Found 379 hits for monomerid = 22880,22881,22883,22566,22890,22891,22893,22567,22542,24226,27213,27193,26226,26390,26391 Target/Host
(Institution) | Ligand | Target/Host
Links | Ligand
Links | Trg + Lig
Links | Ki
nM | ΔG°
kcal/mole | IC50
nM | Kd
nM | EC50/IC50
nM | koff
s-1 | kon
M-1s-1 | pH | Temp
°C |
|---|
Histamine H3 receptor
(Homo sapiens (Human)) | BDBM22542
(4-(1H-imidazol-4-ylmethyl)piperidine | 4-(1H-imida...)Show InChI InChI=1S/C9H15N3/c1-3-10-4-2-8(1)5-9-6-11-7-12-9/h6-8,10H,1-5H2,(H,11,12) | PDB
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| 0.300 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Meiji Seika Kaisha, Ltd
Curated by ChEMBL
| Assay Description
Displacement of [3H] (R)-alpha-methylhistamine from human recombinant histamine H3 receptor expressed in CHO cells after 1 hr by liquid scintillation... |
Bioorg Med Chem 18: 5441-8 (2010)
Article DOI: 10.1016/j.bmc.2010.04.052
BindingDB Entry DOI: 10.7270/Q2C82B88 |
More data for this
Ligand-Target Pair | |
Histamine H3 receptor
(Homo sapiens (Human)) | BDBM22542
(4-(1H-imidazol-4-ylmethyl)piperidine | 4-(1H-imida...)Show InChI InChI=1S/C9H15N3/c1-3-10-4-2-8(1)5-9-6-11-7-12-9/h6-8,10H,1-5H2,(H,11,12) | PDB
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| 0.300 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Meiji Seika Kaisha, Ltd.
Curated by ChEMBL
| Assay Description
Displacement of [3H]-(R)-alpha-methylhistamine from human histamine H3 receptor expressed in CHO cells by liquid scintillation counting |
J Med Chem 53: 6445-56 (2010)
Article DOI: 10.1021/jm100643t
BindingDB Entry DOI: 10.7270/Q2QF8T3X |
More data for this
Ligand-Target Pair | |
Histamine H3 receptor
(GUINEA PIG) | BDBM22542
(4-(1H-imidazol-4-ylmethyl)piperidine | 4-(1H-imida...)Show InChI InChI=1S/C9H15N3/c1-3-10-4-2-8(1)5-9-6-11-7-12-9/h6-8,10H,1-5H2,(H,11,12) | PDB
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| 0.400 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
The Schering Plough Research Institute
Curated by ChEMBL
| Assay Description
Displacement of [3H]-N-alpha-methylhistamine from histamine H3 receptor in guinea pig brain |
Bioorg Med Chem Lett 16: 395-9 (2005)
Article DOI: 10.1016/j.bmcl.2005.09.076
BindingDB Entry DOI: 10.7270/Q29S1QK1 |
More data for this
Ligand-Target Pair | |
Histamine H3 receptor
(Homo sapiens (Human)) | BDBM22542
(4-(1H-imidazol-4-ylmethyl)piperidine | 4-(1H-imida...)Show InChI InChI=1S/C9H15N3/c1-3-10-4-2-8(1)5-9-6-11-7-12-9/h6-8,10H,1-5H2,(H,11,12) | PDB
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| 0.400 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
The R. W. Johnson Pharmaceutical Research Institute
Curated by PDSP Ki Database
| |
Mol Pharmacol 59: 420-6 (2001)
Article DOI: 10.1124/mol.59.3.420
BindingDB Entry DOI: 10.7270/Q26Q1VSR |
More data for this
Ligand-Target Pair | |
Histamine H3 receptor
(Homo sapiens (Human)) | BDBM22542
(4-(1H-imidazol-4-ylmethyl)piperidine | 4-(1H-imida...)Show InChI InChI=1S/C9H15N3/c1-3-10-4-2-8(1)5-9-6-11-7-12-9/h6-8,10H,1-5H2,(H,11,12) | PDB
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| 0.407 | -12.8 | n/a | n/a | n/a | n/a | n/a | 7.4 | 25 |
VU University Amsterdam
| Assay Description
Ligand displacement assays were performed on CHO cells membranes expressing hH3R. Retained radioactivity was determined by liquid scintillation count... |
J Med Chem 51: 2944-53 (2008)
Article DOI: 10.1021/jm7014149
BindingDB Entry DOI: 10.7270/Q24F1P2W |
More data for this
Ligand-Target Pair | |
Hrh3 protein
(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) | KEGG
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| 0.427 | 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
(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
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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| 0.490 | 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 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 | |
Hrh3 protein
(RAT) | BDBM22542
(4-(1H-imidazol-4-ylmethyl)piperidine | 4-(1H-imida...)Show InChI InChI=1S/C9H15N3/c1-3-10-4-2-8(1)5-9-6-11-7-12-9/h6-8,10H,1-5H2,(H,11,12) | KEGG
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| 0.5 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
R. W. Johnson Pharmaceutical Research Institute
Curated by PDSP Ki Database
| |
J Pharmacol Exp Ther 293: 771-8 (2000)
BindingDB Entry DOI: 10.7270/Q2348HX8 |
More data for this
Ligand-Target Pair | |
Histamine H3 receptor
(Homo sapiens (Human)) | BDBM22542
(4-(1H-imidazol-4-ylmethyl)piperidine | 4-(1H-imida...)Show InChI InChI=1S/C9H15N3/c1-3-10-4-2-8(1)5-9-6-11-7-12-9/h6-8,10H,1-5H2,(H,11,12) | PDB
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| 0.501 | 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)) | BDBM22542
(4-(1H-imidazol-4-ylmethyl)piperidine | 4-(1H-imida...)Show InChI InChI=1S/C9H15N3/c1-3-10-4-2-8(1)5-9-6-11-7-12-9/h6-8,10H,1-5H2,(H,11,12) | PDB
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| 0.501 | 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
(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 | |
Hrh3 protein
(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) | KEGG
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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 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 | |
Hrh3 protein
(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) | KEGG
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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 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 H1 receptor
(Cavia porcellus (domestic guinea pig)) | BDBM22567
(3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramin...)Show InChI InChI=1S/C17H23N3O/c1-19(2)12-13-20(17-6-4-5-11-18-17)14-15-7-9-16(21-3)10-8-15/h4-11H,12-14H2,1-3H3 | UniProtKB/SwissProt
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| 0.570 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
University of North Carolina at Chapel Hill
Curated by PDSP Ki Database
| |
J Pharmacol Exp Ther 302: 328-36 (2002)
Article DOI: 10.1124/jpet.302.1.328
BindingDB Entry DOI: 10.7270/Q2JQ0ZK1 |
More data for this
Ligand-Target Pair | |
Hrh3 protein
(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) | KEGG
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| 0.630 | 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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| 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 | |
Hrh3 protein
(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) | KEGG
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| 0.630 | 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 | |
Hrh3 protein
(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) | KEGG
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| 0.654 | 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 H1 receptor
(Homo sapiens (Human)) | BDBM22567
(3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramin...)Show InChI InChI=1S/C17H23N3O/c1-19(2)12-13-20(17-6-4-5-11-18-17)14-15-7-9-16(21-3)10-8-15/h4-11H,12-14H2,1-3H3 | PDB
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Article
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| 0.710 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
The University of Newcastle
Curated by ChEMBL
| Assay Description
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation counting |
J Med Chem 60: 349-361 (2017)
Article DOI: 10.1021/acs.jmedchem.6b01422
BindingDB Entry DOI: 10.7270/Q27M0B6T |
More data for this
Ligand-Target Pair | |
Histamine H1 receptor
(Cavia porcellus (domestic guinea pig)) | BDBM22567
(3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramin...)Show InChI InChI=1S/C17H23N3O/c1-19(2)12-13-20(17-6-4-5-11-18-17)14-15-7-9-16(21-3)10-8-15/h4-11H,12-14H2,1-3H3 | UniProtKB/SwissProt
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| 0.740 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
University of North Carolina at Chapel Hill
Curated by PDSP Ki Database
| |
J Pharmacol Exp Ther 302: 328-36 (2002)
Article DOI: 10.1124/jpet.302.1.328
BindingDB Entry DOI: 10.7270/Q2JQ0ZK1 |
More data for this
Ligand-Target Pair | |
Histamine H1 receptor
(Homo sapiens (Human)) | BDBM24226
(1-[(4-fluorophenyl)methyl]-N-{1-[2-(4-methoxypheny...)Show SMILES COc1ccc(CCN2CCC(CC2)Nc2nc3ccccc3n2Cc2ccc(F)cc2)cc1 Show InChI InChI=1S/C28H31FN4O/c1-34-25-12-8-21(9-13-25)14-17-32-18-15-24(16-19-32)30-28-31-26-4-2-3-5-27(26)33(28)20-22-6-10-23(29)11-7-22/h2-13,24H,14-20H2,1H3,(H,30,31) | PDB
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| 0.800 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Janssen Research Foundation
Curated by PDSP Ki Database
| |
Psychopharmacology (Berl) 124: 57-73 (1996)
Article DOI: 10.1007/bf02245606
BindingDB Entry DOI: 10.7270/Q2610XV6 |
More data for this
Ligand-Target Pair | |
Histamine H1 receptor
(Cavia porcellus (domestic guinea pig)) | BDBM24226
(1-[(4-fluorophenyl)methyl]-N-{1-[2-(4-methoxypheny...)Show SMILES COc1ccc(CCN2CCC(CC2)Nc2nc3ccccc3n2Cc2ccc(F)cc2)cc1 Show InChI InChI=1S/C28H31FN4O/c1-34-25-12-8-21(9-13-25)14-17-32-18-15-24(16-19-32)30-28-31-26-4-2-3-5-27(26)33(28)20-22-6-10-23(29)11-7-22/h2-13,24H,14-20H2,1H3,(H,30,31) | UniProtKB/SwissProt
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| 0.800 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Janssen Research Foundation
Curated by PDSP Ki Database
| |
Psychopharmacology (Berl) 124: 57-73 (1996)
Article DOI: 10.1007/bf02245606
BindingDB Entry DOI: 10.7270/Q2610XV6 |
More data for this
Ligand-Target Pair | |
Histamine H1 receptor
(Homo sapiens (Human)) | BDBM22567
(3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramin...)Show InChI InChI=1S/C17H23N3O/c1-19(2)12-13-20(17-6-4-5-11-18-17)14-15-7-9-16(21-3)10-8-15/h4-11H,12-14H2,1-3H3 | PDB
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| DrugBank
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| 0.950 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Universit£ degli Studi di Siena
Curated by ChEMBL
| Assay Description
Binding affinity to human histamine H1 receptor by radioligand displacement assay |
Eur J Med Chem 63: 85-94 (2013)
Article DOI: 10.1016/j.ejmech.2013.01.044
BindingDB Entry DOI: 10.7270/Q2JH3NKC |
More data for this
Ligand-Target Pair | |
Histamine H1 receptor
(Homo sapiens (Human)) | BDBM22567
(3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramin...)Show InChI InChI=1S/C17H23N3O/c1-19(2)12-13-20(17-6-4-5-11-18-17)14-15-7-9-16(21-3)10-8-15/h4-11H,12-14H2,1-3H3 | PDB
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| 1.01 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
University of North Carolina at Chapel Hill
Curated by PDSP Ki Database
| |
J Pharmacol Exp Ther 302: 328-36 (2002)
Article DOI: 10.1124/jpet.302.1.328
BindingDB Entry DOI: 10.7270/Q2JQ0ZK1 |
More data for this
Ligand-Target Pair | |
Histamine H1 receptor
(Homo sapiens (Human)) | BDBM22567
(3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramin...)Show InChI InChI=1S/C17H23N3O/c1-19(2)12-13-20(17-6-4-5-11-18-17)14-15-7-9-16(21-3)10-8-15/h4-11H,12-14H2,1-3H3 | PDB
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| 1.18 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
University of North Carolina at Chapel Hill
Curated by PDSP Ki Database
| |
J Pharmacol Exp Ther 302: 328-36 (2002)
Article DOI: 10.1124/jpet.302.1.328
BindingDB Entry DOI: 10.7270/Q2JQ0ZK1 |
More data for this
Ligand-Target Pair | |
Histamine H1 receptor
(Cavia porcellus (domestic guinea pig)) | BDBM22567
(3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramin...)Show InChI InChI=1S/C17H23N3O/c1-19(2)12-13-20(17-6-4-5-11-18-17)14-15-7-9-16(21-3)10-8-15/h4-11H,12-14H2,1-3H3 | UniProtKB/SwissProt
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| 1.25 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Université Libre de Bruxelles
Curated by PDSP Ki Database
| |
Eur J Biochem 224: 489-95 (1994)
Article DOI: 10.1111/j.1432-1033.1994.00489.x
BindingDB Entry DOI: 10.7270/Q2H70DB4 |
More data for this
Ligand-Target Pair | |
Histamine H1 receptor
(Homo sapiens (Human)) | BDBM22567
(3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramin...)Show InChI InChI=1S/C17H23N3O/c1-19(2)12-13-20(17-6-4-5-11-18-17)14-15-7-9-16(21-3)10-8-15/h4-11H,12-14H2,1-3H3 | PDB
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| DrugBank
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| 1.30 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Vrije Universiteit Amsterdam
Curated by ChEMBL
| Assay Description
Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by m... |
J Med Chem 59: 9047-9061 (2016)
Article DOI: 10.1021/acs.jmedchem.6b00981
BindingDB Entry DOI: 10.7270/Q2G44S8Z |
More data for this
Ligand-Target Pair | |
Hrh3 protein
(RAT) | BDBM22542
(4-(1H-imidazol-4-ylmethyl)piperidine | 4-(1H-imida...)Show InChI InChI=1S/C9H15N3/c1-3-10-4-2-8(1)5-9-6-11-7-12-9/h6-8,10H,1-5H2,(H,11,12) | KEGG
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| 1.40 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
R. W. Johnson Pharmaceutical Research Institute
Curated by PDSP Ki Database
| |
J Pharmacol Exp Ther 293: 771-8 (2000)
BindingDB Entry DOI: 10.7270/Q2348HX8 |
More data for this
Ligand-Target Pair | |
Histamine H1 receptor
(Homo sapiens (Human)) | BDBM22567
(3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramin...)Show InChI InChI=1S/C17H23N3O/c1-19(2)12-13-20(17-6-4-5-11-18-17)14-15-7-9-16(21-3)10-8-15/h4-11H,12-14H2,1-3H3 | PDB
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| 1.60 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Broad Institute of MIT and Harvard
Curated by ChEMBL
| Assay Description
Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrs |
Bioorg Med Chem Lett 23: 1834-8 (2013)
Article DOI: 10.1016/j.bmcl.2013.01.025
BindingDB Entry DOI: 10.7270/Q2P55PWC |
More data for this
Ligand-Target Pair | |
Histamine H3 receptor
(Homo sapiens (Human)) | BDBM22542
(4-(1H-imidazol-4-ylmethyl)piperidine | 4-(1H-imida...)Show InChI InChI=1S/C9H15N3/c1-3-10-4-2-8(1)5-9-6-11-7-12-9/h6-8,10H,1-5H2,(H,11,12) | PDB
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| 1.60 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
R. W. Johnson Pharmaceutical Research Institute
Curated by PDSP Ki Database
| |
J Pharmacol Exp Ther 293: 771-8 (2000)
BindingDB Entry DOI: 10.7270/Q2348HX8 |
More data for this
Ligand-Target Pair | |
Histamine H1 receptor
(Homo sapiens (Human)) | BDBM22567
(3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramin...)Show InChI InChI=1S/C17H23N3O/c1-19(2)12-13-20(17-6-4-5-11-18-17)14-15-7-9-16(21-3)10-8-15/h4-11H,12-14H2,1-3H3 | PDB
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| 1.70 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Adamed Ltd.
Curated by ChEMBL
| Assay Description
Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells |
J Med Chem 57: 4543-57 (2014)
Article DOI: 10.1021/jm401895u
BindingDB Entry DOI: 10.7270/Q2N29ZHX |
More data for this
Ligand-Target Pair | |
Histamine H1 receptor
(Homo sapiens (Human)) | BDBM22567
(3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramin...)Show InChI InChI=1S/C17H23N3O/c1-19(2)12-13-20(17-6-4-5-11-18-17)14-15-7-9-16(21-3)10-8-15/h4-11H,12-14H2,1-3H3 | PDB
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| 1.70 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Jagiellonian University Collegium Medicum
Curated by ChEMBL
| Assay Description
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in HEK-293 cells |
Eur J Med Chem 92: 221-35 (2015)
Article DOI: 10.1016/j.ejmech.2014.12.045
BindingDB Entry DOI: 10.7270/Q2Q241XV |
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 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 H1 receptor
(Homo sapiens (Human)) | BDBM24226
(1-[(4-fluorophenyl)methyl]-N-{1-[2-(4-methoxypheny...)Show SMILES COc1ccc(CCN2CCC(CC2)Nc2nc3ccccc3n2Cc2ccc(F)cc2)cc1 Show InChI InChI=1S/C28H31FN4O/c1-34-25-12-8-21(9-13-25)14-17-32-18-15-24(16-19-32)30-28-31-26-4-2-3-5-27(26)33(28)20-22-6-10-23(29)11-7-22/h2-13,24H,14-20H2,1H3,(H,30,31) | PDB
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| 2.09 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
University of Regensburg
Curated by ChEMBL
| Assay Description
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting |
Bioorg Med Chem Lett 21: 6274-80 (2011)
Article DOI: 10.1016/j.bmcl.2011.09.001
BindingDB Entry DOI: 10.7270/Q28K7BB7 |
More data for this
Ligand-Target Pair | |
Histamine H1 receptor
(Homo sapiens (Human)) | BDBM22567
(3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramin...)Show InChI InChI=1S/C17H23N3O/c1-19(2)12-13-20(17-6-4-5-11-18-17)14-15-7-9-16(21-3)10-8-15/h4-11H,12-14H2,1-3H3 | PDB
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| 2.09 | 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]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting |
J Med Chem 54: 8195-206 (2011)
Article DOI: 10.1021/jm2011589
BindingDB Entry DOI: 10.7270/Q2QF8T85 |
More data for this
Ligand-Target Pair | |
Histamine H4 receptor
(Rattus norvegicus (rat)) | BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)Show InChI InChI=1S/C14H16ClN3O/c1-17-4-6-18(7-5-17)14(19)13-9-10-8-11(15)2-3-12(10)16-13/h2-3,8-9,16H,4-7H2,1H3 | KEGG
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| 2.40 | 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 of compound towards rat histamine H4 receptor |
J Med Chem 46: 3957-60 (2003)
Article DOI: 10.1021/jm0341047
BindingDB Entry DOI: 10.7270/Q2QJ7J1C |
More data for this
Ligand-Target Pair | |
Histamine H1 receptor
(Homo sapiens (Human)) | BDBM22567
(3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramin...)Show InChI InChI=1S/C17H23N3O/c1-19(2)12-13-20(17-6-4-5-11-18-17)14-15-7-9-16(21-3)10-8-15/h4-11H,12-14H2,1-3H3 | PDB
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| 2.5 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Mayo Foundation for Medical Education and Research and Mayo Clinic
Curated by PDSP Ki Database
| |
Life Sci 68: 29-39 (2000)
Article DOI: 10.1016/s0024-3205(00)00911-5
BindingDB Entry DOI: 10.7270/Q2057DHP |
More data for this
Ligand-Target Pair | |
Histamine H4 receptor
(Rattus norvegicus (rat)) | BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)Show InChI InChI=1S/C14H16ClN3O/c1-17-4-6-18(7-5-17)14(19)13-9-10-8-11(15)2-3-12(10)16-13/h2-3,8-9,16H,4-7H2,1H3 | KEGG
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| 2.60 | -11.7 | 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 H4 receptor
(Rattus norvegicus (rat)) | BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)Show InChI InChI=1S/C14H16ClN3O/c1-17-4-6-18(7-5-17)14(19)13-9-10-8-11(15)2-3-12(10)16-13/h2-3,8-9,16H,4-7H2,1H3 | KEGG
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| 2.70 | -11.7 | 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: 6547-57 (2008)
Article DOI: 10.1021/jm800670r
BindingDB Entry DOI: 10.7270/Q2KH0KM5 |
More data for this
Ligand-Target Pair | |
Histamine H4 receptor
(Rattus norvegicus (rat)) | BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)Show InChI InChI=1S/C14H16ClN3O/c1-17-4-6-18(7-5-17)14(19)13-9-10-8-11(15)2-3-12(10)16-13/h2-3,8-9,16H,4-7H2,1H3 | KEGG
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| 2.70 | -11.7 | 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 | |
Potassium voltage-gated channel subfamily H member 2
(Homo sapiens (Human)) | BDBM24226
(1-[(4-fluorophenyl)methyl]-N-{1-[2-(4-methoxypheny...)Show SMILES COc1ccc(CCN2CCC(CC2)Nc2nc3ccccc3n2Cc2ccc(F)cc2)cc1 Show InChI InChI=1S/C28H31FN4O/c1-34-25-12-8-21(9-13-25)14-17-32-18-15-24(16-19-32)30-28-31-26-4-2-3-5-27(26)33(28)20-22-6-10-23(29)11-7-22/h2-13,24H,14-20H2,1H3,(H,30,31) | PDB
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Article
PubMed
| 2.90 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Global Research and Development
Curated by ChEMBL
| Assay Description
Binding affinity at hERG expressed in HEK293 cells by fluorescence polarization assay |
J Med Chem 50: 2931-41 (2007)
Article DOI: 10.1021/jm0700565
BindingDB Entry DOI: 10.7270/Q2736RR2 |
More data for this
Ligand-Target Pair | |
Histamine H1 receptor
(Homo sapiens (Human)) | BDBM24226
(1-[(4-fluorophenyl)methyl]-N-{1-[2-(4-methoxypheny...)Show SMILES COc1ccc(CCN2CCC(CC2)Nc2nc3ccccc3n2Cc2ccc(F)cc2)cc1 Show InChI InChI=1S/C28H31FN4O/c1-34-25-12-8-21(9-13-25)14-17-32-18-15-24(16-19-32)30-28-31-26-4-2-3-5-27(26)33(28)20-22-6-10-23(29)11-7-22/h2-13,24H,14-20H2,1H3,(H,30,31) | PDB
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PubMed
| 3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Aventis Pharmaceuticals
Curated by ChEMBL
| Assay Description
Binding affinity towards histamine H1 receptor |
J Med Chem 46: 2017-22 (2003)
Article DOI: 10.1021/jm0205651
BindingDB Entry DOI: 10.7270/Q2XD12C8 |
More data for this
Ligand-Target Pair | |
Histamine H1 receptor
(Homo sapiens (Human)) | BDBM22890
(2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-...)Show SMILES OC(=O)COCCN1CCN(CC1)C(c1ccccc1)c1ccc(Cl)cc1 Show InChI InChI=1S/C21H25ClN2O3/c22-19-8-6-18(7-9-19)21(17-4-2-1-3-5-17)24-12-10-23(11-13-24)14-15-27-16-20(25)26/h1-9,21H,10-16H2,(H,25,26) | PDB
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PubMed
| 3.16 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
UCB S.A.
Curated by PDSP Ki Database
| |
Mol Pharmacol 61: 391-9 (2002)
Article DOI: 10.1124/mol.61.2.391
BindingDB Entry DOI: 10.7270/Q2D50KJ8 |
More data for this
Ligand-Target Pair | |
Histamine H4 receptor
(Rattus norvegicus (rat)) | BDBM26226
((12S,17S)-6-(piperazin-1-yl)-11-oxa-3,5-diazatetra...)Show SMILES [H][C@]12CCCC[C@@]1([H])C1=C(CCc3c(nc(N)nc13)N1CCNCC1)O2 |r,t:9| Show InChI InChI=1S/C18H25N5O/c19-18-21-16-12(17(22-18)23-9-7-20-8-10-23)5-6-14-15(16)11-3-1-2-4-13(11)24-14/h11,13,20H,1-10H2,(H2,19,21,22)/t11-,13+/m1/s1 | KEGG
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| Article
PubMed
| 3.40 | -11.5 | 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 H1 receptor
(Homo sapiens (Human)) | BDBM22567
(3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramin...)Show InChI InChI=1S/C17H23N3O/c1-19(2)12-13-20(17-6-4-5-11-18-17)14-15-7-9-16(21-3)10-8-15/h4-11H,12-14H2,1-3H3 | PDB
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| 3.70 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Universite Libre de Bruxelles
Curated by PDSP Ki Database
| |
J Recept Signal Transduct Res 15: 91-102 (1995)
Article DOI: 10.3109/10799899509045210
BindingDB Entry DOI: 10.7270/Q2PZ57BR |
More data for this
Ligand-Target Pair | |
Histamine H4 receptor
(Mus musculus (mouse)) | BDBM22566
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)Show InChI InChI=1S/C14H16ClN3O/c1-17-4-6-18(7-5-17)14(19)13-9-10-8-11(15)2-3-12(10)16-13/h2-3,8-9,16H,4-7H2,1H3 | Reactome pathway
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| Article
PubMed
| 3.89 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Inc.
Curated by ChEMBL
| Assay Description
Displacement of [3H]-histamine from mouse H4R expressed in HEK293T cells |
Bioorg Med Chem Lett 21: 6596-602 (2011)
Article DOI: 10.1016/j.bmcl.2011.07.125
BindingDB Entry DOI: 10.7270/Q20C4W6C |
More data for this
Ligand-Target Pair | |
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