Compile Data Set for Download or QSAR
maximum 50k data

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)

Found 94 hits in this display   

TargetHistamine H4 receptor(Rattus norvegicus (rat))
Johnson & Johnson Pharmaceutical Research And Development

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  2.40nMAssay Description:Binding affinity of compound towards rat histamine H4 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Rattus norvegicus (rat))
Johnson & Johnson Pharmaceutical Research And Development

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  2.60nM ΔG°:  -49.0kJ/molepH: 7.5 T: 2°CAssay Description:The Ki values were calculated based on an experimentally determined appropriate Kd value according to Cheng and Prusoff.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Rattus norvegicus (rat))
Johnson & Johnson Pharmaceutical Research And Development

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  2.70nM ΔG°:  -48.9kJ/molepH: 7.4 T: 2°CAssay Description:Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Rattus norvegicus (rat))
Johnson & Johnson Pharmaceutical Research And Development

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  2.70nM ΔG°:  -48.9kJ/molepH: 7.4 T: 2°CAssay Description:Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  3.89nMAssay Description:Displacement of [3H]-histamine from mouse H4R expressed in HEK293T cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  4nMAssay Description:Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  4nMAssay Description:Antagonist activity at Homo sapiens (human) histamine H4 receptorMore data for this Ligand-Target Pair
In DepthDetails Article
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  4nMAssay Description:Displacement of [3H]histamine from human histamine H4 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  4nMAssay Description:Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  4nMAssay Description:Binding affinity to human histamine H4 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  4nMAssay Description:Displacement of [3H]- histamine from the recombinant human histamine H4 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  4.10nM ΔG°:  -47.9kJ/molepH: 7.5 T: 2°CAssay Description:The Ki values were calculated based on an experimentally determined appropriate Kd value according to Cheng and Prusoff.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  4.17nMAssay Description:Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  4.20nMAssay Description:Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate b...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Rattus norvegicus (rat))
Johnson & Johnson Pharmaceutical Research And Development

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  4.27nMAssay Description:Displacement of [3H]-histamine from rat H4R expressed in HEK293T cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  4.5nMAssay Description:Binding affinity to human histamine H4 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  4.60nM ΔG°:  -47.6kJ/molepH: 7.5 T: 2°CAssay Description:The Ki values were calculated based on an experimentally determined appropriate Kd value according to Cheng and Prusoff.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Rattus norvegicus (rat))
Johnson & Johnson Pharmaceutical Research And Development

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  4.70nM ΔG°:  -47.5kJ/molepH: 7.4 T: 2°CAssay Description:Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  4.90nMAssay Description:Displacement of [3H]histamine from human histamine 4 receptor expressed in HEK293T cell membranes incubated for 1 hr by radioligand binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  5nMAssay Description:Displacement of [3H]histamine from human recombinant histamine H4 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  5nMAssay Description:Displacement of [3H]histamine from human recombinant histamine H4 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  5nMAssay Description:Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  6nMAssay Description:Binding affinity to human histamine H4 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Rattus norvegicus (rat))
Johnson & Johnson Pharmaceutical Research And Development

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  6nMAssay Description:Binding affinity to rat histamine H4 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  6.30nMAssay Description:Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  6.31nMAssay Description:Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  6.80nMAssay Description:Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  6.80nMAssay Description:Antagonist activity at human histamine H4 receptor by functional assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  6.80nMAssay Description:Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamas...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  6.80nMAssay Description:Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  8nMAssay Description:Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  8nMAssay Description:Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  8nMAssay Description:Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  8nMAssay Description:Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  12nM ΔG°:  -45.2kJ/molepH: 7.4 T: 2°CAssay Description:Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  12nM ΔG°:  -45.2kJ/molepH: 7.4 T: 2°CAssay Description:Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  12nMAssay Description:Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate b...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  12nM ΔG°:  -45.2kJ/molepH: 7.4 T: 2°CAssay Description:Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  13nMAssay Description:Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  13nMAssay Description:Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  14nMAssay Description:Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  15.8nMAssay 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 DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  16nMAssay Description:Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  16nMAssay 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 DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  17nMAssay Description:Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  18.6nMAssay Description:Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  35nMAssay Description:Binding affinity to histamine 4 receptor (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  38nMAssay Description:Displacement of [3H]histamine human recombinant histamine H4 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  63nMAssay Description:Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  63nMAssay Description:Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  63nMAssay Description:Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  63nMAssay Description:Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  63nMAssay Description:Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  63nMAssay Description:Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  63nMAssay Description:Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes c...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  69nMAssay Description:Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  126nMAssay Description:Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  977nM ΔG°:  -34.3kJ/molepH: 7.4 T: 2°CAssay Description:Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H2 receptor(Cavia porcellus (domestic guinea pig))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi: >1.00E+3nM ΔG°: >-34.2kJ/molepH: 7.5 T: 2°CAssay Description:The Ki values were calculated based on an experimentally determined appropriate Kd value according to Cheng and Prusoff.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Cavia porcellus (domestic guinea pig))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi: >1.00E+3nM ΔG°: >-34.2kJ/molepH: 7.5 T: 2°CAssay Description:The Ki values were calculated based on an experimentally determined appropriate Kd value according to Cheng and Prusoff.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine receptor H4(GUINEA PIG)
Pfizer

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  1.07E+3nMAssay Description:Displacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Abbott Laboratories

LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  1.32E+3nM ΔG°:  -33.6kJ/molepH: 7.4 T: 2°CAssay Description:Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Abbott Laboratories

LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  1.45E+3nM ΔG°:  -33.3kJ/molepH: 7.4 T: 2°CAssay Description:Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  2.24E+3nM ΔG°:  -32.2kJ/molepH: 7.4 T: 2°CAssay Description:Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  2.24E+3nM ΔG°:  -32.2kJ/molepH: 7.4 T: 2°CAssay Description:Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Abbott Laboratories

LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  4.70E+3nM ΔG°:  -30.4kJ/molepH: 7.5 T: 2°CAssay Description:The Ki values were calculated based on an experimentally determined appropriate Kd value according to Cheng and Prusoff.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  5.01E+3nMAssay 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 DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  5.01E+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 DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  5.13E+3nMAssay Description:Binding affinity to histamine H3 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  5.13E+3nM ΔG°:  -30.2kJ/molepH: 7.5 T: 2°CAssay Description:The Ki values were calculated based on an experimentally determined appropriate Kd value according to Cheng and Prusoff.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H2 receptor(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  8.51E+3nM ΔG°:  -28.9kJ/molepH: 7.4 T: 2°CAssay Description:Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Mus musculus (mouse))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi: >1.00E+4nM ΔG°: >-28.5kJ/molepH: 7.5 T: 2°CAssay Description:The Ki values were calculated based on an experimentally determined appropriate Kd value according to Cheng and Prusoff.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi: >1.00E+4nM ΔG°: >-28.5kJ/molepH: 7.5 T: 2°CAssay Description:The Ki values were calculated based on an experimentally determined appropriate Kd value according to Cheng and Prusoff.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  1.53E+4nMAssay Description:Binding affinity to human histamine H3 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi: >2.00E+4nMAssay Description:Binding affinity to human histamine H3 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  4.68E+4nMAssay Description:Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  3.99E+6nMAssay Description:Antagonist activity at Homo sapiens (human) histamine H4 receptorMore data for this Ligand-Target Pair
In DepthDetails Article
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  4.00E+6nMAssay Description:Antagonist activity at Homo sapiens (human) histamine H4 receptorMore data for this Ligand-Target Pair
In DepthDetails Article
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  1.69E+7nMAssay Description:Antagonist activity at Homo sapiens (human) histamine H4 receptorMore data for this Ligand-Target Pair
In DepthDetails Article
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

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))
Griffin Discoveries

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))
Griffin Discoveries

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))
Griffin Discoveries

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(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataIC50:  40nMAssay Description:Inhibition of histamine H4 receptor-mediated chemotaxis in mouse bone marrow cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataIC50:  86nMAssay Description:Inhibition of histamine H4 receptor-mediated chemotaxis in human eosinophilsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataIC50:  199nMAssay 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))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataIC50:  200nMAssay Description:Antagonist actiivty at human H4R expressed in human U2OS cells assessed as inhibition of [35S]GTPgammaS binding after 30 mins by scintillation proxim...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataIC50:  221nMAssay 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 H3 receptor(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataIC50: >1.00E+5nMAssay Description:Displacement of [3H]-N-alpha-methylhistamine from recombinant human histamine H3 receptor expressed in CHO-K1 cell membranes measured after 30 mins b...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataEC50:  25nMAssay Description:Agonist activity at human H4R expressed in human U2OS cells assessed as recruitment of beta-arrestin after 2 hrs by PathHunter beta-galactosidase enz...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Rattus norvegicus (rat))
Johnson & Johnson Pharmaceutical Research And Development

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataEC50:  741nMAssay Description:Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Cavia porcellus (domestic guinea pig))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKd:  1.58E+3nMAssay 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 DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Mus musculus (mouse))
Pfizer

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataEC50:  794nMAssay Description:Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Griffin Discoveries

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataEC50:  13nMAssay Description:Agonist activity at histamine H4 receptor (unknown origin) assessed as increase in beta-arrestin recruitmentMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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