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Serotonin 4 (5-HT4) receptor Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
(1-(2-(Methylsulfonylamino)ethyl)-4-piperidinyl)methyl 1-methyl-1H-indole-3-carboxylateIC500.21 [1]
PiboserodIC500.63 [1]
PiboserodKi0.25 [1]
TegaserodKi3.98 [1], 31.0 [2]
2-Methoxy-4-amino-5-chlorobenzoic acid 2-(4-phenylpiperazino)ethyl esterKi12.5 [1], 14.3 [2], 23.0 [3], 32.0 [4], 55.0 [5]
2-Methoxy-4-amino-5-chlorobenzoic acid 2-[4-(2-pyrimidinyl)piperazino]ethyl esterKi1.0 [1], 2.47 [2], 3.5 [3], 7.03 [4], 8.1 [5]
SerotoninKi29.51 [1], 109.65 [2], 500.0 [3], 1049.0 [4]
CisaprideIC500.36 [1]
CisaprideKi29.0 [1], 100.0 [2], 125.89 [3]
PF-04995274Ki0.15 [1], 0.32 [2], 0.36 [3], 0.46 [4]
6-Fluoro-N-[[1-[(4-hydroxyoxan-4-yl)methyl]piperidin-4-yl]methyl]-2-oxo-3-propan-2-ylbenzimidazole-1-carboxamideKi1.7 [1], 4.4 [2], 4.9 [3], 5.5 [4]
6-Fluoro-N-[[1-[(4-hydroxyoxan-4-yl)methyl]piperidin-4-yl]methyl]-3,3-dimethyl-2-oxoindole-1-carboxamideKi2.7 [1], 4.6 [2], 6.3 [3], 6.8 [4]
4-Amino-5-chloro-N-{1-[3-(4-fluoro-phenoxy)-propyl]-3-methoxy-piperidin-4-yl}-2-methoxy-benzamideIC50483.0 [1]
4-Amino-5-chloro-N-{1-[3-(4-fluoro-phenoxy)-propyl]-3-methoxy-piperidin-4-yl}-2-methoxy-benzamideKi100.0 [1]
PrucaloprideKi2.51 [1], 7.5 [2], 1000.0 [3]
N-[(1S,5R)-8-[(2S)-2-Hydroxy-3-(4-methylsulfonylpiperazin-1-yl)propyl]-8-azabicyclo[3.2.1]octan-3-yl]-2-oxo-1-propan-2-ylquinoline-3-carboxamideKi12.59 [1]
2-[4-[4-[3-[4-[3-[[4-[[1-[2-(4-Amino-5-chloro-2-methoxybenzoyl)oxyethyl]piperidin-4-yl]amino]-4-oxobutyl]-[(2-methylpropan-2-yl)oxycarbonyl]amino]propyl]phenyl]propyl-[(2-methylpropan-2-yl)oxycarbonyl]amino]butanoylamino]piperidin-1-yl]ethyl 4-amino-5-chloro-2-methoxybenzoateKi10.0 [1], 12.0 [2]
5-MethoxytryptamineKi26.92 [1], 245.47 [2]
3-Piperidin-1-ylpropyl 4-amino-5-chloro-2-methoxybenzoateIC5049.0 [1]
3-Piperidin-1-ylpropyl 4-amino-5-chloro-2-methoxybenzoateKi31.62 [1]
5-Chloro-N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]-3-methyl-1-benzothiophene-2-sulfonamideKi3162.28 [1]
Unii-0ZN0AQ6sbvKi10.0 [1]
3-Cyclopropyl-2-oxo-N-[2-(4-propan-2-ylpiperazin-1-yl)ethyl]benzimidazole-1-carboxamideKi6.7 [1], 16.6 [2]
N-[(1R,5S)-8-Azabicyclo[3.2.1]octan-3-yl]-1-propan-2-ylindazole-3-carboxamideKi63.1 [1]
2-[4-[11-[[4-[[11-[[1-[2-(4-Amino-5-chloro-2-methoxybenzoyl)oxyethyl]piperidin-4-yl]amino]-11-oxoundecyl]amino]-6-(benzylamino)-1,3,5-triazin-2-yl]amino]undecanoylamino]piperidin-1-yl]ethyl 4-amino-5-chloro-2-methoxybenzoateKi113.0 [1]
2-[4-[[11-[[1-[2-(4-Amino-5-chloro-2-methoxybenzoyl)oxyethyl]piperidin-4-yl]amino]-11-oxoundecyl]carbamoyl]piperidin-1-yl]ethyl 4-amino-5-chloro-2-methoxybenzoateKi20.0 [1]
2-[4-[11-[[11-[[1-[2-(4-Amino-5-chloro-2-methoxybenzoyl)oxyethyl]piperidin-4-yl]amino]-11-oxoundecyl]-[2-oxo-2-(piperidin-4-ylmethylamino)ethyl]amino]undecanoylamino]piperidin-1-yl]ethyl 4-amino-5-chloro-2-methoxybenzoateKi50.0 [1]
2-[4-[2-[[12-[2-[1-[2-(4-Amino-5-chloro-2-methoxybenzoyl)oxyethyl]piperidin-4-yl]ethylamino]-12-oxododecanoyl]amino]ethyl]piperidin-1-yl]ethyl 4-amino-5-chloro-2-methoxybenzoateKi9.0 [1], 18.0 [2]
7-Fluoro-5-[(1-propylpiperidin-4-yl)methoxy]benzo[h][1,6]naphthyridineKi0.04 [1]
4-Fluoro-6-[(1-propylpiperidin-4-yl)methoxy]phenanthridineKi3.1 [1]
2-Methoxy-4-amino-5-chlorobenzoic acid 2-[4-(2-chlorophenyl)piperazino]ethyl esterIC50296.0 [1]
2-Methoxy-4-amino-5-chlorobenzoic acid 2-[4-(2-chlorophenyl)piperazino]ethyl esterKi296.0 [1]
2-Methoxy-4-amino-5-chlorobenzoic acid 2-[4-(2-fluorophenyl)piperazino]ethyl esterIC5017.0 [1]
2-Methoxy-4-amino-5-chlorobenzoic acid 2-[4-(2-fluorophenyl)piperazino]ethyl esterKi16.8 [1]
2-Methoxy-4-amino-5-chlorobenzoic acid 2-[4-(3-chlorophenyl)piperazino]ethyl esterIC50162.0 [1]
2-Methoxy-4-amino-5-chlorobenzoic acid 2-[4-(3-chlorophenyl)piperazino]ethyl esterKi162.0 [1]
2-Methoxy-4-amino-5-chlorobenzoic acid 2-[4-(4-methoxyphenyl)piperazino]ethyl esterIC5018.0 [1]
2-Methoxy-4-amino-5-chlorobenzoic acid 2-[4-(4-methoxyphenyl)piperazino]ethyl esterKi17.7 [1]
2-Methoxy-4-amino-5-chlorobenzoic acid 2-[4-(4-chlorophenyl)piperazino]ethyl esterIC50715.0 [1]
2-Methoxy-4-amino-5-chlorobenzoic acid 2-[4-(4-chlorophenyl)piperazino]ethyl esterKi715.0 [1]
2-Methoxy-4-amino-5-chlorobenzoic acid 2-[4-(2-methoxyphenyl)piperazino]ethyl esterIC5064.0 [1]
2-Methoxy-4-amino-5-chlorobenzoic acid 2-[4-(2-methoxyphenyl)piperazino]ethyl esterKi64.0 [1]
2-Methoxy-4-amino-5-chlorobenzoic acid 2-[4-(3-methoxyphenyl)piperazino]ethyl esterIC503.0 [1]
2-Methoxy-4-amino-5-chlorobenzoic acid 2-[4-(3-methoxyphenyl)piperazino]ethyl esterKi3.0 [1]
4-[2-[4-[(2-Methylpyrrolo[3,4-c]quinolin-4-yl)oxymethyl]piperidin-1-yl]ethyl]benzoic acidIC502.8 [1]
4-[2-[4-[(2-Methylpyrrolo[3,4-c]quinolin-4-yl)oxymethyl]piperidin-1-yl]ethyl]benzoic acidKi2.0 [1]
4-[2-[4-[[(1-Propan-2-ylindazole-3-carbonyl)amino]methyl]piperidin-1-yl]ethyl]benzoic acidIC509.8 [1]
4-[2-[4-[[(1-Propan-2-ylindazole-3-carbonyl)amino]methyl]piperidin-1-yl]ethyl]benzoic acidKi0.79 [1]
TropisetronKi199.53 [1]
GR-127935Ki10000.0 [1]
(R)-3-((2-(2-(4-Methylpiperidin-1-yl)ethyl)pyrrolidin-1-yl)sulfonyl)phenolKi1258.93 [1]
5-Chloro-N-(4-methoxy-3-(piperazin-1-yl)phenyl)-3-methylbenzo[b]thiophene-2-sulfonamideKi3981.07 [1]
2-(Diethylamino)ethyl 4-amino-5-chloro-2-methoxybenzoateKi6.31 [1]
SB 204070 hydrochlorideKi0.02 [1]
1-(1-Methylindol-5-yl)-3-(3-methyl-1,2-thiazol-5-yl)ureaKi10000.0 [1]
1-Phenyl-3-[[3-(trifluoromethyl)phenyl]imino]-1h-indol-2-oneKi72.0 [1]
4-(4-Butylpiperidin-1-yl)-1-o-tolylbutan-1-oneKi1000.0 [1]
(1-Butylpiperidin-4-yl)methyl 5-amino-6-iodo-2,3-dihydro-1,4-benzodioxine-8-carboxylateKi2.2 [1]
VelusetragKi19.95 [1]
BarettinKi1910.0 [1]
N-(2,5-Dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamideKi5011.87 [1]
NaluzotanKi5000.0 [1]
4-Methyl-1-[2-[(2R)-1-(3-methylphenyl)sulfonylpyrrolidin-2-yl]ethyl]piperidineKi10000.0 [1]
Methyl 4-[[4-[[(2-propan-2-yl-1H-benzimidazole-4-carbonyl)amino]methyl]piperidin-1-yl]methyl]piperidine-1-carboxylateKi0.4 [1]
CID 10028436Ki1905.46 [1]
NorcisaprideIC5019.0 [1]
N-[1-[3-(3-Oxo-1,4-benzoxazin-4-yl)propyl]piperidin-4-yl]-2-phenylacetamideKi1000.0 [1]
CID 44240743Ki6000.0 [1]
Unii-7qgn8qxg7IKi36.0 [1]
4-Bromo-N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]benzenesulfonamideKi2511.89 [1]
N-[3-[(8As)-3,4,6,7,8,8a-hexahydro-1H-pyrrolo[1,2-a]pyrazin-2-yl]-4-methoxyphenyl]-5-chloro-3-methyl-1-benzothiophene-2-sulfonamideKi5011.87 [1]
2-Methyl-5-(2-(4-(quinolin-8-ylmethyl)piperazin-1-yl)ethoxy)quinolineKi5011.87 [1]
CID 10331436Ki1700.0 [1]
3-Ethyl-N-(8-methyl-8-azabicyclo[3.2.1]octan-3-yl)-2-oxobenzimidazole-1-carboxamideKi13.0 [1]
N-(3-(1-(2-(2-Methylquinolin-5-yloxy)ethyl)piperidin-4-ylmethyl)phenyl)methanesulfonamideKi10000.0 [1]
4-Amino-5-chloro-2-methoxy-N-piperidin-4-YL-benzamideKi1584.89 [1]
CID 44391713Ki0.79 [1]
4-Amino-5-chloro-2-methoxy-N-(piperidin-4-ylmethyl)benzamideKi316.23 [1]
4-Fluoro-N-[3-(1-methyl-piperidin-4-yl)-1H-pyrrolo[3,2-b]pyridin-5-yl]-benzamideKi4000.0 [1]
2-[4-[(6-Amino-1,3-dioxobenzo[de]isoquinolin-2-yl)methyl]piperidin-1-yl]ethyl 4-amino-5-chloro-2-methoxybenzoateKi64.0 [1]
6-Iodo-1-indolinyl 3-piperazino-4-methoxyphenyl sulfoneKi3981.07 [1]
N-Piperidin-4-yl-1-propan-2-ylindazole-3-carboxamideKi398.11 [1]
N-[2-(4-Methylpiperazin-1-yl)ethyl]-2-oxo-3-propan-2-ylbenzimidazole-1-carboxamideKi91.9 [1]
1-((S)-2-Aminopropyl)-1H-indazol-6-olKi515.0 [1]
4-[(Z)-(4-Bromoindol-3-ylidene)methyl]-5-hydroxy-1,3-dihydroimidazole-2-thioneKi2359.0 [1]
4-[(Z)-(7-Bromoindol-3-ylidene)methyl]-5-hydroxy-1,3-dihydroimidazole-2-thioneKi2214.0 [1]
5-[(Z)-(4-Bromoindol-3-ylidene)methyl]-2-methylsulfanyl-1H-imidazol-4-olKi1063.0 [1]
5-[(Z)-(5-Bromoindol-3-ylidene)methyl]-2-methylsulfanyl-1H-imidazol-4-olKi3799.0 [1]
5-[(Z)-(6-Bromoindol-3-ylidene)methyl]-2-methylsulfanyl-1H-imidazol-4-olKi5308.0 [1]
5-[(Z)-(7-Bromoindol-3-ylidene)methyl]-2-methylsulfanyl-1H-imidazol-4-olKi2345.0 [1]
5-[(Z)-Indol-3-ylidenemethyl]-2-(methylamino)-1H-imidazol-4-olKi928.0 [1]
5-[(Z)-(4-Bromoindol-3-ylidene)methyl]-2-(methylamino)-1H-imidazol-4-olKi472.0 [1]
5-[(Z)-(5-Bromoindol-3-ylidene)methyl]-2-(methylamino)-1H-imidazol-4-olKi226.0 [1]
5-[(Z)-(6-Bromoindol-3-ylidene)methyl]-2-(methylamino)-1H-imidazol-4-olKi1156.0 [1]
5-[(Z)-(7-Bromoindol-3-ylidene)methyl]-2-(methylamino)-1H-imidazol-4-olKi603.0 [1]
(1-Butylpiperidin-4-yl)methyl 4-amino-3-methoxybenzoateKi2.4 [1]
7-[2-[2-(3-Chlorophenyl)ethylamino]ethyl]quinolin-2-AmineKi100.0 [1]
1-(3,7,8,9-Tetrahydropyrano[3,2-e]indole-1-yl)propane-2-amineKi1800.0 [1]
N-[3-[(8Ar)-3,4,6,7,8,8a-hexahydro-1H-pyrrolo[1,2-a]pyrazin-2-yl]-4-methoxyphenyl]-5-chloro-3-methyl-1-benzothiophene-2-sulfonamideKi1584.89 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Serotonin 4 (5-HT4) receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc.20 Nov2024https://www.aatbio.com/data-sets/serotonin-4-5-ht4-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024November 20). Quest Database™ Serotonin 4 (5-HT4) receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/serotonin-4-5-ht4-receptor-inhibitors-ic50-ki.
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