Found 25 hits Enz. Inhib. hit(s) with Target = 'Histamine H3 receptor' and Ligand = 'BDBM27213' 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)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
Reactome pathway KEGG
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| 0.490 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Freie Universit£t Berlin
Curated by ChEMBL
| Assay Description Effect on histamine H3 receptors in vitro, on synaptosomes of rat cerebral cortex for the release of [3H]histamine |
J Med Chem 43: 3987-94 (2000)
BindingDB Entry DOI: 10.7270/Q2833SRN |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(Rattus norvegicus (rat)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| 0.490 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Freie Universität Berlin
Curated by ChEMBL
| Assay Description In vitro binding affinity against rat histamine H3 receptor |
J Med Chem 47: 2678-87 (2004)
Article DOI: 10.1021/jm031065q BindingDB Entry DOI: 10.7270/Q2SQ8ZTC |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(Rattus norvegicus (rat)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| 0.490 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Freie Universität Berlin
Curated by ChEMBL
| Assay Description In vitro inhibitory activity against Histamine H3 receptor for K+ evoked depolarization-induced release of [3H]-histamine from synaptosomes of rat ce... |
Bioorg Med Chem Lett 10: 2379-82 (2001)
BindingDB Entry DOI: 10.7270/Q28G8JZ4 |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(Rattus norvegicus (rat)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| 0.490 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Freie Universität Berlin
Curated by ChEMBL
| Assay Description Histamine H3 receptor antagonist activity in an assay with K+ evoked depolarization-induced release of [3H]-histamine from rat synaptosomes. |
J Med Chem 43: 3335-43 (2000)
BindingDB Entry DOI: 10.7270/Q2RR1XGV |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(Rattus norvegicus (rat)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| 0.510 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Abbott Laboratories
Curated by ChEMBL
| Assay Description In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing rat histamine H3 receptor |
J Med Chem 48: 38-55 (2005)
Article DOI: 10.1021/jm040118g BindingDB Entry DOI: 10.7270/Q2571CST |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(Rattus norvegicus (rat)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| 0.630 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
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: 5423-30 (2008)
Article DOI: 10.1021/jm8003625 BindingDB Entry DOI: 10.7270/Q21G0JK0 |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(GUINEA PIG) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| Article PubMed
| 1.74 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Abbott Laboratories
Curated by PDSP Ki Database
| |
J Pharmacol Exp Ther 313: 165-75 (2005)
Article DOI: 10.1124/jpet.104.078303 BindingDB Entry DOI: 10.7270/Q2SN07JC |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(GUINEA PIG) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| 1.74 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Abbott Laboratories
Curated by PDSP Ki Database
| |
J Pharmacol Exp Ther 305: 887-96 (2003)
Article DOI: 10.1124/jpet.102.047183 BindingDB Entry DOI: 10.7270/Q22J69FK |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(Rattus norvegicus (rat)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| 3.90 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Freie Universität Berlin
Curated by ChEMBL
| Assay Description Inhibition of [125I]-iodoproxyfan from rat histamine H3 receptor expressed in CHO-K1 cells |
Bioorg Med Chem Lett 11: 951-4 (2001)
BindingDB Entry DOI: 10.7270/Q28P5ZRB |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(Homo sapiens (Human)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| 46 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Freie Universität Berlin
Curated by ChEMBL
| Assay Description Inhibition of [125I]-iodoproxyfan binding to human histamine H3 receptor of CHO-K1 cells |
Bioorg Med Chem Lett 11: 951-4 (2001)
BindingDB Entry DOI: 10.7270/Q28P5ZRB |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(Homo sapiens (Human)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| 46 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Goethe University
Curated by ChEMBL
| Assay Description Displacement of [3H]Nalpha-methylhistamine from human recombinant histamine H3 receptor expressed in HEK-293 cells |
ACS Med Chem Lett 4: 269-73 (2013)
Article DOI: 10.1021/ml300383n BindingDB Entry DOI: 10.7270/Q2N87C3T |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(Homo sapiens (Human)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| 46 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Freie Universit£t Berlin
Curated by ChEMBL
| Assay Description Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressing CHO cells |
J Med Chem 46: 1523-30 (2003)
Article DOI: 10.1021/jm021084k BindingDB Entry DOI: 10.7270/Q2C24X5N |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(Homo sapiens (Human)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| Article PubMed
| 46 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Jagiellonian University Medical College
Curated by ChEMBL
| Assay Description Displacement of [125I]iodoproxyfan from human full-length histamine H3 receptor expressed in HEK293 cells after 60 mins |
Bioorg Med Chem 19: 2850-8 (2011)
Article DOI: 10.1016/j.bmc.2011.03.046 BindingDB Entry DOI: 10.7270/Q2X63N8N |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(Homo sapiens (Human)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| Article PubMed
| 46 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Jagiellonian University Medical College
Curated by ChEMBL
| Assay Description Displacement of [3H]iodoproxyfan from human histamine H3 receptor expressed in CHO-K1 cells |
Bioorg Med Chem Lett 19: 6682-5 (2009)
Article DOI: 10.1016/j.bmcl.2009.10.005 BindingDB Entry DOI: 10.7270/Q2GM87DG |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(Homo sapiens (Human)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| Article PubMed
| 62.5 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Abbott Laboratories
Curated by PDSP Ki Database
| |
Eur J Pharmacol 487: 183-97 (2004)
Article DOI: 10.1016/j.ejphar.2004.01.015 BindingDB Entry DOI: 10.7270/Q2NZ866C |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(Homo sapiens (Human)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| 63 | -41.1 | 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: 5423-30 (2008)
Article DOI: 10.1021/jm8003625 BindingDB Entry DOI: 10.7270/Q21G0JK0 |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(Homo sapiens (Human)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| Article PubMed
| 63 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
National Institute of Mental Health
Curated by ChEMBL
| Assay Description Binding affinity to human H3 receptor |
J Med Chem 55: 2406-15 (2012)
Article DOI: 10.1021/jm201690h BindingDB Entry DOI: 10.7270/Q2BR8T6Z |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(Homo sapiens (Human)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| Article PubMed
| 63 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Abbott Laboratories
Curated by ChEMBL
| Assay Description In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing human histamine H3 receptor |
J Med Chem 48: 38-55 (2005)
Article DOI: 10.1021/jm040118g BindingDB Entry DOI: 10.7270/Q2571CST |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(Homo sapiens (Human)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| Article PubMed
| 63.1 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Abbott Laboratories
Curated by PDSP Ki Database
| |
J Pharmacol Exp Ther 305: 887-96 (2003)
Article DOI: 10.1124/jpet.102.047183 BindingDB Entry DOI: 10.7270/Q22J69FK |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(Homo sapiens (Human)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| Article PubMed
| 63.1 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Abbott Laboratories
Curated by PDSP Ki Database
| |
J Pharmacol Exp Ther 313: 165-75 (2005)
Article DOI: 10.1124/jpet.104.078303 BindingDB Entry DOI: 10.7270/Q2SN07JC |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(Homo sapiens (Human)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| Article PubMed
| 89.1 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Abbott Laboratories
Curated by PDSP Ki Database
| |
J Pharmacol Exp Ther 313: 165-75 (2005)
Article DOI: 10.1124/jpet.104.078303 BindingDB Entry DOI: 10.7270/Q2SN07JC |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(Homo sapiens (Human)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| Article PubMed
| 89.1 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Abbott Laboratories
Curated by PDSP Ki Database
| |
J Pharmacol Exp Ther 305: 887-96 (2003)
Article DOI: 10.1124/jpet.102.047183 BindingDB Entry DOI: 10.7270/Q22J69FK |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(Homo sapiens (Human)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| Article PubMed
| 89.4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Abbott Laboratories
Curated by PDSP Ki Database
| |
Eur J Pharmacol 487: 183-97 (2004)
Article DOI: 10.1016/j.ejphar.2004.01.015 BindingDB Entry DOI: 10.7270/Q2NZ866C |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(Homo sapiens (Human)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
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| Article PubMed
| 94 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Novo Nordisk A/S
Curated by ChEMBL
| Assay Description Antagonist potency against human histamine H3 receptor expressed in CHO cells was determined by GTPgamma-S-assay |
J Med Chem 47: 2833-8 (2004)
Article DOI: 10.1021/jm031028z BindingDB Entry DOI: 10.7270/Q2T154CW |
More data for this Ligand-Target Pair | |
Histamine H3 receptor
(Homo sapiens (Human)) | BDBM27213
(4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imi...)Show InChI InChI=1S/C16H18N2O2/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14/h5-8,10-12H,1-4,9H2,(H,17,18) | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
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CHEMBL MCE PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| 94 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Novo Nordisk A/S
Curated by ChEMBL
| Assay Description Antagonist potency against human H3 receptor in GTPgamma[S]-Assay |
J Med Chem 48: 306-11 (2005)
Article DOI: 10.1021/jm040873u BindingDB Entry DOI: 10.7270/Q2N0161T |
More data for this Ligand-Target Pair | |