BindingDB BDBM7966 2-(1H-imidazol-4-yl)ethan-1-amine::CHEMBL544208::CHEMBL90::Ceplene::Ergotidine::HISTAMINE DIHYDROCHLORIDE::Histamine::L-histamine::Peremin::[3H]histamine

BDBM7966 2-(1H-imidazol-4-yl)ethan-1-amine::CHEMBL544208::CHEMBL90::Ceplene::Ergotidine::HISTAMINE DIHYDROCHLORIDE::Histamine::L-histamine::Peremin::[3H]histamine

SMILES NCCc1cnc[nH]1

InChI Key InChIKey=NTYJJOPFIAHURM-UHFFFAOYSA-N

Data 78 KI 1 IC50 2 Kd 36 EC50

PDB links: 8 PDB IDs match this monomer.

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 24 hits for monomerid = 7966

Histamine H2 receptor(Cavia porcellus (domestic guinea pig))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 1.00E+3nMAssay Description:Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rateMore data for this Ligand-Target Pair

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Histamine H2 receptor(Cavia porcellus (domestic guinea pig))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 1.20E+3nMAssay Description:Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayMore data for this Ligand-Target Pair

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Histamine H2 receptor(Homo sapiens (Human))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 1.26E+3nMAssay Description:Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayMore data for this Ligand-Target Pair

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Histamine H1 receptor(Homo sapiens (Human))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 190nMAssay Description:Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayMore data for this Ligand-Target Pair

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Histamine H2 receptor(Homo sapiens (Human))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 1.20E+3nMAssay Description:Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayMore data for this Ligand-Target Pair

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Histamine H2 receptor(Cavia porcellus (domestic guinea pig))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 1.20E+3nMAssay Description:Activity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayMore data for this Ligand-Target Pair

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Histamine H3 receptor(Homo sapiens (Human))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 25.1nMAssay Description:Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase act...More data for this Ligand-Target Pair

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Histamine H4 receptor(Homo sapiens (Human))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 11.6nMAssay 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...More data for this Ligand-Target Pair

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Histamine H2 receptor(Cavia porcellus (domestic guinea pig))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 1.00E+3nMAssay Description:Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activityMore data for this Ligand-Target Pair

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Histamine H1 receptor(Homo sapiens (Human))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 191nMAssay Description:Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assayMore data for this Ligand-Target Pair

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Histamine H2 receptor(Homo sapiens (Human))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 1.20E+3nMAssay Description:Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayMore data for this Ligand-Target Pair

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Histamine H3 receptor(Homo sapiens (Human))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 25.1nMAssay Description:Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-sta...More data for this Ligand-Target Pair

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Histamine H4 receptor(Homo sapiens (Human))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 12.0nMAssay Description:Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayMore data for this Ligand-Target Pair

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Histamine H2 receptor(Cavia porcellus (domestic guinea pig))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 1.00E+3nMAssay Description:Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atriumMore data for this Ligand-Target Pair

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Histamine H2 receptor(Homo sapiens (Human))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 1.26E+3nMAssay Description:Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayMore data for this Ligand-Target Pair

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Histamine H2 receptor(Cavia porcellus (domestic guinea pig))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 1.20E+3nMAssay Description:Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayMore data for this Ligand-Target Pair

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Histamine H1 receptor(Homo sapiens (Human))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 191nMAssay Description:Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assayMore data for this Ligand-Target Pair

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Histamine H3 receptor(Homo sapiens (Human))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 12.9nMAssay Description:Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activit...More data for this Ligand-Target Pair

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Histamine H1 receptor(Homo sapiens (Human))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 191nMAssay Description:Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation coun...More data for this Ligand-Target Pair

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Histamine H2 receptor(Cavia porcellus (domestic guinea pig))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 1.00E+3nMAssay Description:Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rateMore data for this Ligand-Target Pair

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Histamine H2 receptor(Homo sapiens (Human))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 1.20E+3nMAssay Description:Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid...More data for this Ligand-Target Pair

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Histamine H4 receptor(Homo sapiens (Human))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 12nMAssay Description:Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[3...More data for this Ligand-Target Pair

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Histamine H3 receptor(Homo sapiens (Human))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 25nMAssay Description:Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding b...More data for this Ligand-Target Pair

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Histamine H4 receptor(Homo sapiens (Human))
University Of Regensburg

Curated by ChEMBL

PNG

BDBM7966(2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 |...)

EC50: 9.12nMAssay Description:Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activ...More data for this Ligand-Target Pair

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Filter my 117 hits

Targets 15▿
- Histamine H1 receptor 26
- Histamine H2 receptor 22
- Histamine H3 receptor 21
- Histamine H4 receptor 19
- Hrh3 protein 13
- 5-hydroxytryptamine receptor 7 4
- Solute carrier family 22 member 1 2
- Solute carrier family 22 member 2 2
- Histamine receptor H4 2
- Solute carrier family 22 member 3 1
- Glutaminyl-peptide cyclotransferase 1
- D(2) dopamine receptor 1
- Nischarin 1
- D(1A) dopamine receptor 1
- Trace amine-associated receptor 1 1
- ...
Publications 50▿
- Eur J Pharmacol 487: 183-97 (2004) 7
- J Med Chem 51: 7193-204 (2009) 6
- Bioorg Med Chem Lett 20: 3173-6 (2010) 6
- J Med Chem 52: 2623-7 (2009) 5
- J Med Chem 54: 1693-703 (2011) 4
- J Pharmacol Exp Ther 302: 328-36 (2002) 4
- Mol Pharmacol 59: 434-41 (2001) 4
- J Med Chem 49: 5587-96 (2006) 4
- J Pharmacol Exp Ther 317: 1262-8 (2006) 4
- Eur J Pharmacol 311: 305-10 (1996) 4
- J Med Chem 52: 6297-313 (2009) 4
- J Med Chem 46: 1980-8 (2003) 4
- Mol Pharmacol 56: 1-10 (1999) 3
- J Pharmacol Exp Ther 293: 771-8 (2000) 3
- J Med Chem 55: 1147-60 (2012) 3
- Biochem Soc Trans 20: 122-5 (1992) 3
- J Pharmacol Exp Ther 271: 452-9 (1994) 3
- J Pharmacol Exp Ther 314: 1310-21 (2005) 2
- Mol Pharmacol 59: 420-6 (2001) 2
- Life Sci 35: 1885-93 (1984) 2
- Pharm Res 18: 1528-34 (2001) 2
- Invest Radiol -2 (1988) 2
- J Pharmacol Exp Ther 305: 1104-15 (2003) 2
- J Med Chem 53: 3840-4 (2010) 2
- J Biol Chem 268: 18200-4 (1993) 2
- J Med Chem 54: 8136-47 (2011) 2
- Eur J Biochem 224: 489-95 (1994) 2
- J Pharmacol Exp Ther 285: 170-7 (1998) 1
- Nat Chem Biol 1: 98-103 (2006) 1
- Mol Pharmacol 61: 391-9 (2002) 1
- Proc Natl Acad Sci U S A 90: 8547-51 (1993) 1
- Bioorg Med Chem Lett 20: 3367-71 (2010) 1
- J Recept Signal Transduct Res 15: 91-102 (1995) 1
- Bioorg Med Chem Lett 2: 1231-1234 (1992) 1
- J Biol Chem 278: 49773-9 (2003) 1
- J Neurochem 55: 1612-6 (1990) 1
- J Med Chem 35: 3239-46 (1992) 1
- Eur J Pharmacol 245: 291-5 (1993) 1
- Proc Natl Acad Sci U S A 75: 6290-4 (1978) 1
- J Med Chem 46: 5812-24 (2003) 1
- Mol Pharmacol 55: 1101-7 (1999) 1
- Nature 304: 65-7 (1983) 1
- Brain Res 304: 1-7 (1984) 1
- J Biol Chem 268: 23422-6 (1993) 1
- Bioorg Med Chem Lett 22: 461-7 (2011) 1
- J Pharmacol Exp Ther 311: 274-81 (2004) 1
- J Med Chem 51: 3145-53 (2008) 1
- Bioorg Med Chem Lett 4: 1913-1916 (1994) 1
- Mol Pharmacol 59: 427-33 (2001) 1
- J Med Chem 53: 2390-400 (2010) 1
- ...
Institutions 35▿
- University Of Regensburg 24
- Hokkaido University 8
- Abbott Laboratories 7
- Vu University Amsterdam 6
- University of Kansas 6
- University of North Carolina At Chapel Hill 5
- Smithkline Beecham Pharmaceuticals 4
- U. 109 4
- Glaxo Research & Development 4
- R. W. Johnson Pharmaceutical Research Institute 4
- Vrije Universiteit Amsterdam 4
- Queen'S Medical Centre 3
- TBA 3
- University Of Heidelberg 3
- Schering-Plough 2
- Kyoto University Hospital 2
- National Institute of Neurological Disorders and Stroke 2
- UniversitÉ 2
- The R. W. Johnson Pharmaceutical Research Institute 2
- UnitÉ 2
- Meiji Seika Kaisha 2
- Griffin Discoveries 2
- Vrije Universiteit 1
- University of Bonn 1
- Universite Libre De Bruxelles 1
- Synaptic Pharmaceutical 1
- Gedeon Richter 1
- The Centre For Addiction and Mental Health 1
- Schering-Plough Research Institute 1
- Probiodrug 1
- Mayo Foundation 1
- Johnson & Johnson Pharmaceutical Research & Development 1
- Ucb Pharma 1
- Hoechst Pharmaceutical Research Laboratories 1
- University of Cambridge 1
- ...
Affinity: 0.14 to 1.4E+6 nM▿
- Ki 78
- IC50 1
- Kd 2
- EC50 36
- Affinity ≤ nM
Xtal structures: 0
Docked structures: 1
Catalog Cmpds: 1