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Histamine H3 receptor Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
ThioperamideIC5016.0 [1], 120.0 [2], 517.5 [3]
1-[4-(3-Piperidinopropoxy)benzyl]piperidineIC500.53 [1]
(R)-4-(2-(2-(2-Methylpyrrolidin-1-yl)ethyl)benzofuran-5-yl)benzonitrileIC500.63 [1]
PitolisantIC5012.0 [1]
PitolisantKi0.3 [1]
CiproxifanKi46.0 [1], 63.1 [2]
ClobenpropitIC501.0 [1]
ClobenpropitKi2.4 [1]
(R)-alpha-MethylhistamineIC502.3 [1]
(R)-alpha-MethylhistamineKi0.88 [1], 4.37 [2]
ImmepipKi0.48 [1]
HistamineKi9.33 [1]
6-((3-Cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy)-N-methyl-3-pyridinecarboxamideIC500.55 [1]
6-((3-Cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy)-N-methyl-3-pyridinecarboxamideKi0.2 [1]
2-Methyl-3-[4-(3-pyrrolidin-1-ylpropoxy)phenyl]-5-(trifluoromethyl)quinazolin-4-oneIC501.7 [1]
2-Methyl-3-[4-(3-pyrrolidin-1-ylpropoxy)phenyl]-5-(trifluoromethyl)quinazolin-4-oneKi0.53 [1], 0.63 [2], 1.7 [3], 6.8 [4]
5-[(3-Cyclobutyl-1,2,4,5-tetrahydro-3-benzazepin-7-yl)oxy]-N-methylpyrazine-2-carboxamideIC500.63 [1]
5-[(3-Cyclobutyl-1,2,4,5-tetrahydro-3-benzazepin-7-yl)oxy]-N-methylpyrazine-2-carboxamideKi0.19 [1], 0.2 [2], 0.21 [3]
ImetitKi0.57 [1], 0.7 [2], 1.58 [3]
4-(1H-Imidazol-5-yl)butan-1-amineKi3.98 [1], 4.07 [2], 4.3 [3]
[4-[4-[3-[(2S,5S)-2,5-Dimethylpyrrolidin-1-yl]propoxy]phenyl]phenyl]-morpholin-4-ylmethanoneKi0.49 [1], 1.58 [2], 2.0 [3], 12.0 [4]
FluoxetineKi7300.0 [1]
ConessineKi3.47 [1], 5.01 [2], 5.37 [3]
4-(3-(4-(Piperidinyl)but-1-ynyl)benzyl)morpholineKi0.8 [1], 1.0 [2], 1.18 [3], 1.3 [4]
(2R)-2-Amino-1-[4-[3-[4-(cyclopropanecarbonyl)phenoxy]propyl]piperazin-1-yl]propan-1-oneKi758.58 [1], 760.0 [2], 794.33 [3]
1-(6-((3-Cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[D]azepin-7-YL)oxy)pyridin-3-YL)pyrrolidin-2-oneKi0.1 [1], 0.12 [2], 0.2 [3], 10.0 [4]
ImmethridineKi0.77 [1], 0.79 [2], 0.85 [3]
2-[[(2R)-1-[4-[4-[3-(Azepan-1-yl)propoxy]phenyl]butyl]pyrrolidin-2-yl]methyl]-4-[(4-chlorophenyl)methyl]phthalazin-1-oneKi0.25 [1]
4-(4-((1-Isopropylpiperidin-4-yl)oxy)benzyl)morpholineKi2.1 [1], 2.14 [2]
2-(4-Piperidinopropoxyphenyl)-7-methylimidazo[1,2-a]pyridineKi2.0 [1]
(R)-2-(2,7-Dimethylpyrazolo[1,5-a]pyrimidin-6-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolineKi0.24 [1]
(S)-1-(2-(Pyrrolidin-1-ylmethyl)pyrrolidin-1-yl)-3-(4-(trifluoromethyl)phenyl)prop-2-en-1-oneKi4.7 [1], 5.0 [2], 6.7 [3], 7.0 [4]
2-Methyl-6-[4-[3-[(2R)-2-methylpyrrolidin-1-yl]propoxy]phenyl]pyridazin-3-oneKi1.0 [1], 1.4 [2]
1-[[4-(3-Piperidin-1-ylpropoxy)phenyl]methyl]piperidin-4-olIC500.72 [1]
1-[[4-(3-Piperidin-1-ylpropoxy)phenyl]methyl]piperidin-4-olKi0.59 [1], 0.74 [2]
AzelastineKi147.91 [1], 158.49 [2]
ProxyfanKi2.51 [1], 2.7 [2], 12.59 [3]
IodoproxyfanKi0.63 [1], 41.0 [2]
(5-Chloro-1H-benzimidazol-2-yl)(4-methylpiperazin-1-yl)methanoneKi3981.07 [1], 14053.0 [2], 20000.0 [3]
ImpentamineKi5.01 [1], 5.13 [2]
Unii-5P909hkp24Ki93.0 [1], 93.33 [2], 100.0 [3]
MethimepipKi1.0 [1]
CID 11452311IC502.51 [1]
CID 11452311Ki0.13 [1], 0.32 [2]
4,4'-Bis(piperidinomethyl)-1,1'-biphenylKi0.3 [1], 0.34 [2], 3.39 [3]
4-(3-Piperidin-1-ylpropoxy)benzonitrileKi11.0 [1], 25.0 [2], 25.12 [3]
2-(2-(4-Tert-Butylphenylthio)ethyl)-1H-imidazoleKi0.17 [1], 0.43 [2]
4-[4-[3-[(2R)-2-Methylpyrrolidin-1-yl]propoxy]phenyl]-1H-pyridazin-6-oneKi2.8 [1], 3.0 [2], 15.0 [3]
4-[2-(1H-Imidazol-4-yl)ethyl]piperidineKi19.95 [1]
[4-(3-Piperidin-1-yl-propoxy)-phenyl]-quinolin-4-yl-amine; Oxalic acidKi0.09 [1], 0.1 [2], 0.5 [3]
1-Cyano-3-[[(2R,5R)-5-(1H-imidazol-5-yl)oxolan-2-yl]methyl]-2-methylguanidineKi1995.26 [1], 2187.76 [2], 2200.0 [3]
4-[3-(1h-Imidazol-4-yl)propyl]piperidineKi4.47 [1]
2-[1-(6-Ethoxypyridazin-3-yl)-5-methylpyrazol-4-yl]-6-[2-[(2R)-2-methylpyrrolidin-1-yl]ethyl]quinolineKi0.19 [1], 0.2 [2]
3-Methyl-2-(4-(3-(pyrrolidin-1-yl)propoxy)phenyl)quinazolin-4(3H)-oneIC500.68 [1]
3-Methyl-2-(4-(3-(pyrrolidin-1-yl)propoxy)phenyl)quinazolin-4(3H)-oneKi0.22 [1], 4.2 [2]
(R)-2-(5-Methyl-1-(pyridin-2-yl)-1H-pyrazol-4-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolineKi0.26 [1]
(R)-2-(4-Methyl-2-(pyrrolidin-1-yl)pyrimidin-5-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolineKi0.29 [1], 0.3 [2]
2-Methyl-3-(4-(3-(pyrrolidin-1-yl)propoxy)phenyl)quinazolin-4(3H)-oneIC501.7 [1], 3.5 [2]
2-Methyl-3-(4-(3-(pyrrolidin-1-yl)propoxy)phenyl)quinazolin-4(3H)-oneKi1.09 [1]
(R)-2-Methyl-3-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-1,8-naphthyridineKi0.3 [1], 0.34 [2]
1-[4-[4-[(Dimethylamino)methyl]phenyl]phenyl]-N,N-dimethylmethanamineKi1.32 [1], 1.86 [2]
(R)-2-(1,3-Dimethyl-1H-pyrazol-4-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolineKi0.45 [1], 0.5 [2]
1-[2-[4-[4-(2-Piperidin-1-ylethyl)phenyl]phenyl]ethyl]piperidineKi1.18 [1], 1.2 [2]
4-[4-[4-(3-Piperidin-1-ylpropoxy)phenyl]cyclohexyl]morpholineKi0.41 [1], 0.67 [2]
N,N-Dimethyl-4-[4-(3-piperidin-1-ylpropoxy)phenyl]cyclohexan-1-amineKi0.2 [1], 0.21 [2], 0.3 [3]
5-(3-Benzhydryloxypropyl)-1H-imidazoleKi17.0 [1], 24.0 [2]
N-Ethyl-4-[4-[2-[(2R)-2-methylpyrrolidin-1-yl]ethyl]phenyl]benzenesulfonamideKi1.0 [1], 4.57 [2], 8.0 [3]
4-[4-[2-[(2R)-2-Methylpyrrolidin-1-yl]ethyl]phenyl]-N-(oxan-4-yl)benzenesulfonamideKi1.0 [1], 1.58 [2], 7.0 [3]
4-[4-[4-[2-[(2R)-2-Methylpyrrolidin-1-yl]ethyl]phenyl]phenyl]sulfonylmorpholineKi1.0 [1], 1.58 [2], 3.0 [3]
(2S,3S)-8-Methoxy-3-methyl-2-[4-(3-pyrrolidin-1-ylpropoxy)phenyl]-2,3-dihydro-1,4lambda6-benzoxathiine 4,4-dioxideIC500.43 [1]
(2S,3S)-8-Methoxy-3-methyl-2-[4-(3-pyrrolidin-1-ylpropoxy)phenyl]-2,3-dihydro-1,4lambda6-benzoxathiine 4,4-dioxideKi0.4 [1], 1.0 [2]
1-[4-[4-(3-Piperidin-1-ylpropoxy)phenyl]cyclohexyl]piperidin-4-olKi0.57 [1], 0.92 [2]
2-[4-[3-(Dibutylamino)propoxy]phenyl]-8-methylimidazo[1,2-a]pyridineKi4.0 [1], 2700.0 [2], 4000.0 [3]
(4-Fluorophenyl)(2-(2-((2R)-2-methyl-1-pyrrolidinyl)ethyl)-1-benzofuran-5-yl)methanoneKi0.27 [1], 1.9 [2]
2-[4-(3-Piperidin-1-yl-propoxy)-benzyl]-1,2,3,4-tetrahydro-isoquinolineKi1.7 [1], 2.95 [2]
2-(1-Cyclobutylpiperidin-4-yl)-6-(1-cyclobutylpiperidin-4-yl)oxy-3,4-dihydroisoquinolin-1-oneIC504.8 [1]
2-(1-Cyclobutylpiperidin-4-yl)-6-(1-cyclobutylpiperidin-4-yl)oxy-3,4-dihydroisoquinolin-1-oneKi0.03 [1], 0.8 [2]
4-(1-Propan-2-ylpiperidin-4-yl)oxy-N-(1-propan-2-ylpyrrolidin-3-yl)benzamideIC50323.8 [1]
4-(1-Propan-2-ylpiperidin-4-yl)oxy-N-(1-propan-2-ylpyrrolidin-3-yl)benzamideKi0.9 [1], 5.7 [2]
4-(1-Cyclopentylpiperidin-4-yl)oxy-N-(1-propan-2-ylpyrrolidin-3-yl)benzamideIC50273.9 [1]
4-(1-Cyclopentylpiperidin-4-yl)oxy-N-(1-propan-2-ylpyrrolidin-3-yl)benzamideKi1.0 [1], 8.6 [2]
N-[1-(2-Methylpropyl)pyrrolidin-3-yl]-4-(1-propan-2-ylpiperidin-4-yl)oxybenzamideIC50458.7 [1]
N-[1-(2-Methylpropyl)pyrrolidin-3-yl]-4-(1-propan-2-ylpiperidin-4-yl)oxybenzamideKi1.0 [1], 1.2 [2]
6-(1-Propan-2-ylpiperidin-4-yl)oxy-2-(1-propan-2-ylpyrrolidin-3-yl)-3,4-dihydroisoquinolin-1-oneIC5014.3 [1]
6-(1-Propan-2-ylpiperidin-4-yl)oxy-2-(1-propan-2-ylpyrrolidin-3-yl)-3,4-dihydroisoquinolin-1-oneKi0.1 [1], 2.1 [2]
ClozapineKi631.0 [1], 1000.0 [2]
(R)-4-(2-(2-(2-Methylpyrrolidin-1-yl)-ethyl)benzofuran-5-yl)benzonitrileKi0.95 [1]
2-(Diaminomethylideneamino)ethylsulfanylmethanimidamideKi316.23 [1], 1000.0 [2]
CipralisantKi2.14 [1], 3.98 [2]
N,N-Diallyl-5-methoxytryptamineKi1698.24 [1], 10000.0 [2]
PF-03654746Ki1.7 [1], 2.29 [2]
4'-(3-((3R)-3-(Dimethylamino)pyrrolidinyl)propoxy)(1,1'-biphenyl)-4-carbonitrileKi2.75 [1], 4.0 [2]
Aplysamine-1Ki30.0 [1]
5-[2-(5,5-Dimethylhex-1-ynyl)cyclopropyl]-1H-imidazoleKi2.14 [1], 2.15 [2]
3-(1H-Imidazol-5-yl)propyl carbamimidothioateKi2.51 [1], 3.16 [2]
1H-Imidazole-4-propanamineKi48.98 [1], 50.12 [2]



References

This online tool may be cited as follows

MLA

"Quest Database™ Histamine H3 receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc.10 May2024https://www.aatbio.com/data-sets/histamine-h3-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 10). Quest Database™ Histamine H3 receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/histamine-h3-receptor-inhibitors-ic50-ki.
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