Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kJ/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Histamine H3 receptor (Rattus norvegicus (rat)) | BDBM22566 (5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...) | PDB Reactome pathway KEGG UniProtKB/SwissProt GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | 1.32E+3 | -33.6 | n/a | n/a | n/a | n/a | n/a | 7.4 | 25 |
Abbott Laboratories | Assay Description Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac... | J Med Chem 51: 6571-80 (2008) Article DOI: 10.1021/jm8005959 BindingDB Entry DOI: 10.7270/Q24J0CD9 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histamine H3 receptor (Rattus norvegicus (rat)) | BDBM22566 (5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...) | PDB Reactome pathway KEGG UniProtKB/SwissProt GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | 1.45E+3 | -33.3 | n/a | n/a | n/a | n/a | n/a | 7.4 | 25 |
Abbott Laboratories | Assay Description Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac... | J Med Chem 51: 7094-8 (2008) Article DOI: 10.1021/jm8007618 BindingDB Entry DOI: 10.7270/Q2862DS6 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histamine H3 receptor (Homo sapiens (Human)) | BDBM22566 (5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...) | PDB Reactome pathway KEGG UniProtKB/SwissProt DrugBank antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | 2.24E+3 | -32.2 | n/a | n/a | n/a | n/a | n/a | 7.4 | 25 |
Abbott Laboratories | Assay Description Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac... | J Med Chem 51: 6571-80 (2008) Article DOI: 10.1021/jm8005959 BindingDB Entry DOI: 10.7270/Q24J0CD9 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histamine H3 receptor (Homo sapiens (Human)) | BDBM22566 (5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...) | PDB Reactome pathway KEGG UniProtKB/SwissProt DrugBank antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | 2.24E+3 | -32.2 | n/a | n/a | n/a | n/a | n/a | 7.4 | 25 |
Abbott Laboratories | Assay Description Competition radioligand binding assays were performed with increasing concentrations of test compound in the presence of [3H]ligand. All binding reac... | J Med Chem 51: 7094-8 (2008) Article DOI: 10.1021/jm8007618 BindingDB Entry DOI: 10.7270/Q2862DS6 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histamine H3 receptor (Rattus norvegicus (rat)) | BDBM22566 (5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...) | PDB Reactome pathway KEGG UniProtKB/SwissProt GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | 4.70E+3 | -30.4 | n/a | n/a | n/a | n/a | n/a | 7.5 | 25 |
Johnson & Johnson Pharmaceutical | Assay Description The Ki values were calculated based on an experimentally determined appropriate Kd value according to Cheng and Prusoff. | J Pharmacol Exp Ther 309: 404-13 (2004) Article DOI: 10.1124/jpet.103.061754 BindingDB Entry DOI: 10.7270/Q2VX0DTD | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histamine H3 receptor (Homo sapiens (Human)) | BDBM22566 (5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...) | PDB Reactome pathway KEGG UniProtKB/SwissProt DrugBank antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | 5.01E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
VU University Amsterdam Curated by ChEMBL | Assay Description Displacement of [3H]histamine from human H3 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting | J Med Chem 54: 8136-47 (2011) Article DOI: 10.1021/jm201042n BindingDB Entry DOI: 10.7270/Q2MW2JDX | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histamine H3 receptor (Homo sapiens (Human)) | BDBM22566 (5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...) | PDB Reactome pathway KEGG UniProtKB/SwissProt DrugBank antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | 5.01E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Vrije Universiteit Amsterdam | Assay Description Ligand displacement assays were performed on The SK-N-MC/hH3R cell homogenates. Retained radioactivity was determined by liquid scintillation countin... | J Pharmacol Exp Ther 314: 1310-21 (2005) Article DOI: 10.1124/jpet.105.087965 BindingDB Entry DOI: 10.7270/Q2KD1W6V | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histamine H3 receptor (Homo sapiens (Human)) | BDBM22566 (5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...) | PDB Reactome pathway KEGG UniProtKB/SwissProt DrugBank antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | 5.13E+3 | -30.2 | n/a | n/a | n/a | n/a | n/a | 7.5 | 25 |
Johnson & Johnson Pharmaceutical | Assay Description The Ki values were calculated based on an experimentally determined appropriate Kd value according to Cheng and Prusoff. | J Pharmacol Exp Ther 309: 404-13 (2004) Article DOI: 10.1124/jpet.103.061754 BindingDB Entry DOI: 10.7270/Q2VX0DTD | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histamine H3 receptor (Homo sapiens (Human)) | BDBM22566 (5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...) | PDB Reactome pathway KEGG UniProtKB/SwissProt DrugBank antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | 5.13E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Johnson & Johnson Pharmaceutical Research and Development Curated by ChEMBL | Assay Description Binding affinity to histamine H3 receptor | J Med Chem 48: 8289-98 (2005) Article DOI: 10.1021/jm0502081 BindingDB Entry DOI: 10.7270/Q2C24W00 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histamine H3 receptor (Homo sapiens (Human)) | BDBM22566 (5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...) | PDB Reactome pathway KEGG UniProtKB/SwissProt DrugBank antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | 1.53E+4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Inc. Curated by ChEMBL | Assay Description Binding affinity to human histamine H3 receptor | Bioorg Med Chem Lett 22: 1156-9 (2012) Article DOI: 10.1016/j.bmcl.2011.11.098 BindingDB Entry DOI: 10.7270/Q2Q81DJD | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histamine H3 receptor (Homo sapiens (Human)) | BDBM22566 (5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...) | PDB Reactome pathway KEGG UniProtKB/SwissProt DrugBank antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | >2.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Inc. Curated by ChEMBL | Assay Description Binding affinity to human histamine H3 receptor | Bioorg Med Chem Lett 22: 1156-9 (2012) Article DOI: 10.1016/j.bmcl.2011.11.098 BindingDB Entry DOI: 10.7270/Q2Q81DJD | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Histamine H3 receptor (Homo sapiens (Human)) | BDBM22566 (5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...) | PDB Reactome pathway KEGG UniProtKB/SwissProt DrugBank antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid UniChem Patents Similars | Article PubMed | n/a | n/a | >1.00E+5 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | 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... | Citation and Details Article DOI: 10.1021/acs.jmedchem.7b01855 BindingDB Entry DOI: 10.7270/Q2ZG6WZQ | |||||||||||
More data for this Ligand-Target Pair |