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Serotonin 1b (5-HT1b) receptor Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
SumatriptanKi23.1 [1]
SerotoninIC505.0 [1], 6.5 [2], 12.0 [3], 16.0 [4]
SerotoninKi6.76 [1]
6-((1-(2-((2-Methylquinolin-5-yl)oxy)ethyl)piperidin-4-yl)methyl)-2H-1,4-benzoxazin-3(4H)-oneKi10.0 [1]
6-[2-[4-(2-Methylquinolin-5-yl)piperazin-1-yl]ethyl]-4H-1,4-benzoxazin-3-oneKi0.2 [1], 0.5 [2], 251.19 [3]
3-(2-Pyrrolidin-1-ylethyl)-5-(1,2,4-triazol-4-yl)-1H-indoleIC5028.0 [1], 30.2 [2]
GR-127935Ki0.14 [1], 1.0 [2], 4.31 [3]
1-(3-(5-(1,2,4-Triazol-4-yl)-1H-indol-3-yl)propyl)-4-(2-(3-fluorophenyl)ethyl)piperazineIC5072.0 [1], 75.0 [2]
3-[3-(4-Benzylpiperazino)propyl]-5-(4H-1,2,4-triazol-4-yl)-1H-indoleIC508.1 [1], 11.0 [2]
N-Benzyl-1-[(3S)-1-[2-[5-(1,2,4-triazol-4-yl)-1H-indol-3-yl]ethyl]pyrrolidin-3-yl]methanamineIC5037.0 [1], 47.0 [2]
SB 224289Ki6.31 [1], 10.0 [2]
4-Fluoro-N-[3-(1-methylpiperidin-4-yl)-1H-indol-5-yl]benzamideKi83.0 [1], 240.0 [2]
5-(4H-1,2,4-Triazole-4-yl)-3-[3-[4-(methylbenzylamino)piperidino]propyl]-1H-indoleIC50140.0 [1], 145.0 [2]
N-(3-(1-(2-(2-Methylquinolin-5-yloxy)ethyl)piperidin-4-ylmethyl)phenyl)methanesulfonamideKi2.0 [1]
8-[2-[4-(2-Methylquinolin-5-yl)piperazin-1-yl]ethyl]-4H-1,4-benzoxazin-3-oneKi1.0 [1]
4-Methyl-8-[2-[4-(2-methylquinolin-5-yl)piperazin-1-yl]ethyl]-1,4-benzoxazin-3-oneKi1.58 [1], 3.98 [2]
1-[2-[4-(6-Fluoro-1H-indol-3-yl)-3,6-dihydro-2H-pyridin-1-yl]ethyl]-3,4-dihydro-1H-isochromene-6-carboxamideKi203.0 [1], 281.0 [2]
N,N-Dimethyl-2-[5-(1,2,4-triazol-4-yl)-1H-indol-3-yl]ethanamineIC501.3 [1], 1.4 [2]
4-Methyl-6-[2-[4-(2-methylquinolin-5-yl)piperazin-1-yl]ethyl]-1,4-benzoxazin-3-oneKi0.5 [1], 2.0 [2]
Trifluoro-methanesulfonic acid 3-(2-dimethylamino-ethyl)-1H-indol-5-yl esterIC5098.0 [1]
Trifluoro-methanesulfonic acid 3-(2-dimethylamino-ethyl)-1H-indol-5-yl esterKi28.0 [1], 32.0 [2]
Trifluoro-methanesulfonic acid 3-(2-diethylamino-ethyl)-1H-indol-5-yl esterIC50530.0 [1]
Trifluoro-methanesulfonic acid 3-(2-diethylamino-ethyl)-1H-indol-5-yl esterKi37.0 [1], 171.0 [2]
Trifluoro-methanesulfonic acid 3-(2-dipropylamino-ethyl)-1H-indol-5-yl esterIC50660.0 [1]
Trifluoro-methanesulfonic acid 3-(2-dipropylamino-ethyl)-1H-indol-5-yl esterKi88.0 [1], 246.0 [2]
PropranololIC505011.87 [1]
PropranololKi10000.0 [1]
8-OH-DpatKi559.0 [1], 638.0 [2]
KetanserinIC506500.0 [1], 10000.0 [2]
ErgotamineKi2.1 [1], 3.1 [2]
TolazolineKi10000.0 [1]
RizatriptanIC5041.0 [1]
RizatriptanKi10.1 [1]
ZolmitriptanIC506.17 [1]
ZolmitriptanKi4.2 [1]
XylometazolineKi13.0 [1], 14.0 [2]
1-NaphthylpiperazineKi10.1 [1], 10.6 [2]
3-[3-(Dimethylamino)propyl]-4-hydroxy-N-(4-pyridin-4-ylphenyl)benzamideKi12.1 [1], 14.0 [2]
2-[1-(Benzenesulfonyl)-5-methoxyindol-3-yl]-N,N-dimethylethanamineKi2200.0 [1], 9210.0 [2]
N,N-Diallyl-5-methoxytryptamineKi128.82 [1], 741.31 [2]
2,6,3,5-Ethanediylidenepentaleno(1,6-bc)pyrrol-2(1H)-ol, octahydro-1-(phenylmethyl)-Ki10000.0 [1]
CID 9870500Ki3.98 [1], 7.94 [2]
ThalictruberineKi100.0 [1]
CID 9847194IC50150.0 [1], 185.0 [2]
N,N-Dipropyl-6,7,8,9-tetrahydro-3H-benzo[e]indol-8-amineKi349.0 [1]
Dipropyl-(S)-6,7,8,9-tetrahydro-3H-benzo[e]indol-8-yl-amineKi2275.0 [1]
Dipropyl-(R)-6,7,8,9-tetrahydro-3H-benzo[e]indol-8-yl-amineKi139.0 [1]
5-(4H-1,2,4-Triazole-4-yl)-3-[3-(4-benzylpiperidino)propyl]-1H-indoleIC5019.0 [1]
5-Chloro-N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]-3-methyl-1-benzothiophene-2-sulfonamideKi794.33 [1]
3-[3-(4-Fluoro-4-benzylpiperidino)propyl]-5-(4H-1,2,4-triazole-4-yl)-1H-indoleIC5015.0 [1]
2-Methyl-5-(2-(4-(quinolin-8-ylmethyl)piperazin-1-yl)ethoxy)quinolineKi199.53 [1]
2-(2,6-Dimethyl-benzyl)-4,5-dihydro-1H-imidazoleKi10000.0 [1]
3-(3-Dimethylamino-propyl)-4-methoxy-N-(4-pyridin-4-yl-phenyl)-benzamideKi15.4 [1], 70.1 [2]
2-(Dimethylamino)-N-[3-[[1-[2-(2-methylquinolin-5-yl)oxyethyl]piperidin-4-yl]methyl]phenyl]acetamideKi6.31 [1]
N-Benzyl-N-methyl-1-[(3S)-1-[2-[5-(1,2,4-triazol-4-yl)-1H-indol-3-yl]ethyl]pyrrolidin-3-yl]methanamineIC5032.0 [1], 33.0 [2]
3-[3-[4-(2-Fluorophenethyl)piperazino]propyl]-5-(4H-1,2,4-triazol-4-yl)-1H-indoleIC5098.0 [1], 100.0 [2]
3-[3-[4-(4-Fluorophenethyl)piperazino]propyl]-5-(4H-1,2,4-triazol-4-yl)-1H-indoleIC50120.0 [1]
Benzyl-{1-[3-(5-[1,2,4]triazol-4-yl-1H-indol-3-yl)-propyl]-piperidin-4-yl}-amineIC50120.0 [1], 125.0 [2]
3-[2-(4-Methylpiperazino)ethyl]-5-(4H-1,2,4-triazol-4-yl)-1H-indoleIC50304.0 [1], 310.0 [2]
(3R)-N-Benzyl-N-methyl-1-[2-[5-(1,2,4-triazol-4-yl)-1H-indol-3-yl]ethyl]pyrrolidin-3-amineIC50209.0 [1], 210.0 [2]
3-[3-(4-Phenethylpiperazino)propyl]-5-(4H-1,2,4-triazol-4-yl)-1H-indoleIC50166.0 [1], 170.0 [2]
(R)-beta-[[1-[3-[5-(4H-1,2,4-Triazol-4-yl)-1H-indol-3-yl]propyl]piperidin-4-yl]amino]benzeneethanolIC50110.0 [1], 114.0 [2]
3-(3-Piperidinopropyl)-5-(4H-1,2,4-triazol-4-yl)-1H-indoleIC5015.0 [1]
3-[2-((R)-3-Benzyloxymethyl-pyrrolidin-1-yl)-ethyl]-5-[1,2,4]triazol-4-yl-1H-indoleIC5085.0 [1], 88.0 [2]
N-[(1R)-1-Phenylethyl]-1-[3-[5-(1,2,4-triazol-4-yl)-1H-indol-3-yl]propyl]piperidin-4-amineIC5035.0 [1]
N-Benzyl-N-methyl-1-[1-[3-[5-(1,2,4-triazol-4-yl)-1H-indol-3-yl]propyl]piperidin-4-yl]methanamineIC5027.0 [1], 28.0 [2]
[2-(5-Ethyl-1H-indol-3-yl)-ethyl]-dimethyl-amineKi5.5 [1], 286.0 [2]
Benzyl-{(R)-1-[2-(5-[1,2,4]triazol-4-yl-1H-indol-3-yl)-ethyl]-pyrrolidin-3-ylmethyl}-amineIC5047.0 [1], 50.0 [2]
N-[4-[2-[4-[3-[5-(1,2,4-Triazol-4-yl)-1H-indol-3-yl]propyl]piperazin-1-yl]ethyl]phenyl]acetamideIC50251.0 [1], 260.0 [2]
2-(5-((4-((3-(2-Aminoethyl)-1H-indol-5-yloxy)methyl)phenyl)methoxy)-1H-indol-3-yl)ethanamineKi0.1 [1]
2-(5-(2-(8-(4-Methylpiperazin-1-yl)naphthalen-2-yloxy)ethoxy)-1H-indol-3-yl)ethanamineKi0.76 [1]
3-(2-Piperidinoethyl)-5-(4H-1,2,4-triazol-4-yl)-1H-indoleIC50568.0 [1], 570.0 [2]
3-[3-[4-(3,4-Difluorophenethyl)piperazino]propyl]-5-(4H-1,2,4-triazol-4-yl)-1H-indoleIC5083.0 [1], 98.0 [2]
5-(2-Pyridin-2-ylethyl)-5-azahexacyclo[5.4.1.02,6.03,10.04,8.09,12]dodecan-4-olKi956.0 [1]
2-(4-Bromo-2,6-dimethyl-benzyl)-4,5-dihydro-1H-imidazoleKi1570.0 [1]
1-Methyl-2-(2,6-dimethyl-4-tert-butylbenzyl)-2-imidazolineKi5000.0 [1]
1-[3-[2-(Dimethylamino)ethyl]-1H-indol-5-yl]-N-[[4-[[[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methylsulfonyl-methylamino]methyl]phenyl]methyl]-N-methylmethanesulfonamideKi0.64 [1]
N,N-Dimethyl-2-(5-(1-methyl-3,6-dihydro-2H-pyridin-4-yl)-1H-indol-3-yl)ethanamineKi610.0 [1]
3-[2-((R)-3-Benzyloxy-pyrrolidin-1-yl)-ethyl]-5-[1,2,4]triazol-4-yl-1H-indoleIC50145.0 [1], 280.0 [2]
3-[3-(4-Methylpiperazino)propyl]-5-(4H-1,2,4-triazol-4-yl)-1H-indoleIC50309.0 [1], 430.0 [2]
(4S)-4-[[3-[2-[(3S)-3-[(Benzylamino)methyl]pyrrolidin-1-yl]ethyl]-1H-indol-5-yl]methyl]-1,3-oxazolidin-2-oneIC5049.0 [1]
N-[4-Methoxy-3-(4-methylpiperazin-1-yl)phenyl]-4-(2-methoxyphenyl)piperazine-1-carboxamideKi2.0 [1], 12.4 [2]
3-[(Z)-3-(Dimethylamino)prop-1-enyl]-4-methoxy-N-(4-pyridin-4-ylphenyl)benzamideKi6.1 [1], 19.0 [2]
Trifluoromethanesulfonic acid 3-(2-aminoethyl)-1H-indol-5-yl esterKi14.0 [1], 18.0 [2]
3-((E)-3-Dimethylamino-propenyl)-4-methoxy-N-(4-pyridin-4-yl-phenyl)-benzamideKi13.6 [1], 18.8 [2]
3-(3-Dimethylamino-prop-1-ynyl)-4-methoxy-N-(4-pyridin-4-yl-phenyl)-benzamideKi16.2 [1], 22.3 [2]
(4S)-4-[[3-[2-[(3S)-3-[[[(1S)-1-Phenylethyl]amino]methyl]pyrrolidin-1-yl]ethyl]-1H-indol-5-yl]methyl]-1,3-oxazolidin-2-oneIC5049.0 [1], 50.0 [2]
[(4S,5S)-2-(4-Butoxyphenyl)-5-methyl-4,5-dihydro-1,3-thiazol-4-yl]methanolIC502100.0 [1]
[(4S,5S)-2-(4-Butoxyphenyl)-5-methyl-4,5-dihydro-1,3-thiazol-4-yl]methanolKi10000.0 [1]
[(4S,5S)-2-(4-Hexoxyphenyl)-5-methyl-4,5-dihydro-1,3-thiazol-4-yl]methanolIC501900.0 [1]
[(4S,5S)-2-(4-Hexoxyphenyl)-5-methyl-4,5-dihydro-1,3-thiazol-4-yl]methanolKi10000.0 [1]
1-[3-[2-[(3S)-3-[(Benzylamino)methyl]pyrrolidin-1-yl]ethyl]-1H-indol-5-yl]-N-methylmethanesulfonamideIC5062.0 [1]
8-[4-(5-Methoxyspiro[2,4-dihydrochromene-3,2'-pyrrolidine]-1'-yl)butyl]-8-azaspiro[4.5]decane-7,9-dioneIC503801.89 [1], 6606.93 [2]
ClozapineKi1000.0 [1]
RisperidoneKi10.0 [1]
OlanzapineKi1000.0 [1]
PrazosinKi7700.0 [1]
QuetiapineKi1000.0 [1]
AripiprazoleKi1000.0 [1]
PindololKi10000.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Serotonin 1b (5-HT1b) receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc.21 Dec2024https://www.aatbio.com/data-sets/serotonin-1b-5-ht1b-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024December 21). Quest Database™ Serotonin 1b (5-HT1b) receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/serotonin-1b-5-ht1b-receptor-inhibitors-ic50-ki.
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