Found 19 hits Enz. Inhib. hit(s) with Target = 'Histamine H4 receptor' and Ligand = 'BDBM7966' 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 H4 receptor
(Homo sapiens (Human)) | BDBM7966
(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)Show InChI InChI=1S/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8) | PDB
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| 2.5 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
SmithKline Beecham Pharmaceuticals
Curated by PDSP Ki Database
| |
Mol Pharmacol 59: 434-41 (2001)
Article DOI: 10.1124/mol.59.3.434 BindingDB Entry DOI: 10.7270/Q2Z899ZR |
More data for this Ligand-Target Pair | |
Histamine H4 receptor
(Homo sapiens (Human)) | BDBM7966
(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)Show InChI InChI=1S/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8) | PDB
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| 8.10 | 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 H4 receptor
(Homo sapiens (Human)) | BDBM7966
(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)Show InChI InChI=1S/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8) | PDB
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| 9 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Griffin Discoveries BV
Curated by ChEMBL
| Assay Description Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes |
Bioorg Med Chem Lett 22: 461-7 (2011)
Article DOI: 10.1016/j.bmcl.2011.10.104 BindingDB Entry DOI: 10.7270/Q2D79BT2 |
More data for this Ligand-Target Pair | |
Histamine H4 receptor
(Homo sapiens (Human)) | BDBM7966
(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)Show InChI InChI=1S/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8) | PDB
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| 12.0 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Griffin Discoveries BV
Curated by ChEMBL
| Assay Description Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells |
J Med Chem 53: 2390-400 (2010)
Article DOI: 10.1021/jm901379s BindingDB Entry DOI: 10.7270/Q2G44RJ4 |
More data for this Ligand-Target Pair | |
Histamine H4 receptor
(Homo sapiens (Human)) | BDBM7966
(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)Show InChI InChI=1S/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8) | PDB
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| 12.0 | 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 histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting |
J Med Chem 54: 1693-703 (2011)
Article DOI: 10.1021/jm1013488 BindingDB Entry DOI: 10.7270/Q20G3MDD |
More data for this Ligand-Target Pair | |
Histamine H4 receptor
(Homo sapiens (Human)) | BDBM7966
(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)Show InChI InChI=1S/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8) | PDB
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| 13.4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Gedeon Richter Plc
Curated by ChEMBL
| Assay Description Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells |
J Med Chem 51: 3145-53 (2008)
Article DOI: 10.1021/jm7014777 BindingDB Entry DOI: 10.7270/Q2M046BP |
More data for this Ligand-Target Pair | |
Histamine H4 receptor
(Homo sapiens (Human)) | BDBM7966
(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)Show InChI InChI=1S/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8) | PDB
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| 15.8 | 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 H4 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 H4 receptor
(Homo sapiens (Human)) | BDBM7966
(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)Show InChI InChI=1S/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8) | PDB
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| 16 | -46.3 | n/a | n/a | n/a | n/a | n/a | 7.4 | 37 |
Vrije Universiteit Amsterdam
| Assay Description Ligand displacement assays were performed on The SK-N-MC/hH4R 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 H4 receptor
(Homo sapiens (Human)) | BDBM7966
(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)Show InChI InChI=1S/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8) | PDB
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| 17 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
SmithKline Beecham Pharmaceuticals
Curated by PDSP Ki Database
| |
Mol Pharmacol 59: 434-41 (2001)
Article DOI: 10.1124/mol.59.3.434 BindingDB Entry DOI: 10.7270/Q2Z899ZR |
More data for this Ligand-Target Pair | |
Histamine H4 receptor
(Homo sapiens (Human)) | BDBM7966
(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)Show InChI InChI=1S/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8) | PDB
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| 39.8 | 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 H4 receptor
(Homo sapiens (Human)) | BDBM7966
(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)Show InChI InChI=1S/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8) | PDB
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| 60 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Johnson& Johnson Pharmaceutical Research& Development
Curated by ChEMBL
| Assay Description Displacement of [3H]histamine from human recombinant histamine H4 receptor |
Bioorg Med Chem Lett 20: 3367-71 (2010)
Article DOI: 10.1016/j.bmcl.2010.04.017 BindingDB Entry DOI: 10.7270/Q23J3D4Z |
More data for this Ligand-Target Pair | |
Histamine H4 receptor
(Homo sapiens (Human)) | BDBM7966
(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)Show InChI InChI=1S/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8) | PDB
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| 3.44E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
The Centre for Addiction and Mental Health
Curated by PDSP Ki Database
| |
Mol Pharmacol 59: 427-33 (2001)
Article DOI: 10.1124/mol.59.3.427 BindingDB Entry DOI: 10.7270/Q22Z1438 |
More data for this Ligand-Target Pair | |
Histamine H4 receptor
(Homo sapiens (Human)) | BDBM7966
(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)Show InChI InChI=1S/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8) | PDB
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| n/a | n/a | n/a | n/a | 12.0 | n/a | n/a | n/a | n/a |
University of Regensburg
Curated by ChEMBL
| Assay Description Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay |
J Med Chem 52: 6297-313 (2009)
Article DOI: 10.1021/jm900526h BindingDB Entry DOI: 10.7270/Q2PN96VG |
More data for this Ligand-Target Pair | |
Histamine H4 receptor
(Homo sapiens (Human)) | BDBM7966
(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)Show InChI InChI=1S/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8) | PDB
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| DrugBank Article PubMed
| n/a | n/a | n/a | n/a | 11.6 | n/a | n/a | n/a | n/a |
University of Regensburg
Curated by ChEMBL
| Assay Description Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-s... |
J Med Chem 51: 7193-204 (2009)
Article DOI: 10.1021/jm800841w BindingDB Entry DOI: 10.7270/Q2RN38T6 |
More data for this Ligand-Target Pair | |
Histamine H4 receptor
(Homo sapiens (Human)) | BDBM7966
(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)Show InChI InChI=1S/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8) | PDB
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| DrugBank Article PubMed
| n/a | n/a | n/a | n/a | 1.80E+3 | n/a | n/a | n/a | n/a |
Hokkaido University
Curated by ChEMBL
| Assay Description Agonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assay |
J Med Chem 49: 5587-96 (2006)
Article DOI: 10.1021/jm0603318 BindingDB Entry DOI: 10.7270/Q2MW2GRK |
More data for this Ligand-Target Pair | |
Histamine H4 receptor
(Homo sapiens (Human)) | BDBM7966
(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)Show InChI InChI=1S/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8) | PDB
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| DrugBank Article PubMed
| n/a | n/a | n/a | n/a | 75 | n/a | n/a | n/a | n/a |
Hokkaido University
Curated by ChEMBL
| Assay Description Inhibition of human Histamine H4 receptor |
J Med Chem 46: 1980-8 (2003)
Article DOI: 10.1021/jm020415q BindingDB Entry DOI: 10.7270/Q2XG9QG6 |
More data for this Ligand-Target Pair | |
Histamine H4 receptor
(Homo sapiens (Human)) | BDBM7966
(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)Show InChI InChI=1S/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8) | PDB
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| DrugBank Article PubMed
| n/a | n/a | n/a | n/a | 12 | n/a | n/a | n/a | n/a |
University of Regensburg
Curated by ChEMBL
| Assay Description Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[3... |
J Med Chem 52: 2623-7 (2009)
Article DOI: 10.1021/jm9000693 BindingDB Entry DOI: 10.7270/Q2P270BN |
More data for this Ligand-Target Pair | |
Histamine H4 receptor
(Homo sapiens (Human)) | BDBM7966
(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)Show InChI InChI=1S/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8) | PDB
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| DrugBank Article PubMed
| n/a | n/a | n/a | n/a | 9.12 | n/a | n/a | n/a | n/a |
University of Regensburg
Curated by ChEMBL
| Assay Description Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activ... |
Bioorg Med Chem Lett 20: 3173-6 (2010)
Article DOI: 10.1016/j.bmcl.2010.03.082 BindingDB Entry DOI: 10.7270/Q2RF5W9M |
More data for this Ligand-Target Pair | |
Histamine H4 receptor
(Homo sapiens (Human)) | BDBM7966
(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)Show InChI InChI=1S/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8) | PDB
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| DrugBank Article PubMed
| n/a | n/a | n/a | n/a | 25.1 | n/a | n/a | n/a | n/a |
VU University Amsterdam
Curated by ChEMBL
| Assay Description Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferas... |
J Med Chem 54: 1693-703 (2011)
Article DOI: 10.1021/jm1013488 BindingDB Entry DOI: 10.7270/Q20G3MDD |
More data for this Ligand-Target Pair | |