Compile Data Set for Download or QSAR
Report error Found 134 Enz. Inhib. hit(s) with all data for entry = 50010420
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50214615(CHEBI:64177 | Clobenpropit)
Affinity DataKi:  0.251nMAssay Description:Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H3R expressed in HEK293T cells by Nano-BRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50214615(CHEBI:64177 | Clobenpropit)
Affinity DataKi:  0.339nMAssay Description:Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H3R expressed in HEK293T cells measured after 30 mins by furimazine substrate b...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50214615(CHEBI:64177 | Clobenpropit)
Affinity DataKi:  0.501nMAssay Description:Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H3R expressed in baculovirus infected Sf9 insect cell membranes co...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538682(CHEMBL4597218)
Affinity DataKi:  0.537nMAssay Description:Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H3R expressed in HEK293T cells measured after 30 mins by furimazine substrate b...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538678(CHEMBL4642520)
Affinity DataKi:  0.912nMAssay Description:Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H3R expressed in baculovirus infected Sf9 insect cell membranesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538678(CHEMBL4642520)
Affinity DataKd:  0.970nMAssay Description:Binding affinity to human recombinant NLuc/GPCR-fused H3R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538678(CHEMBL4642520)
Affinity DataKd:  0.970nMAssay Description:Binding affinity to human recombinant NLuc/GPCR-fused H3R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Mouse)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538682(CHEMBL4597218)
Affinity DataKi:  1.20nMAssay 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 Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538682(CHEMBL4597218)
Affinity DataKi:  1.20nMAssay 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 Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538677(CHEMBL4635634)
Affinity DataKd:  1.35nMAssay Description:Binding affinity to human recombinant NLuc/GPCR-fused H3R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538677(CHEMBL4635634)
Affinity DataKd:  1.40nMAssay Description:Binding affinity to human recombinant NLuc/GPCR-fused H3R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
University of Regensburg

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
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538677(CHEMBL4635634)
Affinity DataEC50:  1.70nMAssay Description:Agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538677(CHEMBL4635634)
Affinity DataKi:  2.5nMAssay Description:Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H3R expressed in baculovirus infected Sf9 insect cell membranesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538677(CHEMBL4635634)
Affinity DataKd:  2.5nMAssay Description:Binding affinity to human recombinant NLuc/GPCR-fused H3R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in pres...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50214615(CHEBI:64177 | Clobenpropit)
Affinity DataKi:  2.5nMAssay Description:Displacement of [3H]-N-alpha-methylhistamine from human recombinant H3R expressed in human SK-N-MC cell membranesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538677(CHEMBL4635634)
Affinity DataKd:  2.54nMAssay Description:Binding affinity to human recombinant NLuc/GPCR-fused H3R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in pres...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538682(CHEMBL4597218)
Affinity DataKi:  3.20nMAssay Description:Displacement of [3H]-N-alpha-methylhistamine from Galphai2/Gbeta1gamma2-coupled human recombinant H3R expressed in baculovirus infected Sf9 insect ce...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50121205(CHEBI:18295 | Histamine)
Affinity DataEC50:  3.30nMAssay Description:Agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM22566(CHEMBL129198 | 5-chloro-2-[(4-methylpiperazin-1-yl...)
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 Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50170164(Imbutamine)
Affinity DataKi:  4.30nMAssay Description:Displacement of [3H]-N-alpha-methylhistamine from Galphai2/Gbeta1gamma2-coupled human recombinant H3R expressed in baculovirus infected Sf9 insect ce...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538682(CHEMBL4597218)
Affinity DataKi:  5nMAssay 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 Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538677(CHEMBL4635634)
Affinity DataKd:  9.16nMAssay Description:Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in pres...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538677(CHEMBL4635634)
Affinity DataKd:  9.20nMAssay Description:Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in pres...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50121205(CHEBI:18295 | Histamine)
Affinity DataKi:  10nMAssay Description:Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H3R expressed in baculovirus infected Sf9 insect cell membranes co...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50121205(CHEBI:18295 | Histamine)
Affinity DataKi:  10nMAssay Description:Displacement of [3H]-N-alpha-methylhistamine from human recombinant H3R expressed in human SK-N-MC cell membranesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538676(CHEMBL4636487)
Affinity DataKi:  12nMAssay Description:Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H3R expressed in baculovirus infected Sf9 insect cell membranesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Mouse)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM22566(CHEMBL129198 | 5-chloro-2-[(4-methylpiperazin-1-yl...)
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 Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538681(CHEMBL4595327)
Affinity DataKi:  12nMAssay 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 Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50170164(Imbutamine)
Affinity DataKi:  13nMAssay Description:Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM22566(CHEMBL129198 | 5-chloro-2-[(4-methylpiperazin-1-yl...)
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 Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538681(CHEMBL4595327)
Affinity DataKi:  13nMAssay 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 Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50121205(CHEBI:18295 | Histamine)
Affinity DataKi:  13nMAssay Description:Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Mouse)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538682(CHEMBL4597218)
Affinity DataEC50:  13nMAssay Description:Agonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538679(CHEMBL4634235)
Affinity DataKi:  13nMAssay Description:Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H3R expressed in baculovirus infected Sf9 insect cell membranesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538677(CHEMBL4635634)
Affinity DataKi:  14nMAssay 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 Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
University of Regensburg

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
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50121205(CHEBI:18295 | Histamine)
Affinity DataEC50:  17nMAssay Description:Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538677(CHEMBL4635634)
Affinity DataKd:  17nMAssay Description:Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538677(CHEMBL4635634)
Affinity DataKd:  18nMAssay Description:Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50121205(CHEBI:18295 | Histamine)
Affinity DataKi:  19nMAssay Description:Displacement of [3H]-N-alpha-methylhistamine from Galphai2/Gbeta1gamma2-coupled human recombinant H3R expressed in baculovirus infected Sf9 insect ce...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataIC50: 20nMAssay Description:Inverse agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells assessed as reduction in histamine-induced inhibition of forsko...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Mouse)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM22914(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Affinity DataEC50:  28nMAssay Description:Antagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Mouse)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538677(CHEMBL4635634)
Affinity DataKd:  31nMAssay Description:Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in pres...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Mouse)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538681(CHEMBL4595327)
Affinity DataKi:  31nMAssay 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 Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Mouse)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538677(CHEMBL4635634)
Affinity DataKd:  31.2nMAssay Description:Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in pres...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50474435(Homohistamine)
Affinity DataKi:  32nMAssay Description:Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50121205(CHEBI:18295 | Histamine)
Affinity DataEC50:  34nMAssay Description:Agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment b...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H4 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50538678(CHEMBL4642520)
Affinity DataKi:  34nMAssay 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 Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetHistamine H3 receptor(Human)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM50474426(Impentamine)
Affinity DataKi:  37nMAssay Description:Displacement of [3H]-N-alpha-methylhistamine from Galphai2/Gbeta1gamma2-coupled human recombinant H3R expressed in baculovirus infected Sf9 insect ce...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
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