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G-protein coupled receptor 4 Inhibitors (IC50, Ki)

Structure
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Compound Name
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Standard Type
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Standard Values (in nM)
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CID 68379135IC5067.0 [1], 70.0 [2], 74.0 [3]
GPR4 antagonist 1IC5055.0 [1], 110.0 [2], 114.0 [3]
4-[2,2-Dimethylpropyl-[[4-[3-(4-propan-2-ylpiperazin-1-yl)prop-1-ynyl]phenyl]methyl]amino]pyrimidine-2-carbonitrileIC501930.0 [1], 23000.0 [2]
4-[2,2-Dimethylpropyl-[[4-[(E)-3-(4-piperidin-1-ylpiperidin-1-yl)prop-1-enyl]phenyl]methyl]amino]pyrimidine-2-carbonitrileIC50490.0 [1], 23000.0 [2]
4-[(E)-3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]piperazin-2-oneIC5027.0 [1], 890.0 [2]
(2R)-3-[4-[(E)-3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]piperazin-1-yl]propane-1,2-diolIC5021.0 [1], 67.0 [2]
2-Ethyl-5,7-dimethyl-3-[[4-[3-(4-propan-2-ylpiperazin-1-yl)propyl]phenyl]methyl]pyrazolo[1,5-a]pyrimidineIC5013.0 [1], 20.0 [2]
3-[(2-Ethyl-5,7-dimethylimidazo[4,5-b]pyridin-3-yl)methyl]-8-(piperidin-1-ylmethyl)-6,11-dihydro-5H-benzo[b][1]benzazepineIC5067.0 [1]
3-[(2-Ethylbenzimidazol-1-yl)methyl]-6,11-dihydro-5H-benzo[b][1]benzazepineIC5010000.0 [1]
3-(Benzimidazol-1-ylmethyl)-6,11-dihydro-5H-benzo[b][1]benzazepineIC5010000.0 [1]
3-[(2-Ethyl-5,7-dimethylimidazo[4,5-b]pyridin-3-yl)methyl]-10H-phenothiazineIC50910.0 [1]
N-[4-(Dimethylamino)butyl]-4-[[2,2-dimethylpropyl-(2,6-dimethylpyrimidin-4-yl)amino]methyl]benzamideIC50160.0 [1]
1-[2-[1-[4-[[2,2-Dimethylpropyl-(2,6-dimethylpyrimidin-4-yl)amino]methyl]phenyl]triazol-4-yl]ethyl]piperidin-4-olIC5050.0 [1]
2-Chloro-N-(2,2-dimethylpropyl)-N-[[4-[(E)-3-(4-piperidin-1-ylpiperidin-1-yl)prop-1-enyl]phenyl]methyl]pyrimidin-4-amineIC50360.0 [1]
N-(2,2-Dimethylpropyl)-2-methoxy-N-[[4-[3-(4-propan-2-ylpiperazin-1-yl)prop-1-ynyl]phenyl]methyl]pyrimidin-4-amineIC50140.0 [1]
4-N-(2,2-Dimethylpropyl)-2-N,2-N-dimethyl-4-N-[[4-[(E)-3-(4-piperidin-1-ylpiperidin-1-yl)prop-1-enyl]phenyl]methyl]pyrimidine-2,4-diamineIC504800.0 [1]
2-Chloro-N-(2,2-dimethylpropyl)-N-[[4-[3-(4-propan-2-ylpiperazin-1-yl)prop-1-ynyl]phenyl]methyl]pyrimidin-4-amineIC50300.0 [1]
6-Ethyl-2,4-dimethyl-7-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]pyrrolo[2,3-d]pyrimidineIC5011600.0 [1]
5,7-Dimethyl-2-propan-2-yl-3-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]imidazo[4,5-b]pyridineIC502440.0 [1]
N-(2,2-Dimethylpropyl)-2,6-dimethyl-N-[[4-[3-(4-propan-2-ylpiperazin-1-yl)prop-1-ynyl]phenyl]methyl]pyrimidin-4-amineIC50800.0 [1]
N-(2,2-Dimethylpropyl)-2-methyl-N-[[4-[(E)-3-(4-piperidin-1-ylpiperidin-1-yl)prop-1-enyl]phenyl]methyl]pyrimidin-4-amineIC50380.0 [1]
2-Ethyl-3-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]imidazo[4,5-b]pyridineIC509100.0 [1]
N-(2,2-Dimethylpropyl)-2,6-dimethyl-N-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]pyrimidin-4-amineIC50330.0 [1]
5-(Dimethylamino)-N-[4-[[2,2-dimethylpropyl-(2,6-dimethylpyrimidin-4-yl)amino]methyl]phenyl]pentanamideIC50200.0 [1]
N-(2,2-Dimethylpropyl)-N-[[4-[(E)-3-(4-piperidin-1-ylpiperidin-1-yl)prop-1-enyl]phenyl]methyl]-6-(trifluoromethyl)pyrimidin-4-amineIC502970.0 [1]
N-(2,2-Dimethylpropyl)-2-methoxy-N-[[4-[(E)-3-(4-piperidin-1-ylpiperidin-1-yl)prop-1-enyl]phenyl]methyl]pyrimidin-4-amineIC50700.0 [1]
5,7-Dimethyl-2-(2-methylpropyl)-3-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]imidazo[4,5-b]pyridineIC507310.0 [1]
N-(2,2-Dimethylpropyl)-2,6-dimethyl-N-[[4-[(E)-3-(4-piperidin-1-ylpiperidin-1-yl)prop-1-enyl]phenyl]methyl]pyrimidin-4-amineIC50410.0 [1]
4-[3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]propyl]-1-propan-2-ylpiperidin-4-olIC5063.0 [1]
2-Ethyl-6,8-dimethyl-3-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]imidazo[1,2-b]pyridazineIC5074.0 [1]
3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]-1-piperidin-4-ylpropan-1-olIC5024.0 [1]
2-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]-5-piperazin-1-yl-1,3,4-oxadiazoleIC50368.0 [1]
3-[(2-Ethyl-5,7-dimethylimidazo[4,5-b]pyridin-3-yl)methyl]-6,11-dihydro-5H-benzo[b][1]benzazepineIC50900.0 [1]
4-[(2-Ethyl-5,7-dimethylimidazo[4,5-b]pyridin-3-yl)methyl]-N-phenylanilineIC5010000.0 [1]
5,7-Dimethyl-3-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]-2-propylimidazo[4,5-b]pyridineIC50760.0 [1]
2,5,7-Trimethyl-3-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]imidazo[4,5-b]pyridineIC50410.0 [1]
1-[(E)-3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]piperazin-2-oneIC5073.0 [1]
4-[3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]propyl]piperidin-4-olIC5050.0 [1]
3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]-1-piperazin-1-ylpropan-1-oneIC5053.0 [1]
2-Ethyl-5,7-dimethyl-3-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]pyrazolo[1,5-a]pyrimidineIC5043.0 [1]
3-[(2-Ethyl-5,7-dimethylimidazo[4,5-b]pyridin-3-yl)methyl]-8-[(4-methylpiperazin-1-yl)methyl]-6,11-dihydro-5H-benzo[b][1]benzazepineIC50130.0 [1]
4-[5-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]-1,3,4-oxadiazol-2-yl]cyclohexan-1-amineIC505.0 [1]
[4-[(E)-3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]piperazin-1-yl]-[(2S,3R)-3-hydroxypyrrolidin-2-yl]methanoneIC5035.0 [1]
2-Ethyl-5,7-dimethyl-3-[[4-[4-(piperazin-1-ylmethyl)triazol-1-yl]phenyl]methyl]pyrazolo[1,5-a]pyrimidineIC5038.0 [1]
2-Ethyl-3-[[4-[(E)-3-[(3S)-3-(methoxymethyl)piperazin-1-yl]prop-1-enyl]phenyl]methyl]-5,7-dimethylpyrazolo[1,5-a]pyrimidineIC5033.0 [1]
2-Ethyl-5,7-dimethyl-3-[[4-[(E)-3-piperazin-1-ylprop-1-enyl]phenyl]methyl]pyrazolo[1,5-a]pyrimidineIC5010.0 [1]
2-Amino-1-[4-[(E)-3-[4-[(2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]piperazin-1-yl]ethanoneIC5038.0 [1]
(2S)-1-[4-[5-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]-1,3,4-oxadiazol-2-yl]piperidin-1-yl]-3-hydroxy-2-(methylamino)propan-1-oneIC5015.0 [1]
Tert-butyl 4-[3-[4-[(2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]propanoyl]piperazine-1-carboxylateIC5054.0 [1]
1-[[1-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]pyrazol-4-yl]methyl]azetidin-3-olIC50118.0 [1]
2-Ethyl-5,7-dimethyl-3-[[4-[4-(piperazin-1-ylmethyl)pyrazol-1-yl]phenyl]methyl]pyrazolo[1,5-a]pyrimidineIC5043.0 [1]
Tert-butyl 4-[(E)-2-[4-[(2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]ethenyl]-4-hydroxypiperidine-1-carboxylateIC5045.0 [1]
2-Ethyl-5,7-dimethyl-3-[[4-[(E)-3-[(3S)-3-methylpiperazin-1-yl]prop-1-enyl]phenyl]methyl]pyrazolo[1,5-a]pyrimidineIC5019.0 [1]
2-Ethyl-5,7-dimethyl-3-[[4-[(E)-3-[4-(1-methyltetrazol-5-yl)piperidin-1-yl]prop-1-enyl]phenyl]methyl]pyrazolo[1,5-a]pyrimidineIC5033.0 [1]
Tert-butyl 4-[3-[4-[(2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]propyl]-4-hydroxypiperidine-1-carboxylateIC5047.0 [1]
4-[(E)-3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]piperidin-4-olIC5044.0 [1]
Tert-butyl N-[2-[4-[(E)-3-[4-[(2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]-4-hydroxypiperidin-1-yl]-2-oxoethyl]-N-methylcarbamateIC5034.0 [1]
[(2S)-4-[(E)-3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]piperazin-2-yl]methanolIC5028.0 [1]
4-[[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenoxy]methyl]cyclohexan-1-amineIC5035.0 [1]
Tert-butyl 4-[2-[4-[(2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenoxy]ethyl]piperazine-1-carboxylateIC5044.0 [1]
1-[[1-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]pyrazol-4-yl]methyl]piperidin-4-amineIC5026.0 [1]
Tert-butyl 3-[(E)-3-[4-[(2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]-3-hydroxyazetidine-1-carboxylateIC5034.0 [1]
4-[2-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenoxy]ethyl]piperidin-4-olIC50110.0 [1]
2-Ethyl-3-[[4-[2-[(3R)-3-(methoxymethyl)piperazin-1-yl]ethoxy]phenyl]methyl]-5,7-dimethylpyrazolo[1,5-a]pyrimidineIC5059.0 [1]
2-Ethyl-5,7-dimethyl-3-[[4-(piperidin-4-ylmethoxy)phenyl]methyl]pyrazolo[1,5-a]pyrimidineIC5022.0 [1]
(2S)-1-[4-[(E)-3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]piperazin-1-yl]-3-hydroxy-2-(methylamino)propan-1-oneIC5051.0 [1]
[4-[[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenoxy]methyl]piperidin-1-yl]-[(2S,3R)-3-hydroxypyrrolidin-2-yl]methanoneIC5019.0 [1]
(2S,4S)-4-[(E)-3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]-2-methylpiperidin-4-olIC5015.0 [1]
(2R)-3-[4-[(E)-3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]-4-hydroxypiperidin-1-yl]propane-1,2-diolIC5024.0 [1]
Tert-butyl 4-[[1-[4-[(2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]triazol-4-yl]methyl]-4-hydroxypiperidine-1-carboxylateIC5077.0 [1]
1-[[1-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]pyrazol-4-yl]methyl]azetidin-3-amineIC5021.0 [1]
(2S,3R)-N-[4-[[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenoxy]methyl]cyclohexyl]-3-hydroxypyrrolidine-2-carboxamideIC5054.0 [1]
1-[(2S)-4-[(E)-3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]-1-methylpiperazin-2-yl]-N,N-dimethylmethanamineIC507.0 [1]
(2R)-1-[Tert-butyl(dimethyl)silyl]oxy-3-[4-[(E)-3-[4-[(2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]piperazin-1-yl]propan-2-olIC5030.0 [1]
(E)-3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]-1-(4-methylpiperazin-1-yl)prop-2-en-1-oneIC5081.0 [1]
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References

This online tool may be cited as follows

MLA

"Quest Database™ G-protein coupled receptor 4 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Dec. 2024, https://www.aatbio.com/data-sets/g-protein-coupled-receptor-4-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, December 21). Quest Database™ G-protein coupled receptor 4 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/g-protein-coupled-receptor-4-inhibitors-ic50-ki.
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