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Histamine H4 receptor Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
1-[(5-Chloro-1H-indol-2-yl)carbonyl]-4-methylpiperazineIC5086.0 [1]
1-[(5-Chloro-1H-indol-2-yl)carbonyl]-4-methylpiperazineKi46.0 [1]
ThioperamideIC50667.0 [1], 680.0 [2], 977.0 [3]
HistamineKi14.45 [1]
(5-Chloro-1H-benzimidazol-2-yl)(4-methylpiperazin-1-yl)methanoneIC50138.0 [1], 530.0 [2]
(5-Chloro-1H-benzimidazol-2-yl)(4-methylpiperazin-1-yl)methanoneKi39.6 [1]
AdriforantIC500.65 [1], 1.3 [2], 4.9 [3], 30.0 [4]
ImmepipKi4.57e+16 [1]
ImetitKi1.6 [1], 3.6 [2], 6.31 [3]
4-(1H-Imidazol-5-yl)butan-1-amineKi10.0 [1], 12.7 [2], 14.45 [3], 6.92e+16 [4]
(5-Amino-1H-indol-2-yl)(4-methylpiperazin-1-yl)methanoneKi15.0 [1], 25.12 [2], 31.62 [3], 14996848.36 [4]
(R)-alpha-MethylhistamineKi146.0 [1], 184.0 [2], 251.19 [3], 4168690000000000.0 [4]
Jnj-39758979Ki12.0 [1], 12.5 [2], 10000.0 [3]
(5-Fluoro-1H-indol-2-yl)(4-methylpiperazin-1-yl)methanoneKi15.0 [1], 15.85 [2], 14996848.36 [3]
2-Chloro-6-(4-methylpiperazin-1-yl)benzo[b][1,4]benzoxazepineKi6.0 [1], 25.12 [2], 28.18 [3], 102.33 [4]
6-Chloro-2-(4-methylpiperazin-1-yl)-N-(thiophen-2-ylmethyl)quinazolin-4-amineIC5069.18 [1]
6-Chloro-2-(4-methylpiperazin-1-yl)-N-(thiophen-2-ylmethyl)quinazolin-4-amineKi7.59 [1], 42.66 [2]
(5-Hydroxy-1H-indol-2-yl)-(4-methyl-piperazin-1-yl)-methanoneKi23.0 [1], 25.12 [2], 23014418.17 [3]
(7-Amino-1H-indol-2-yl)-(4-methyl-piperazin-1-yl)-methanoneKi8.0 [1], 15.85 [2], 7998342.55 [3]
(7-Methyl-1H-indol-2-yl)-(4-methyl-piperazin-1-yl)-methanoneKi7.0 [1], 12.59 [2], 6998419.96 [3]
(4,5-Dichloro-1H-indol-2-yl)(4-methylpiperazin-1-yl)methanoneKi5.0 [1], 6.31 [2], 5000345.35 [3]
8-Chloro-4-(4-methylpiperazin-1-yl)benzofuro[3,2-d]pyrimidineIC5019.0 [1]
8-Chloro-4-(4-methylpiperazin-1-yl)benzofuro[3,2-d]pyrimidineKi4.7 [1], 5.0 [2], 19.0 [3]
Piperazine, 1-((5-methoxyindol-2-yl)carbonyl)-4-methyl-Ki1000.0 [1], 3000.0 [2], 5011.87 [3]
(5-Methyl-1H-indol-2-yl)(4-methylpiperazin-1-yl)methanoneKi46.0 [1], 50.12 [2], 46025657.36 [3]
(7-Chloro-1H-indol-2-yl)(4-methylpiperazin-1-yl)methanoneKi19.0 [1], 19.95 [2], 19010782.8 [3]
(5-Bromo-1H-indol-2-yl)-(4-methyl-piperazin-1-yl)-methanoneKi8.0 [1], 31.62 [2], 7998342.55 [3]
[(3As,6aR)-2-methyl-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrol-5-yl]-(5,6-difluoro-1H-benzimidazol-2-yl)methanimineKi9.5 [1], 10.0 [2], 17.2 [3]
4-(4-Chlorophenyl)-6-(4-methylpiperazin-1-yl)pyrimidin-2-amineKi2.0 [1], 3.16 [2], 63.1 [3], 199.53 [4]
N-(3,3-Dimethylbutyl)-6-(4-methylpiperazin-1-yl)pyrimidin-4-amineKi37.0 [1], 82.0 [2], 92.0 [3]
[(3Ar,6aS)-2-methyl-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrol-5-yl]-(5,6-difluoro-1H-benzimidazol-2-yl)methanoneKi53.0 [1], 128.0 [2], 236.0 [3]
6-N-(3,3-Dimethylbutyl)-4-N-[(3S)-pyrrolidin-3-yl]pyrimidine-4,6-diamineKi502.0 [1], 572.0 [2]
[(3Ar,6aS)-2-methyl-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrol-5-yl]-(5-chloro-1H-indol-2-yl)methanoneKi16.0 [1], 27.0 [2]
[(3Ar,6aS)-2-methyl-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrol-5-yl]-(6-fluoro-1H-benzimidazol-2-yl)methanoneKi39.0 [1], 83.0 [2], 145.0 [3]
DiphenhydramineIC5011000.0 [1]
DiphenhydramineKi11000.0 [1], 42657.95 [2]
DimapritKi90.0 [1], 316.23 [2]
CiproxifanKi612.0 [1], 1862.09 [2]
2-(Diaminomethylideneamino)ethylsulfanylmethanimidamideKi25.12 [1], 31.62 [2]
ImpentamineKi251.19 [1], 2691530000000000.0 [2]
6,7-Dichloro-3-(4-methylpiperazin-1-yl)-1H-quinoxalin-2-oneKi5.62 [1], 6.0 [2]
2-(4-Methylpiperazin-1-yl)quinazolineKi7585.78 [1]
6-Chloro-N-(furan-3-ylmethyl)-2-(4-methylpiperazin-1-yl)quinazolin-4-amineIC50144.54 [1]
6-Chloro-N-(furan-3-ylmethyl)-2-(4-methylpiperazin-1-yl)quinazolin-4-amineKi26.92 [1], 89.13 [2]
1-Cyano-3-[[(2R,5R)-5-(1H-imidazol-5-yl)oxolan-2-yl]methyl]-2-methylguanidineKi125.0 [1], 125.89 [2]
12-Chloro-6-[(3R)-3-(methylamino)pyrrolidin-1-yl]-8-oxa-3,5,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaen-4-amineKi9.0 [1], 9.4 [2]
7-(Furan-2-yl)-4-piperazin-1-ylquinazolin-2-amineIC50106.0 [1]
7-(Furan-2-yl)-4-piperazin-1-ylquinazolin-2-amineKi15.14 [1], 16.0 [2]
[5-[[3-[[6-(3,3-Dimethylbutylamino)pyrimidin-4-yl]amino]pyrrolidin-1-yl]methyl]furan-2-yl]methanolKi2110.0 [1]
(5,7-Dimethyl-1H-indol-2-yl)(4-methylpiperazin-1-yl)methanoneKi31.0 [1], 30974192.99 [2]
(4-Bromo-1H-indol-2-yl)(4-methylpiperazin-1-yl)methanoneKi32.0 [1], 31988951.1 [2]
(R)-8-Chloro-4-(3-(methylamino)pyrrolidin-1-yl)benzofuro[3,2-d]pyrimidin-2-amineIC501.0 [1], 3.0 [2]
(R)-8-Chloro-4-(3-(methylamino)pyrrolidin-1-yl)benzofuro[3,2-d]pyrimidin-2-amineKi0.4 [1]
(S)-8-Chloro-4-(3-(methylamino)pyrrolidin-1-yl)benzofuro[3,2-d]pyrimidin-2-amineIC504.0 [1], 13.0 [2]
(S)-8-Chloro-4-(3-(methylamino)pyrrolidin-1-yl)benzofuro[3,2-d]pyrimidin-2-amineKi2.0 [1]
2-[[6-Chloro-2-(4-methylpiperazin-1-yl)quinazolin-4-yl]amino]-N-phenylethanesulfonamideIC5033.11 [1]
2-[[6-Chloro-2-(4-methylpiperazin-1-yl)quinazolin-4-yl]amino]-N-phenylethanesulfonamideKi4.0 [1], 4.9 [2]
(4-Methylpiperazin-1-yl)-(1H-pyrrolo[2,3-b]pyridin-2-yl)methanoneKi1995.26 [1], 3100.0 [2], 29900.0 [3]
4-(4-Bromophenyl)-6-(4-methylpiperazin-1-yl)-1,3,5-triazin-2-amineIC501630.0 [1]
4-(4-Bromophenyl)-6-(4-methylpiperazin-1-yl)-1,3,5-triazin-2-amineKi520.0 [1], 524.0 [2]
(5,7-Difluoro-1H-indol-2-yl)(4-methylpiperazin-1-yl)methanoneKi14.0 [1], 13995873.23 [2]
(5,7-Dichloro-1H-indol-2-yl)(4-methylpiperazin-1-yl)methanoneKi11.0 [1], 5000345.35 [2]
(7-Bromo-1H-indol-2-yl)-(4-methylpiperazin-1-yl)methanoneKi61.0 [1], 61094202.49 [2]
ClozapineKi199.53 [1], 501.19 [2]
KetotifenIC5021000.0 [1]
KetotifenKi21000.0 [1]
DesloratadineIC5016000.0 [1]
DesloratadineKi16000.0 [1]
ImpromidineKi12.3 [1], 25.12 [2]
BurimamideKi39.81 [1], 180.0 [2]
PitolisantKi10000.0 [1], 100000.0 [2]
IodophenpropitKi7.8 [1], 16.0 [2]
IodoproxyfanKi12.59 [1]
MethimepipKi1995.26 [1]
ImmethridineKi245.47 [1], 251.19 [2]
3-(1H-Imidazol-5-yl)propyl carbamimidothioateKi10.0 [1], 12.59 [2]
2-(4-Methylpiperazin-1-yl)quinoxalineKi891.25 [1], 1060.0 [2]
1H-Imidazole-4-propanamineKi31.62 [1], 2.88e+16 [2]
3-Benzyl-2-(4-methylpiperazinyl)-quinoxalineKi39.81 [1]
(7As,11aS)-4-piperazin-1-yl-5,6,7a,8,9,10,11,11a-octahydro-[1]benzofuro[2,3-h]quinazolin-2-amineKi5.75 [1], 79.43 [2]
2-(2-(4-Tert-Butylphenylthio)ethyl)-1H-imidazoleKi1.1 [1]
3-(4-Methylpiperazin-1-yl)-1H-quinoxalin-2-oneKi61.66 [1], 63.1 [2]
5H-Benzo(6,7)cyclohepta(1,2-d)pyrimidin-2-amine, 4-((3R)-3-amino-1-pyrrolidinyl)-6,7-dihydro-Ki4.7 [1], 5.0 [2]
(4-(Piperazin-1-yl)-6,7-dihydro-5H-benzo(6,7)cyclohepta(1,2-d)pyrimidin-2-yl)amineKi71.0 [1], 79.43 [2]
N-Benzyl-2-(4-methylpiperazin-1-yl)quinazolin-4-amineKi1071.52 [1]
ImifuramineKi794.33 [1], 891.25 [2]
2-(4-Methylpiperazino)-4-quinazolinamineKi1737.8 [1], 2137.96 [2]
(1R,2S)-trans-2-[2-(4-Chlorobenzylamino)ethyl]-1-(1H-imidazol-4-yl)cyclopropaneIC50110.0 [1]
(1R,2S)-trans-2-[2-(4-Chlorobenzylamino)ethyl]-1-(1H-imidazol-4-yl)cyclopropaneKi7.6 [1]
6-Chloro-2-(4-methylpiperazin-1-yl)quinazolin-4-amineKi104.71 [1], 154.88 [2]
4-[2-Amino-6-(4-methylpiperazin-1-yl)pyrimidin-4-yl]benzonitrileKi34.67 [1], 35.0 [2]
N4-Benzyl-6-(4-methylpiperazin-1-yl)pyrimidine-2,4-diamineKi20.0 [1], 98.0 [2]
6-Chloro-2-(4-methylpiperazin-1-yl)-N-propan-2-ylquinazolin-4-amineKi758.58 [1]
6-Chloro-N-(cyclohexylmethyl)-2-(4-methylpiperazin-1-yl)quinazolin-4-amineKi588.84 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Histamine H4 receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc.21 Dec2024https://www.aatbio.com/data-sets/histamine-h4-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024December 21). Quest Database™ Histamine H4 receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/histamine-h4-receptor-inhibitors-ic50-ki.
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