3,2-d...)
Affinity DataIC50:  30nMAssay Description:Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50537206(CHEMBL4483783)
Affinity DataIC50:  32nMAssay Description:Antagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-ind...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50315323((R)-1-(8-chlorobenzofuro[3,2-d]pyrimidin-4-yl)-N-m...)
Affinity DataIC50:  33nMAssay Description:Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361015(CHEMBL592379)
Affinity DataIC50:  33.1nMAssay Description:Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294386(US9586959, Compound 49)
Affinity DataIC50:  34nMpH: 7.5 T: 2°CAssay Description:In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofac...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294386(US9586959, Compound 49)
Affinity DataIC50:  34nMAssay Description:Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta sc...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294407(US9586959, Compound 69 | US9586959, Compound 95)
Affinity DataIC50:  35nMpH: 7.5 T: 2°CAssay Description:In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofac...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294373(US9586959, Compound 104 | US9586959, Compound 24 |...)
Affinity DataIC50:  36nMpH: 7.5 T: 2°CAssay Description:In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofac...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50315339(8-chloro-2-methyl-4-(4-methylpiperazin-1-yl)benzof...)
Affinity DataIC50:  37nMAssay Description:Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50315342(8-chloro-4-(4-methylpiperazin-1-yl)-2-(trifluorome...)
Affinity DataIC50:  39nMAssay Description:Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity ass...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294361(US9586959, Compound 4)
Affinity DataIC50:  40nMpH: 7.5 T: 2°CAssay Description:In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofac...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50315323((R)-1-(8-chlorobenzofuro[3,2-d]pyrimidin-4-yl)-N-m...)
Affinity DataIC50:  41nMAssay Description:Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity ass...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294414(US9586959, Compound 92)
Affinity DataIC50:  42nMpH: 7.5 T: 2°CAssay Description:In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofac...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294407(US9586959, Compound 69 | US9586959, Compound 95)
Affinity DataIC50:  44nMpH: 7.5 T: 2°CAssay Description:In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofac...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361010(CHEMBL1935572)
Affinity DataIC50:  46nMAssay Description:Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50361035(CHEMBL1935571)
Affinity DataIC50:  47nMAssay Description:Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294377(US9586959, Compound 29)
Affinity DataIC50:  49nMpH: 7.5 T: 2°CAssay Description:In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofac...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294377(US9586959, Compound 29)
Affinity DataIC50:  52nMAssay Description:Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta sc...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294415(US9586959, Compound 93)
Affinity DataIC50:  53nMAssay Description:Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta sc...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294368(US9586959, Compound 18)
Affinity DataIC50:  55nMpH: 7.5 T: 2°CAssay Description:In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofac...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294408(US9586959, Compound 74)
Affinity DataIC50:  60nMpH: 7.5 T: 2°CAssay Description:In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofac...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294416(US9586959, Compound 94)
Affinity DataIC50:  62nMpH: 7.5 T: 2°CAssay Description:In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofac...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294416(US9586959, Compound 94)
Affinity DataIC50:  62nMAssay Description:Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta sc...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294409(US9586959, Compound 75)
Affinity DataIC50:  64nMpH: 7.5 T: 2°CAssay Description:In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofac...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetHistamine H4 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM294366(US9586959, Compound 16)
Affinity DataIC50:  65nMpH: 7.5 T: 2°CAssay Description:In vitro profiling protein kinases was performed using the HotSpot assay platform. Briefly, specific kinase/substrate pairs along with required cofac...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
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