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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
Target
Histamine H4 receptor
(Rattus norvegicus (rat))
Johnson & Johnson Pharmaceutical Research And Development
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 2.40nM
Assay Description:
Binding affinity of compound towards rat histamine H4 receptor
More data for this Ligand-Target Pair
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Target
Histamine H4 receptor
(Rattus norvegicus (rat))
Johnson & Johnson Pharmaceutical Research And Development
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 2.60nM ΔG°: -49.0kJ/mole
pH: 7.5 T: 2°C
Assay 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
Target Info
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Target
Histamine H4 receptor
(Rattus norvegicus (rat))
Johnson & Johnson Pharmaceutical Research And Development
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 2.70nM ΔG°: -48.9kJ/mole
pH: 7.4 T: 2°C
Assay 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
Target Info
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Target
Histamine H4 receptor
(Rattus norvegicus (rat))
Johnson & Johnson Pharmaceutical Research And Development
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 2.70nM ΔG°: -48.9kJ/mole
pH: 7.4 T: 2°C
Assay 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
Target Info
Reactome pathway
KEGG
UniProtKB/SwissProt
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Copy BDB DOI
Target
Histamine H4 receptor
(Mus musculus (mouse))
Pfizer
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 3.89nM
Assay Description:
Displacement of [3H]-histamine from mouse H4R expressed in HEK293T cells
More data for this Ligand-Target Pair
Target Info
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 4nM
Assay Description:
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
More data for this Ligand-Target Pair
Target Info
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KEGG
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Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 4nM
Assay Description:
Antagonist activity at Homo sapiens (human) histamine H4 receptor
More data for this Ligand-Target Pair
Target Info
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KEGG
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MCE
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PC sid
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In Depth
Details
Article
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 4nM
Assay Description:
Displacement of [3H]histamine from human histamine H4 receptor
More data for this Ligand-Target Pair
Target Info
PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
Ligand Info
Purchase
CHEMBL
MCE
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PC sid
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 4nM
Assay Description:
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
More data for this Ligand-Target Pair
Target Info
PDB
Reactome pathway
KEGG
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GoogleScholar
Ligand Info
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CHEMBL
MCE
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PC sid
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 4nM
Assay Description:
Binding affinity to human histamine H4 receptor
More data for this Ligand-Target Pair
Target Info
PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
Ligand Info
Purchase
CHEMBL
MCE
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PC sid
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 4nM
Assay Description:
Displacement of [3H]- histamine from the recombinant human histamine H4 receptor
More data for this Ligand-Target Pair
Target Info
PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
Ligand Info
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CHEMBL
MCE
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PC sid
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 4.10nM ΔG°: -47.9kJ/mole
pH: 7.5 T: 2°C
Assay 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
Target Info
PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
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GoogleScholar
Ligand Info
Purchase
CHEMBL
MCE
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PC sid
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 4.17nM
Assay Description:
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
More data for this Ligand-Target Pair
Target Info
PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
Ligand Info
Purchase
CHEMBL
MCE
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PC sid
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 4.20nM
Assay 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
Target Info
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In Depth
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Copy BDB DOI
Target
Histamine H4 receptor
(Rattus norvegicus (rat))
Johnson & Johnson Pharmaceutical Research And Development
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 4.27nM
Assay Description:
Displacement of [3H]-histamine from rat H4R expressed in HEK293T cells
More data for this Ligand-Target Pair
Target Info
Reactome pathway
KEGG
UniProtKB/SwissProt
GoogleScholar
Ligand Info
Purchase
CHEMBL
MCE
PC cid
PC sid
Patents
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 4.5nM
Assay Description:
Binding affinity to human histamine H4 receptor
More data for this Ligand-Target Pair
Target Info
PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
Ligand Info
Purchase
CHEMBL
MCE
PC cid
PC sid
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Mus musculus (mouse))
Pfizer
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 4.60nM ΔG°: -47.6kJ/mole
pH: 7.5 T: 2°C
Assay 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
Target Info
Reactome pathway
KEGG
UniProtKB/SwissProt
GoogleScholar
Ligand Info
Purchase
CHEMBL
MCE
PC cid
PC sid
Patents
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Rattus norvegicus (rat))
Johnson & Johnson Pharmaceutical Research And Development
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 4.70nM ΔG°: -47.5kJ/mole
pH: 7.4 T: 2°C
Assay 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
Target Info
Reactome pathway
KEGG
UniProtKB/SwissProt
GoogleScholar
Ligand Info
Purchase
CHEMBL
MCE
PC cid
PC sid
Patents
Similars
In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 4.90nM
Assay Description:
Displacement of [3H]histamine from human histamine 4 receptor expressed in HEK293T cell membranes incubated for 1 hr by radioligand binding assay
More data for this Ligand-Target Pair
Target Info
PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
Ligand Info
Purchase
CHEMBL
MCE
PC cid
PC sid
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 5nM
Assay Description:
Displacement of [3H]histamine from human recombinant histamine H4 receptor
More data for this Ligand-Target Pair
Target Info
PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
Ligand Info
Purchase
CHEMBL
MCE
PC cid
PC sid
Patents
Similars
In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 5nM
Assay Description:
Displacement of [3H]histamine from human recombinant histamine H4 receptor
More data for this Ligand-Target Pair
Target Info
PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
Ligand Info
Purchase
CHEMBL
MCE
PC cid
PC sid
Patents
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 5nM
Assay Description:
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
More data for this Ligand-Target Pair
Target Info
PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
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antibodypedia
GoogleScholar
Ligand Info
Purchase
CHEMBL
MCE
PC cid
PC sid
Patents
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 6nM
Assay Description:
Binding affinity to human histamine H4 receptor
More data for this Ligand-Target Pair
Target Info
PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
Ligand Info
Purchase
CHEMBL
MCE
PC cid
PC sid
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Rattus norvegicus (rat))
Johnson & Johnson Pharmaceutical Research And Development
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 6nM
Assay Description:
Binding affinity to rat histamine H4 receptor
More data for this Ligand-Target Pair
Target Info
Reactome pathway
KEGG
UniProtKB/SwissProt
GoogleScholar
Ligand Info
Purchase
CHEMBL
MCE
PC cid
PC sid
Patents
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 6.30nM
Assay Description:
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
More data for this Ligand-Target Pair
Target Info
PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
Ligand Info
Purchase
CHEMBL
MCE
PC cid
PC sid
Patents
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 6.31nM
Assay Description:
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
More data for this Ligand-Target Pair
Target Info
PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
Ligand Info
Purchase
CHEMBL
MCE
PC cid
PC sid
Patents
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 6.80nM
Assay 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
Target Info
PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
Ligand Info
Purchase
CHEMBL
MCE
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PC sid
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 6.80nM
Assay Description:
Antagonist activity at human histamine H4 receptor by functional assay
More data for this Ligand-Target Pair
Target Info
PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
Ligand Info
Purchase
CHEMBL
MCE
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PC sid
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 6.80nM
Assay 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
Target Info
PDB
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KEGG
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CHEMBL
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PC sid
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 6.80nM
Assay 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
Target Info
PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
Ligand Info
Purchase
CHEMBL
MCE
PC cid
PC sid
Patents
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 8nM
Assay Description:
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
More data for this Ligand-Target Pair
Target Info
PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
antibodypedia
GoogleScholar
Ligand Info
Purchase
CHEMBL
MCE
PC cid
PC sid
Patents
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 8nM
Assay Description:
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
More data for this Ligand-Target Pair
Target Info
PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
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CHEMBL
MCE
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PC sid
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 8nM
Assay 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
Target Info
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 8nM
Assay Description:
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 12nM ΔG°: -45.2kJ/mole
pH: 7.4 T: 2°C
Assay Description:
Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac...
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
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Affinity Data
Ki: 12nM ΔG°: -45.2kJ/mole
pH: 7.4 T: 2°C
Assay Description:
Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac...
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Target
Histamine H4 receptor
(Mus musculus (mouse))
Pfizer
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 12nM
Assay 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...
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
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Affinity Data
Ki: 12nM ΔG°: -45.2kJ/mole
pH: 7.4 T: 2°C
Assay Description:
Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac...
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Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 13nM
Assay Description:
Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 13nM
Assay Description:
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 14nM
Assay Description:
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 15.8nM
Assay Description:
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 16nM
Assay Description:
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
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Copy BDB DOI
Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 16nM
Assay Description:
Ligand displacement assays were performed on The SK-N-MC/hH4R cell homogenates. Retained radioactivity was determined by liquid scintillation countin...
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 17nM
Assay Description:
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 18.6nM
Assay Description:
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillat...
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 35nM
Assay Description:
Binding affinity to histamine 4 receptor (unknown origin)
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 38nM
Assay Description:
Displacement of [3H]histamine human recombinant histamine H4 receptor
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 63nM
Assay Description:
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 63nM
Assay Description:
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co...
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
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Affinity Data
Ki: 63nM
Assay Description:
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
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Affinity Data
Ki: 63nM
Assay Description:
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 63nM
Assay Description:
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 63nM
Assay Description:
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 63nM
Assay Description:
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes c...
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 69nM
Assay Description:
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2
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Target
Histamine H4 receptor
(Mus musculus (mouse))
Pfizer
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 126nM
Assay Description:
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
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Target
Histamine H1 receptor
(Homo sapiens (Human))
Abbott Laboratories
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 977nM ΔG°: -34.3kJ/mole
pH: 7.4 T: 2°C
Assay Description:
Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac...
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Target
Histamine H2 receptor
(Cavia porcellus (domestic guinea pig))
Johnson & Johnson Pharmaceutical
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: >1.00E+3nM ΔG°: >-34.2kJ/mole
pH: 7.5 T: 2°C
Assay Description:
The Ki values were calculated based on an experimentally determined appropriate Kd value according to Cheng and Prusoff.
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Target
Histamine H1 receptor
(Cavia porcellus (domestic guinea pig))
Johnson & Johnson Pharmaceutical
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: >1.00E+3nM ΔG°: >-34.2kJ/mole
pH: 7.5 T: 2°C
Assay Description:
The Ki values were calculated based on an experimentally determined appropriate Kd value according to Cheng and Prusoff.
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Target
Histamine receptor H4
(GUINEA PIG)
Pfizer
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 1.07E+3nM
Assay Description:
Displacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cells
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Target
Histamine H3 receptor
(Rattus norvegicus (rat))
Abbott Laboratories
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 1.32E+3nM ΔG°: -33.6kJ/mole
pH: 7.4 T: 2°C
Assay Description:
Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac...
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Target
Histamine H3 receptor
(Rattus norvegicus (rat))
Abbott Laboratories
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 1.45E+3nM ΔG°: -33.3kJ/mole
pH: 7.4 T: 2°C
Assay Description:
Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac...
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Target
Histamine H3 receptor
(Homo sapiens (Human))
Abbott Laboratories
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 2.24E+3nM ΔG°: -32.2kJ/mole
pH: 7.4 T: 2°C
Assay Description:
Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac...
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Target
Histamine H3 receptor
(Homo sapiens (Human))
Abbott Laboratories
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 2.24E+3nM ΔG°: -32.2kJ/mole
pH: 7.4 T: 2°C
Assay Description:
Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac...
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Target
Histamine H3 receptor
(Rattus norvegicus (rat))
Abbott Laboratories
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 4.70E+3nM ΔG°: -30.4kJ/mole
pH: 7.5 T: 2°C
Assay Description:
The Ki values were calculated based on an experimentally determined appropriate Kd value according to Cheng and Prusoff.
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Histamine H3 receptor
(Homo sapiens (Human))
Abbott Laboratories
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 5.01E+3nM
Assay Description:
Displacement of [3H]histamine from human H3 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
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Target
Histamine H3 receptor
(Homo sapiens (Human))
Abbott Laboratories
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 5.01E+3nM
Assay Description:
Ligand displacement assays were performed on The SK-N-MC/hH3R cell homogenates. Retained radioactivity was determined by liquid scintillation countin...
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Target
Histamine H3 receptor
(Homo sapiens (Human))
Abbott Laboratories
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 5.13E+3nM
Assay Description:
Binding affinity to histamine H3 receptor
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Target
Histamine H3 receptor
(Homo sapiens (Human))
Abbott Laboratories
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 5.13E+3nM ΔG°: -30.2kJ/mole
pH: 7.5 T: 2°C
Assay Description:
The Ki values were calculated based on an experimentally determined appropriate Kd value according to Cheng and Prusoff.
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Target
Histamine H2 receptor
(Homo sapiens (Human))
Abbott Laboratories
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 8.51E+3nM ΔG°: -28.9kJ/mole
pH: 7.4 T: 2°C
Assay Description:
Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac...
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Target
Histamine H1 receptor
(Mus musculus (mouse))
Johnson & Johnson Pharmaceutical
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: >1.00E+4nM ΔG°: >-28.5kJ/mole
pH: 7.5 T: 2°C
Assay Description:
The Ki values were calculated based on an experimentally determined appropriate Kd value according to Cheng and Prusoff.
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Target
Histamine H1 receptor
(Homo sapiens (Human))
Abbott Laboratories
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: >1.00E+4nM ΔG°: >-28.5kJ/mole
pH: 7.5 T: 2°C
Assay Description:
The Ki values were calculated based on an experimentally determined appropriate Kd value according to Cheng and Prusoff.
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Target
Histamine H3 receptor
(Homo sapiens (Human))
Abbott Laboratories
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 1.53E+4nM
Assay Description:
Binding affinity to human histamine H3 receptor
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Target
Histamine H3 receptor
(Homo sapiens (Human))
Abbott Laboratories
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: >2.00E+4nM
Assay Description:
Binding affinity to human histamine H3 receptor
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Target
Histamine H1 receptor
(Homo sapiens (Human))
Abbott Laboratories
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 4.68E+4nM
Assay Description:
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 3.99E+6nM
Assay Description:
Antagonist activity at Homo sapiens (human) histamine H4 receptor
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 4.00E+6nM
Assay Description:
Antagonist activity at Homo sapiens (human) histamine H4 receptor
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Ki: 1.69E+7nM
Assay Description:
Antagonist activity at Homo sapiens (human) histamine H4 receptor
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
IC50: 5.30nM
Assay Description:
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
IC50: 13nM
Assay Description:
Antagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-ind...
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
IC50: 29nM
Assay Description:
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta sc...
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
IC50: 30nM
Assay Description:
Antagonist activity at H4R in human eosinophils assessed as inhibition of imetit-induced shape change by GAFS assay
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Target
Histamine H4 receptor
(Mus musculus (mouse))
Pfizer
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
IC50: 40nM
Assay Description:
Inhibition of histamine H4 receptor-mediated chemotaxis in mouse bone marrow cells
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
IC50: 86nM
Assay Description:
Inhibition of histamine H4 receptor-mediated chemotaxis in human eosinophils
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
IC50: 199nM
Assay Description:
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
IC50: 200nM
Assay Description:
Antagonist actiivty at human H4R expressed in human U2OS cells assessed as inhibition of [35S]GTPgammaS binding after 30 mins by scintillation proxim...
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
IC50: 221nM
Assay Description:
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation
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Target
Histamine H3 receptor
(Homo sapiens (Human))
Abbott Laboratories
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
IC50: >1.00E+5nM
Assay Description:
Displacement of [3H]-N-alpha-methylhistamine from recombinant human histamine H3 receptor expressed in CHO-K1 cell membranes measured after 30 mins b...
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
EC50: 25nM
Assay 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...
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Target
Histamine H4 receptor
(Rattus norvegicus (rat))
Johnson & Johnson Pharmaceutical Research And Development
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
EC50: 741nM
Assay Description:
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assay
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Target
Histamine H1 receptor
(Cavia porcellus (domestic guinea pig))
Johnson & Johnson Pharmaceutical
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
Kd: 1.58E+3nM
Assay Description:
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
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Target
Histamine H4 receptor
(Mus musculus (mouse))
Pfizer
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
EC50: 794nM
Assay Description:
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
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Target
Histamine H4 receptor
(Homo sapiens (Human))
Griffin Discoveries
Curated by
ChEMBL
Ligand
BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
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Affinity Data
EC50: 13nM
Assay Description:
Agonist activity at histamine H4 receptor (unknown origin) assessed as increase in beta-arrestin recruitment
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