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Serotonin 3a (5-HT3a) receptor Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
BemesetronIC5010.0 [1]
BemesetronKi3.9 [1]
OndansetronIC500.09 [1]
OndansetronKi2.8 [1], 3.4 [2], 16.0 [3], 16.2 [4]
TropisetronKi2.7 [1], 2.82 [2], 5.3 [3]
AlosetronKi0.5 [1]
(3R)-N-Isoquinolin-3-ylspiro[1-azabicyclo[2.2.2]octane-3,5'-4H-1,3-oxazole]-2'-amineIC50480.0 [1]
ClozapineKi186.21 [1], 1000.0 [2]
GranisetronKi1.45 [1], 3.98 [2]
3-Amino-2-[4-(4-quinolin-2-ylpiperazin-1-yl)butyl]-5,6,7,8-tetrahydroquinazolin-4-oneIC508.9 [1], 8.93 [2]
3-Amino-2-[4-(4-quinolin-2-ylpiperazin-1-yl)butyl]-5,6,7,8-tetrahydroquinazolin-4-oneKi4.72 [1]
6-Chloro-2-(1,4-diazabicyclo[3.2.2]nonan-4-yl)-[1,3]oxazolo[4,5-b]pyridineIC50484.0 [1]
6-Chloro-2-(1,4-diazabicyclo[3.2.2]nonan-4-yl)-[1,3]oxazolo[4,5-b]pyridineKi1370.0 [1]
6-Chloro-2-(1,4-diazabicyclo[3.2.2]nonan-4-yl)-5-methyl-[1,3]oxazolo[4,5-b]pyridineIC5070.0 [1]
6-Chloro-2-(1,4-diazabicyclo[3.2.2]nonan-4-yl)-5-methyl-[1,3]oxazolo[4,5-b]pyridineKi244.0 [1]
FaciniclineIC502.8 [1], 32.7 [2]
FaciniclineKi2.0 [1]
1-(2-((2,4-Dimethylphenyl)thio)phenyl)piperazine hydrochlorideIC5012.0 [1]
1-(2-((2,4-Dimethylphenyl)thio)phenyl)piperazine hydrochlorideKi3.7 [1], 23.0 [2]
SumatriptanIC509.3 [1], 10000.0 [2]
CisaprideKi1995.26 [1]
PalonosetronIC500.83 [1]
PalonosetronKi0.03 [1]
TegaserodKi2511.89 [1], 10000.0 [2]
AlcuroniumIC50100000.0 [1]
AlcuroniumKi100000.0 [1]
ZacoprideKi0.39 [1], 0.7 [2]
RamosetronKi0.06 [1]
(S)-ZacoprideKi0.18 [1], 5011.87 [2]
2-(5-Methoxy-2-methyl-1H-indol-3-yl)ethanamineKi10000.0 [1]
5-[2-[4-(2,3-Dimethylphenyl)piperazin-1-yl]ethyl]-2H-benzotriazoleKi10000.0 [1]
N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-1-benzofuran-6-carboxamideIC50962.0 [1]
N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-1-benzofuran-6-carboxamideKi310.0 [1]
N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-1-benzothiophene-6-carboxamideIC50188.0 [1]
N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-1-benzothiophene-6-carboxamideKi174.0 [1]
(3R)-N-Isoquinolin-1-ylspiro[1-azabicyclo[2.2.2]octane-3,5'-4H-1,3-oxazole]-2'-amineIC501600.0 [1]
Trimethyl-[[20-[(trimethylazaniumyl)methyl]-3,13-diazapentacyclo[11.7.0.03,11.04,9.014,19]icosa-1(20),4,6,8,10,14,16,18-octaen-10-yl]methyl]azanium;diiodideIC50100000.0 [1]
Trimethyl-[[20-[(trimethylazaniumyl)methyl]-3,13-diazapentacyclo[11.7.0.03,11.04,9.014,19]icosa-1(20),4,6,8,10,14,16,18-octaen-10-yl]methyl]azanium;diiodideKi100000.0 [1]
(3R)-N-(6-Phenylpyrimidin-4-yl)spiro[1-azabicyclo[2.2.2]octane-3,5'-4H-1,3-oxazole]-2'-amineIC509200.0 [1]
(3R)-N-Pyridin-2-ylspiro[1-azabicyclo[2.2.2]octane-3,5'-4H-1,3-oxazole]-2'-amineIC5015.0 [1]
N-[(3R)-1-Azabicyclo[2.2.2]octan-3-yl]-1-benzofuran-5-carboxamideIC50580.0 [1]
N-[(3R)-1-Azabicyclo[2.2.2]octan-3-yl]-1-benzofuran-5-carboxamideKi663.0 [1]
4-[2-(1H-Benzotriazol-5-yl)ethyl]-1-(2-methoxyphenyl)piperazineKi10000.0 [1]
4-[2-(1H-Benzotriazol-5-yl)ethyl]-1-(1-naphthyl)piperazineKi10000.0 [1]
3-Methyl-8-[(1-propylpiperidin-4-yl)methoxy]-5-thia-1,7-diazatricyclo[7.3.0.02,6]dodeca-2(6),3,7,9,11-pentaeneIC506.92 [1], 385.0 [2]
(1R,9R,18S,19S,21R,22R,23R,25R,32S,34R,35R,36S)-24-Phenyl-10,26-dioxa-8,15,24,31-tetrazaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneIC5012589.25 [1]
(1R,9R,18S,19S,21R,22R,23R,25R,32S,34R,35R,36S)-24-Phenyl-10,26-dioxa-8,15,24,31-tetrazaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneKi3162.28 [1]
(2E)-2-[(1R,9Z,11S,13S,17S,18R,20R,27S,29R,30R,31S)-19-Phenyl-21-oxa-8,14,19,26-tetrazadecacyclo[24.5.2.211,14.01,27.02,7.08,31.010,18.013,17.020,30.024,29]pentatriaconta-2,4,6,9,23-pentaen-35-ylidene]ethanolIC502511.89 [1]
(2E)-2-[(1R,9Z,11S,13S,17S,18R,20R,27S,29R,30R,31S)-19-Phenyl-21-oxa-8,14,19,26-tetrazadecacyclo[24.5.2.211,14.01,27.02,7.08,31.010,18.013,17.020,30.024,29]pentatriaconta-2,4,6,9,23-pentaen-35-ylidene]ethanolKi1995.26 [1]
10-[(3S)-1-Azabicyclo[2.2.2]octan-3-yl]-1,2,10-triazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraen-9-oneKi8.0 [1], 8.1 [2]
6-[(3S)-1-Azabicyclo[2.2.2]octan-3-yl]-2-methyl-2,6-diazatricyclo[6.3.1.04,12]dodeca-1(11),3,8(12),9-tetraen-7-oneKi0.7 [1], 1.0 [2]
10-[(3S)-1-Azabicyclo[2.2.2]octan-3-yl]-6-chloro-3-methyl-1,10-diazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraen-9-oneKi0.2 [1]
10-[(3S)-1-Azabicyclo[2.2.2]octan-3-yl]-6-chloro-1,2,10-triazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraen-9-oneKi0.5 [1]
10-[(3S)-1-Azabicyclo[2.2.2]octan-3-yl]-1,10-diazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraen-9-oneKi3.1 [1], 4.0 [2]
10-[(3S)-1-Azabicyclo[2.2.2]octan-3-yl]-1,3,10-triazatricyclo[6.4.1.04,13]trideca-4,6,8(13)-triene-2,9-dioneKi5.7 [1], 7.0 [2]
10-[(3R)-1-Azabicyclo[2.2.2]octan-3-yl]-1,10-diazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraen-9-oneKi67.6 [1], 74.0 [2]
10-[(3S)-1-Azabicyclo[2.2.2]octan-3-yl]-2,2-dioxo-2lambda6-thia-1,3,10-triazatricyclo[6.4.1.04,13]trideca-4,6,8(13)-trien-9-oneKi701.0 [1]
[20-[[Dimethyl-[(4-nitrophenyl)methyl]azaniumyl]methyl]-3,13-diazapentacyclo[11.7.0.03,11.04,9.014,19]icosa-1(20),4,6,8,10,14,16,18-octaen-10-yl]methyl-dimethyl-[(4-nitrophenyl)methyl]azaniumIC5031622.78 [1]
[20-[[Dimethyl-[(4-nitrophenyl)methyl]azaniumyl]methyl]-3,13-diazapentacyclo[11.7.0.03,11.04,9.014,19]icosa-1(20),4,6,8,10,14,16,18-octaen-10-yl]methyl-dimethyl-[(4-nitrophenyl)methyl]azaniumKi100000.0 [1]
N-[(3S)-1-Azabicyclo[2.2.2]octan-3-yl]-6-chloro-1-propan-2-ylbenzimidazole-4-carboxamideKi0.14 [1], 602.56 [2]
[20-[[Dimethyl(prop-2-enyl)azaniumyl]methyl]-3,13-diazapentacyclo[11.7.0.03,11.04,9.014,19]icosa-1(20),4,6,8,10,14,16,18-octaen-10-yl]methyl-dimethyl-prop-2-enylazaniumIC50100000.0 [1]
[20-[[Dimethyl(prop-2-enyl)azaniumyl]methyl]-3,13-diazapentacyclo[11.7.0.03,11.04,9.014,19]icosa-1(20),4,6,8,10,14,16,18-octaen-10-yl]methyl-dimethyl-prop-2-enylazaniumKi100000.0 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-Dimethyl-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneIC5031622.78 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-Dimethyl-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneKi10000.0 [1]
(1R,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-24-Phenyl-15-prop-2-enyl-10,26-dioxa-8,24,31-triaza-15-azoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneIC5031622.78 [1]
(1R,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-24-Phenyl-15-prop-2-enyl-10,26-dioxa-8,24,31-triaza-15-azoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneKi19952.62 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-24-Phenyl-15,31-bis(prop-2-enyl)-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneIC50100000.0 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-24-Phenyl-15,31-bis(prop-2-enyl)-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneKi100000.0 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-Bis[(E)-but-2-enyl]-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneIC50100000.0 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-Bis[(E)-but-2-enyl]-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneKi15848.93 [1]
2-[(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-31-(2-Acetyloxyethyl)-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaen-15-yl]ethyl acetateIC50100000.0 [1]
2-[(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-31-(2-Acetyloxyethyl)-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaen-15-yl]ethyl acetateKi100000.0 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-Di(cyclohex-2-en-1-yl)-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneIC503981.07 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-Di(cyclohex-2-en-1-yl)-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneKi2511.89 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-Dibenzyl-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneIC50100000.0 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-Dibenzyl-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneKi100000.0 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-Bis[(3,4-dimethoxyphenyl)methyl]-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneIC5031622.78 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-Bis[(3,4-dimethoxyphenyl)methyl]-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneKi25118.86 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-Bis[(4-bromophenyl)methyl]-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneIC5031622.78 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-Bis[(4-bromophenyl)methyl]-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneKi6309.57 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-Bis[(4-nitrophenyl)methyl]-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneIC50100000.0 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-Bis[(4-nitrophenyl)methyl]-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneKi25118.86 [1]
(2E)-2-[(1S,9Z,11S,13S,17R,18R,20R,27S,29R,30R,31S)-14,26-Dimethyl-19-phenyl-21-oxa-8,19-diaza-14,26-diazoniadecacyclo[24.5.2.211,14.01,27.02,7.08,31.010,18.013,17.020,30.024,29]pentatriaconta-2,4,6,9,23-pentaen-35-ylidene]ethanolIC503981.07 [1]
(2E)-2-[(1S,9Z,11S,13S,17R,18R,20R,27S,29R,30R,31S)-14,26-Dimethyl-19-phenyl-21-oxa-8,19-diaza-14,26-diazoniadecacyclo[24.5.2.211,14.01,27.02,7.08,31.010,18.013,17.020,30.024,29]pentatriaconta-2,4,6,9,23-pentaen-35-ylidene]ethanolKi6309.57 [1]
(2E)-2-[(1S,9Z,11S,13S,17R,18R,20R,27S,29R,30R,31S)-14,26-Di(cyclohex-2-en-1-yl)-19-phenyl-21-oxa-8,19-diaza-14,26-diazoniadecacyclo[24.5.2.211,14.01,27.02,7.08,31.010,18.013,17.020,30.024,29]pentatriaconta-2,4,6,9,23-pentaen-35-ylidene]ethanolIC5031622.78 [1]
(2E)-2-[(1S,9Z,11S,13S,17R,18R,20R,27S,29R,30R,31S)-14,26-Di(cyclohex-2-en-1-yl)-19-phenyl-21-oxa-8,19-diaza-14,26-diazoniadecacyclo[24.5.2.211,14.01,27.02,7.08,31.010,18.013,17.020,30.024,29]pentatriaconta-2,4,6,9,23-pentaen-35-ylidene]ethanolKi39810.72 [1]
(2E)-2-[(1S,9Z,11S,13S,17R,18R,20R,27S,29R,30R,31S)-14,26-Bis[(3,4-dimethoxyphenyl)methyl]-19-phenyl-21-oxa-8,19-diaza-14,26-diazoniadecacyclo[24.5.2.211,14.01,27.02,7.08,31.010,18.013,17.020,30.024,29]pentatriaconta-2,4,6,9,23-pentaen-35-ylidene]ethanolIC5031622.78 [1]
(2E)-2-[(1S,9Z,11S,13S,17R,18R,20R,27S,29R,30R,31S)-14,26-Bis[(3,4-dimethoxyphenyl)methyl]-19-phenyl-21-oxa-8,19-diaza-14,26-diazoniadecacyclo[24.5.2.211,14.01,27.02,7.08,31.010,18.013,17.020,30.024,29]pentatriaconta-2,4,6,9,23-pentaen-35-ylidene]ethanolKi100000.0 [1]
(2E)-2-[(1S,9Z,11S,13S,18R,20R,27S,29R,30R,31S)-14,26-Bis[(4-nitrophenyl)methyl]-19-phenyl-21-oxa-8,19-diaza-14,26-diazoniadecacyclo[24.5.2.211,14.01,27.02,7.08,31.010,18.013,17.020,30.024,29]pentatriaconta-2,4,6,9,23-pentaen-35-ylidene]ethanolIC5031622.78 [1]
(2E)-2-[(1S,9Z,11S,13S,18R,20R,27S,29R,30R,31S)-14,26-Bis[(4-nitrophenyl)methyl]-19-phenyl-21-oxa-8,19-diaza-14,26-diazoniadecacyclo[24.5.2.211,14.01,27.02,7.08,31.010,18.013,17.020,30.024,29]pentatriaconta-2,4,6,9,23-pentaen-35-ylidene]ethanolKi100000.0 [1]
(2E)-2-[(1S,9Z,11S,13S,25Z,27S,33S,35S,36S,38E)-38-(2-Hydroxyethylidene)-14,30-dimethyl-8,24-diaza-14,30-diazoniaundecacyclo[25.5.2.211,14.11,26.110,17.02,7.013,17.018,23.030,33.08,35.024,36]octatriaconta-2,4,6,9,18,20,22,25-octaen-28-ylidene]ethanolIC50100000.0 [1]
(2E)-2-[(1S,9Z,11S,13S,25Z,27S,33S,35S,36S,38E)-38-(2-Hydroxyethylidene)-14,30-dimethyl-8,24-diaza-14,30-diazoniaundecacyclo[25.5.2.211,14.11,26.110,17.02,7.013,17.018,23.030,33.08,35.024,36]octatriaconta-2,4,6,9,18,20,22,25-octaen-28-ylidene]ethanolKi100000.0 [1]
N-[(3R)-1-Azabicyclo[2.2.2]octan-3-yl]-6-chloro-1-propan-2-yl-4-benzimidazolecarboxamideKi0.14 [1], 0.54 [2]
6-Chloro-N-(8-methyl-8-azabicyclo[3.2.1]octan-3-yl)-1-propan-2-ylbenzimidazole-4-carboxamideKi1.0 [1], 19.95 [2]
RisperidoneKi1000.0 [1]
OlanzapineKi1000.0 [1]
QuetiapineKi1000.0 [1]
AripiprazoleKi1000.0 [1]
BuspironeKi10000.0 [1]
MirtazapineKi2900.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Serotonin 3a (5-HT3a) receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc.19 Nov2024https://www.aatbio.com/data-sets/serotonin-3a-5-ht3a-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024November 19). Quest Database™ Serotonin 3a (5-HT3a) receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/serotonin-3a-5-ht3a-receptor-inhibitors-ic50-ki.
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