Target Validation Information
Target ID T64765
Target Name Histamine H3 receptor
Target Type
Clinical Trial
Drug Potency against Target Aerophobin-1 Drug Info IC50 = 9000 nM
Des-bromoaplysamine-1 Drug Info Ki = 89 nM [527879]
(R)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline Drug Info Ki = 41 nM [530904]
2-(2-(4-tert-Butylphenylthio)ethyl)-1H-imidazole Drug Info Ki = 0.43 nM [531088]
3-((1H-imidazol-4-yl)methyl)pyridine Drug Info Ki = 76 nM [531088]
2-((1H-imidazol-4-yl)methyl)pyridine Drug Info Ki = 1800 nM [531088]
2-(1,4'-bipiperidin-1'-yl)thiazolo[4,5-b]pyridine Drug Info Ki = 139 nM [530397]
2-(1,4'-bipiperidin-1'-yl)thiazolo[4,5-c]pyridine Drug Info Ki = 128 nM [530397]
4-((1H-imidazol-4-yl)methyl)-1-heptylpiperidine Drug Info Ki = 2 nM [527818]
VERONGAMINE Drug Info IC50 = 500 nM
5-phenyl-2-(4-(piperidin-1-yl)butyl)oxazole Drug Info Ki = 63 nM [531116]
(R)-3-(1H-imidazol-4-yl)propyl sec-butylcarbamate Drug Info Ki = 19 nM [530465]
(S)-3-(1H-imidazol-4-yl)propyl sec-butylcarbamate Drug Info Ki = 23 nM [530465]
4-((2S,3R)-2-Methyl-pyrrolidin-3-yl)-1H-imidazole Drug Info Ki = 33 nM [533720]
1-(3-methoxyphenethyl)pyrrolidine Drug Info Ki = 260 nM [529212]
2-(4-Cyclopropyl-piperazin-1-yl)-quinoline Drug Info Ki = 13 nM [527370]
2-(4-Cyclopentyl-piperazin-1-yl)-quinoline Drug Info Ki = 28 nM [527370]
2-(4-Methyl-piperazin-1-yl)-quinoline Drug Info Ki = 410 nM [527370]
4-[3-(4-Butyl-phenoxy)-propyl]-1H-imidazole Drug Info Ki = 60 nM [525896]
4-[3-(4-Ethynyl-phenoxy)-propyl]-1H-imidazole Drug Info Ki = 2.3 nM [525896]
N-benzyl-4-cyclopentylpiperazine-1-carboxamide Drug Info Ki = 94 nM [528367]
CONESSINE Drug Info Ki = 24.5 nM [530254]
2-((2-ethoxyphenoxy)methyl)-4-isopropylmorpholine Drug Info Ki = 9000 nM [529751]
4-isopropyl-2-(phenoxymethyl)morpholine Drug Info Ki = 4800 nM [529751]
(S)-2-(2-(2-methylpyrrolidin-1-yl)ethyl)phenol Drug Info Ki = 220 nM [529212]
ST-1025 Drug Info Ki = 11.2 nM [531116]
2-(2-(pyrrolidin-1-yl)ethyl)phenol Drug Info Ki = 340 nM [529212]
4-(3-Phenoxy-propyl)-1H-imidazole Drug Info Ki = 4.9 nM [526023]
4-(2-(3,4-Dimethylphenylamino)ethyl)-1H-imidazole Drug Info Ki = 9.9 nM [530846]
Cipralisant Drug Info Ki = 5.25 nM [552481]
CARCININE Drug Info Ki = 294 nM [529632]
APLYSAMINE Drug Info IC50 = 500 nM [529632]
4-(6-Cyclopentyl-hex-3-ynyl)-1H-imidazole Drug Info Ki = 0.95 nM [534790]
(1H-indol-2-yl)(piperazin-1-yl)methanone Drug Info Ki = 9000 nM [527934]
GT-2016 Drug Info Ki = 40 nM [534790]
JNJ-28583867 Drug Info Ki = 10.6 nM [529199]
ST-1093 Drug Info Ki = 20 nM [531116]
N-methyl-2-(pyridin-2-yl)ethanamine Drug Info Ki = 2030 nM [530151]
2-(ethoxycarbonyl)-1H-indole-5-carboxylic acid Drug Info Ki = 7 nM [530151]
1-(3-(4-(fluoromethyl)phenoxy)propyl)piperidine Drug Info Ki = 17.3 nM [530019]
1-(3-(4-(2-fluoroethyl)phenoxy)propyl)piperidine Drug Info Ki = 43 nM [530019]
UCL-2138 Drug Info Ki = 11 nM [530019]
(1R,2S)-2-(1H-Imidazol-4-yl)-1-methyl-propylamine Drug Info Ki = 0.8 nM [533720]
(1R,2R)-2-(1H-Imidazol-4-yl)-1-methyl-propylamine Drug Info Ki = 11 nM [533720]
4-((1H-Imidazol-4-yl)methyl)-1-phenylpiperidine Drug Info Ki = 30 nM
4-(2-(4-tert-Butylphenylamino)ethyl)-1H-imidazole Drug Info Ki = 0.89 nM [530846]
4-(2-(4-Cyclohexylphenylamino)ethyl)-1H-imidazole Drug Info Ki = 4.1 nM [530846]
4-(2-(Cyclohexylamino)ethyl)-1H-imidazole Drug Info Ki = 1600 nM [530846]
IODOPROXYFAN Drug Info Ki = 71 nM [526023]
4-[3-(4-Methoxy-phenoxy)-propyl]-1H-imidazole Drug Info Ki = 7.9 nM [526023]
ABT-239 Drug Info Ki = 0.45 nM [552941]
1-(4-nitrophenethyl)pyrrolidine Drug Info Ki = 360 nM [529212]
5-(2-(pyrrolidin-1-yl)ethyl)isothiazole Drug Info Ki = 190 nM [529212]
1-(2-(naphthalen-2-yl)ethyl)pyrrolidine Drug Info Ki = 30 nM [529212]
1-(4-methoxyphenethyl)pyrrolidine Drug Info Ki = 370 nM [529212]
2-(2-(pyrrolidin-1-yl)ethyl)-1H-indole Drug Info Ki = 219 nM [529212]
(S)-1-(4-nitrophenethyl)-2-methylpyrrolidine Drug Info Ki = 260 nM [529212]
4-((2R,3S)-2-Methyl-pyrrolidin-3-yl)-1H-imidazole Drug Info Ki = 8.7 nM [533720]
4-(2-(Phenylamino)ethyl)-1H-imidazole Drug Info Ki = 56 nM [530846]
4-(2-(4-Methylphenylamino)ethyl)-1H-imidazole Drug Info Ki = 14 nM [530846]
(1S,2S)-2-(1H-Imidazol-4-yl)-cyclopentylamine Drug Info Ki = 740 nM [533720]
2-(3-Methyl-3H-imidazol-4-yl)-ethylamine Drug Info Ki = 1 nM [534790]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [531079]
1-(3-(2-(3-methoxyphenoxy)ethoxy)propyl)azepane Drug Info Ki = 62 nM [530044]
4-Butyl-1-[3-(phenylpropoxy)propyl]piperidine Drug Info Ki = 274 nM [529673]
1-(3-(3-phenylpropoxy)propyl)piperidine Drug Info Ki = 3.1 nM [529673]
4-Benzyl-1-[3-phenylpropoxy)propyl]piperidine Drug Info Ki = 326 nM [529673]
VUF-5296 Drug Info Ki = 42.2 nM [526614]
4-Hept-3-ynyl-1H-imidazole Drug Info Ki = 27 nM [534790]
A-317920 Drug Info Ki = 12 nM [529586]
VUF-5297 Drug Info Ki = 4.3 nM [526614]
4-(8-Phenyl-oct-3-ynyl)-1H-imidazole Drug Info Ki = 3.5 nM [534790]
GSK189254A Drug Info Ki = 0.26 nM [531215]
Pitolisant Drug Info Ki = 0.16 nM [530044]
4-(4-Phenyl-butyl)-1H-imidazole Drug Info Ki = 12 nM [526023]
4-(6-Cyclohexyl-hex-3-ynyl)-1H-imidazole Drug Info Ki = 2.9 nM [534790]
4-(7-Methyl-oct-3-ynyl)-1H-imidazole Drug Info Ki = 3.7 nM [534790]
(S)-1-(3-methoxyphenethyl)-2-methylpyrrolidine Drug Info Ki = 170 nM [529212]
(S)-1-(4-methoxyphenethyl)-2-methylpyrrolidine Drug Info Ki = 63 nM [529212]
(R)-2-(2-(2-methylpyrrolidin-1-yl)ethyl)phenol Drug Info Ki = 240 nM [529212]
1-(2-p-tolyl-ethyl)-pyrrolidine Drug Info Ki = 81 nM [529212]
1-(2-m-tolyl-ethyl)-pyrrolidine Drug Info Ki = 200 nM [529212]
5-methoxy-2-(2-(pyrrolidin-1-yl)ethyl)-1H-indole Drug Info Ki = 230 nM [529212]
(S)-2-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine Drug Info Ki = 340 nM [529212]
4-(7,7-Dimethyl-oct-3-ynyl)-1H-imidazole Drug Info Ki = 0.8 nM [534790]
(S)-4-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine Drug Info Ki = 140 nM [529212]
(R)-3-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine Drug Info Ki = 320 nM [529212]
4-(2-(pyrrolidin-1-yl)ethyl)pyridine Drug Info Ki = 320 nM [529212]
2-(4-Isopropyl-piperazin-1-yl)-quinoline Drug Info Ki = 6.8 nM [527370]
(R)-1-(4-methoxyphenethyl)-2-methylpyrrolidine Drug Info Ki = 12 nM [529212]
(R)-2-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine Drug Info Ki = 200 nM [529212]
(R)-1-(2-methoxyphenethyl)-2-methylpyrrolidine Drug Info Ki = 110 nM [529212]
4-Hex-3-ynyl-1H-imidazole Drug Info Ki = 79 nM [534790]
GR-175737 Drug Info Ki = 7 nM [534790]
4-(2-(4-Methoxyphenylamino)ethyl)-1H-imidazole Drug Info Ki = 24 nM [530846]
2-(4-Propyl-piperazin-1-yl)-quinoline Drug Info Ki = 6 nM [527370]
2-[4-(1-Ethyl-propyl)-piperazin-1-yl]-quinoline Drug Info Ki = 2.9 nM [527370]
1-(4-(benzyloxy)phenethyl)pyrrolidine Drug Info Ki = 40 nM [529212]
(R)-1-(3-methoxyphenethyl)-2-methylpyrrolidine Drug Info Ki = 160 nM [529212]
(S)-1-(2-methoxyphenethyl)-2-methylpyrrolidine Drug Info Ki = 240 nM [529212]
(S)-2-methyl-1-(2-m-tolyl-ethyl)-pyrrolidine Drug Info Ki = 240 nM [529212]
1-[2-(2,4,6-trimethyl-phenyl)-ethyl]-pyrrolidine Drug Info Ki = 230 nM [529212]
1-(2-methoxyphenethyl)pyrrolidine Drug Info Ki = 260 nM [529212]
(R)-2-methyl-1-(2-m-tolyl-ethyl)-pyrrolidine Drug Info Ki = 30 nM [529212]
4-Propyl-1-[3-(phenylpropoxy)propyl]piperidine Drug Info Ki = 249 nM [529673]
4-(2-(3-tert-Butylphenylamino)ethyl)-1H-imidazole Drug Info Ki = 2.2 nM [530846]
2-(2-(pyrrolidin-1-yl)ethyl)pyridine Drug Info Ki = 320 nM [529212]
(R)-4-(2-(2-methylpyrrolidin-1-yl)ethyl)pyridine Drug Info Ki = 320 nM [529212]
5-ethyl-2-(2-(pyrrolidin-1-yl)ethyl)pyridine Drug Info Ki = 160 nM [529212]
(R)-2-methyl-1-(2-p-tolyl-ethyl)-pyrrolidine Drug Info Ki = 37 nM [529212]
(S)-2-methyl-1-(2-p-tolyl-ethyl)-pyrrolidine Drug Info Ki = 330 nM [529212]
(R)-1-(4-nitrophenethyl)-2-methylpyrrolidine Drug Info Ki = 280 nM [529212]
Action against Disease Model Cipralisant GT-2331 demonstrated full agonism relative to (R)-alpha-methylhistamine in cAMP assays. In [35S]GTPgammaS binding assays, GT-2331 demonstrated partial agonism. Imetit showed full agonism in most assays, but it was slightly less efficacious in a neurotransmitter release assay and in [35S]GTPgammaS binding at the h uMan H3 receptor. To further examine these ligands, we coexpressed G alpha16 or chimeric G alpha q/i5 in h uMan embryonic kidney cells expressing the h uMan H3 receptor and assayed intracellular calci uM and cAMP levels. GT-2331 demonstrated full agonism in all assays of cAMP activity. However, in cells expressing G alpha16, they exhibited minimal agonism in calci uM mobilization assays, whereas imetit showed partial agonism. When G alpha q/i5 was used, the activity of both GT-2331 and proxyfan increased, whereas imetit became a full agonist [536066] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations The H3-/- mice showed a decrease in overall locomotion, wheel-running behavior, and body temperature during the dark phase but maintained normal circadian rhythmicity. H3-/- mice were insensitive to the wake-promoting effects of the H3 receptor antagonist thioperamide. H3 receptor-deficient mouse represents a valuable model for studying histaminergic regulation of a variety of behaviors and neurotransmitter systems, including dopamine and acetylcholine. [536066]
References
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Ref 533720J Med Chem. 1995 May 12;38(10):1593-9.A novel pyrrolidine analog of histamine as a potent, highly selective histamine H3 receptor agonist.
Ref 534790Bioorg Med Chem Lett. 1998 May 19;8(10):1133-8.New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine.
Ref 531079J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
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Ref 529673Bioorg Med Chem. 2008 Sep 15;16(18):8729-36. Epub 2008 Jul 29.Piperidine variations in search for non-imidazole histamine H(3) receptor ligands.
Ref 529673Bioorg Med Chem. 2008 Sep 15;16(18):8729-36. Epub 2008 Jul 29.Piperidine variations in search for non-imidazole histamine H(3) receptor ligands.
Ref 526614J Med Chem. 2003 May 8;46(10):1980-8.Cyclopropane-based conformational restriction of histamine. (1S,2S)-2-(2-aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a highly selective agonist for the histamine H3 receptor, having a cis-cyclopropane structure.
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Ref 534790Bioorg Med Chem Lett. 1998 May 19;8(10):1133-8.New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine.
Ref 531215J Med Chem. 2010 Nov 11;53(21):7869-73.Diaryldiamines with dual inhibition of the histamine H(3) receptor and the norepinephrine transporter and the efficacy of 4-(3-(methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in pain.
Ref 530044Bioorg Med Chem. 2009 Apr 15;17(8):3037-42. Epub 2009 Mar 14.Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands.
Ref 526023Bioorg Med Chem Lett. 2001 Apr 9;11(7):951-4.Different antagonist binding properties of human and rat histamine H3 receptors.
Ref 534790Bioorg Med Chem Lett. 1998 May 19;8(10):1133-8.New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine.
Ref 534790Bioorg Med Chem Lett. 1998 May 19;8(10):1133-8.New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 534790Bioorg Med Chem Lett. 1998 May 19;8(10):1133-8.New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 527370J Med Chem. 2005 Jan 13;48(1):306-11.2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 534790Bioorg Med Chem Lett. 1998 May 19;8(10):1133-8.New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine.
Ref 534790Bioorg Med Chem Lett. 1998 May 19;8(10):1133-8.New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine.
Ref 530846J Med Chem. 2010 May 13;53(9):3840-4.Role of hydrophobic substituents on the terminal nitrogen of histamine in receptor binding and agonist activity: development of an orally active histamine type 3 receptor agonist and evaluation of its antistress activity in mice.
Ref 527370J Med Chem. 2005 Jan 13;48(1):306-11.2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists.
Ref 527370J Med Chem. 2005 Jan 13;48(1):306-11.2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 529673Bioorg Med Chem. 2008 Sep 15;16(18):8729-36. Epub 2008 Jul 29.Piperidine variations in search for non-imidazole histamine H(3) receptor ligands.
Ref 530846J Med Chem. 2010 May 13;53(9):3840-4.Role of hydrophobic substituents on the terminal nitrogen of histamine in receptor binding and agonist activity: development of an orally active histamine type 3 receptor agonist and evaluation of its antistress activity in mice.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Ref 529212Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.

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