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Neurokinin 3 receptor Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
TalnetantIC502.4 [1], 6.1 [2], 8.4 [3], 16.6 [4]
OsanetantIC500.21 [1], 0.8 [2]
SenktideIC5022.0 [1]
SenktideKi3.16 [1]
3-Methyl-2-phenyl-N-[(1S)-1-phenylpropyl]quinoline-4-carboxamideIC506.7 [1], 7.1 [2], 8.8 [3], 15.0 [4]
3-Methyl-2-phenyl-N-[(1S)-1-phenylpropyl]quinoline-4-carboxamideKi4.2 [1], 7.94 [2]
Neurokinin BIC503.0 [1], 9.7 [2], 10.0 [3], 76.0 [4]
Neurokinin BKi0.79 [1]
[(8R)-8-Methyl-3-(2-methyl-1,3-thiazol-4-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-thiophen-2-ylphenyl)methanoneIC5015.85 [1], 16.0 [2]
[(8R)-8-Methyl-3-(2-methyl-1,3-thiazol-4-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-thiophen-2-ylphenyl)methanoneKi12.59 [1], 16.0 [2]
Phenyl-[(2-phenyl-quinoline-4-carbonyl)-amino]-acetic acid methyl esterKi30.7 [1], 31.0 [2], 31.62 [3]
[(8R)-8-Methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-thiophen-2-ylphenyl)methanoneIC502.0 [1], 3.98 [2]
[(8R)-8-Methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-thiophen-2-ylphenyl)methanoneKi3.16 [1]
Tert-butyl N-[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamateIC501500.0 [1], 1550.0 [2], 1600.0 [3]
FezolinetantIC5018.0 [1], 19.95 [2]
FezolinetantKi23.0 [1], 25.12 [2]
CID 5311350IC5016.0 [1], 40.0 [2]
2-Phenyl-N-(1-phenylethyl)quinoline-4-carboxamideIC509900.0 [1]
2-Phenyl-N-(1-phenylethyl)quinoline-4-carboxamideKi251.19 [1], 264.0 [2]
N',2-Diphenylquinoline-4-carbohydrazideIC504.5 [1], 8.8 [2], 28.0 [3], 30.0 [4]
[(8R)-3-[2-(2,4-Difluorophenyl)-1,3-thiazol-4-yl]-8-methyl-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-thiophen-2-ylphenyl)methanoneIC5019.95 [1]
[(8R)-3-[2-(2,4-Difluorophenyl)-1,3-thiazol-4-yl]-8-methyl-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-thiophen-2-ylphenyl)methanoneKi2.0 [1]
[3-(2-Methyl-1,3-thiazol-4-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-thiophen-2-ylphenyl)methanoneIC5079.43 [1], 83.0 [2]
[3-(2-Methyl-1,3-thiazol-4-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-thiophen-2-ylphenyl)methanoneKi79.43 [1], 83.0 [2]
[(8R)-8-Methyl-3-(4-methyl-1,3-thiazol-2-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-thiophen-2-ylphenyl)methanoneIC507.94 [1], 8.0 [2]
[(8R)-8-Methyl-3-(4-methyl-1,3-thiazol-2-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-thiophen-2-ylphenyl)methanoneKi6.0 [1], 6.31 [2]
[(8R)-8-Methyl-3-(3-methyl-1,2,4-oxadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-thiophen-2-ylphenyl)methanoneIC5025.12 [1], 33.0 [2]
[(8R)-8-Methyl-3-(3-methyl-1,2,4-oxadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-thiophen-2-ylphenyl)methanoneKi25.12 [1], 29.0 [2]
[(8R)-8-Methyl-3-(6-methylpyridin-2-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-thiophen-2-ylphenyl)methanoneIC5010.0 [1], 11.0 [2]
[(8R)-8-Methyl-3-(6-methylpyridin-2-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-thiophen-2-ylphenyl)methanoneKi10.0 [1]
(4-Fluorophenyl)-[(8R)-8-methyl-3-[3-(trifluoromethyl)-1,2,4-thiadiazol-5-yl]-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanoneIC506.31 [1], 7.0 [2]
(4-Fluorophenyl)-[(8R)-8-methyl-3-[3-(trifluoromethyl)-1,2,4-thiadiazol-5-yl]-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanoneKi7.94 [1], 11.0 [2]
(4-Chlorophenyl)-[(8R)-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanoneIC5031.62 [1], 32.0 [2]
(4-Chlorophenyl)-[(8R)-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanoneKi19.0 [1], 19.95 [2]
(4-Fluorophenyl)-[(8R)-8-(2-hydroxyethyl)-3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanoneIC5073.0 [1], 79.43 [2]
(4-Fluorophenyl)-[(8R)-8-(2-hydroxyethyl)-3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanoneKi31.62 [1], 32.0 [2]
[(8R)-8-Methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-phenylmethanoneIC5063.1 [1], 93.0 [2]
[(8R)-8-Methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-phenylmethanoneKi50.12 [1], 60.0 [2]
(4-Fluorophenyl)-[(8R)-8-methyl-3-(3-methyl-1,2,4-oxadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanoneIC50158.49 [1], 160.0 [2]
(4-Fluorophenyl)-[(8R)-8-methyl-3-(3-methyl-1,2,4-oxadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanoneKi110.0 [1], 125.89 [2]
[(8R)-8-Methyl-3-(2-propan-2-yl-1,3-oxazol-4-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-thiophen-2-ylphenyl)methanoneIC502.0 [1], 3.98 [2]
[(8R)-8-Methyl-3-(2-propan-2-yl-1,3-oxazol-4-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-thiophen-2-ylphenyl)methanoneKi3.0 [1], 3.16 [2]
N-(alpha-Ethylbenzyl)-3-hydroxy-2-phenylquinoline-4-carboxamideKi2.4 [1], 2.51 [2]
SB 218795Ki13.0 [1], 925.0 [2]
(MePhe7)neurokinin BIC503.0 [1], 12.0 [2]
(MePhe7)neurokinin BKi0.3 [1]
2-Phenyl-N-(1-phenylpropyl)quinoline-4-carboxamideKi31.62 [1], 34.0 [2]
3-Hexyl-2-phenyl-N-(1-phenylpropyl)quinoline-4-carboxamideKi50.12 [1], 55.4 [2]
N-(2-Hydroxy-1-phenylethyl)-2-phenylquinoline-4-carboxamideKi199.53 [1], 207.0 [2]
2-Phenyl-N-(2,2,2-trifluoro-1-phenylethyl)quinoline-4-carboxamideKi454.0 [1], 501.19 [2]
3-Butyl-2-phenyl-N-(1-phenylpropyl)quinoline-4-carboxamideKi15.2 [1], 15.85 [2]
3-Methoxy-2-phenyl-N-(1-phenylpropyl)quinoline-4-carboxamideKi5.8 [1], 6.31 [2]
2-Phenyl-N-(1-phenylpropyl)-3-propylquinoline-4-carboxamideKi12.59 [1], 13.7 [2]
2-Phenyl-N-(1-phenyloctyl)quinoline-4-carboxamideKi4874.0 [1], 5011.87 [2]
N-(2-Methyl-1-phenylpropyl)-2-phenylquinoline-4-carboxamideKi74.3 [1], 79.43 [2]
3-Ethyl-2-phenyl-N-(1-phenylpropyl)quinoline-4-carboxamideKi6.31 [1], 7.1 [2]
N-[2-(Methylamino)-2-oxo-1-phenylethyl]-2-phenylquinoline-4-carboxamideKi426.0 [1], 501.19 [2]
2-Phenyl-2-[(2-phenylquinolin-4-yl)formamido]acetamideKi983.0 [1], 1000.0 [2]
N-[2-(Dimethylamino)-2-oxo-1-phenylethyl]-2-phenylquinoline-4-carboxamideKi488.0 [1], 501.19 [2]
N-(3-Hydroxy-1-phenylpropyl)-2-phenylquinoline-4-carboxamideKi382.0 [1], 398.11 [2]
2,3-Diphenyl-N-(1-phenylpropyl)quinoline-4-carboxamideKi45.3 [1], 50.12 [2]
3-Phenyl-3-[(2-phenyl-quinoline-4-carbonyl)-amino]-propionic acid methyl esterKi973.0 [1], 1000.0 [2]
N-(2-Oxo-1-phenylpropyl)-2-phenylquinoline-4-carboxamideKi25.12 [1], 27.4 [2]
N-(1,2-Diphenylethyl)-2-phenylquinoline-4-carboxamideKi3162.28 [1], 3511.0 [2]
Methyl (2R)-2-phenyl-2-[(2-phenylquinoline-4-carbonyl)amino]acetateKi13.3 [1], 926.0 [2]
2-Phenyl-N-(1-phenylbutyl)quinoline-4-carboxamideKi47.2 [1], 50.12 [2]
(3-(4-Chlorophenyl)-1-methyl-1H-pyrazol-5-yl)(4-(2-methoxyphenyl)piperazin-1-yl)methanoneIC50180.0 [1]
(3-(4-Chlorophenyl)-1-methyl-1H-pyrazol-5-yl)(4-(2-methoxyphenyl)piperazin-1-yl)methanoneKi540.0 [1]
[5-(4-Chlorophenyl)-1-methylpyrazol-3-yl]-[4-(2-methoxyphenyl)piperazin-1-yl]methanoneIC50180.0 [1]
[5-(4-Chlorophenyl)-1-methylpyrazol-3-yl]-[4-(2-methoxyphenyl)piperazin-1-yl]methanoneKi370.0 [1]
SerlopitantIC502400.0 [1]
SerlopitantKi2.4 [1]
CID 9852253Ki74.0 [1]
1-{[5-(4-Chlorophenyl)isoxazol-3-yl]carbonyl}-4-(2-methoxyphenyl)piperazineIC501100.0 [1]
1-{[5-(4-Chlorophenyl)isoxazol-3-yl]carbonyl}-4-(2-methoxyphenyl)piperazineKi1800.0 [1]
[1-(1-Carbamoyl-2-phenyl-ethylcarbamoyl)-2-(1H-indol-3-yl)-ethyl]-carbamic acid tert-butyl esterIC502080.0 [1], 3000.0 [2]
3-Methyl-2-phenyl-N-(1-phenylpropyl)quinoline-4-carboxamideKi10.0 [1]
CID 10270385Ki870.0 [1], 533000.0 [2]
2-Phenyl-N-(1-phenylpentyl)quinoline-4-carboxamideKi146.0 [1], 158.49 [2]
N',2-Diphenylquinoline-4-carbohydrazide 8mIC503.0 [1], 4.0 [2]
(2S)-N-[(4-Chlorophenyl)methyl]-2-(3,4-dichlorophenyl)-4-(6-fluoro-1-methyl-2-oxospiro[3,1-benzoxazine-4,4'-piperidine]-1'-yl)-N-methylbutanamideKi0.4 [1], 3981.07 [2]
4-[4-[Acetyl(propyl)amino]piperidin-1-yl]-2-(3,4-dichlorophenyl)-N-[(1R)-1-(4-fluorophenyl)-2-hydroxyethyl]-2-methylbutanamideKi0.5 [1], 5011.87 [2]
[(1S)-2-Methyl-1-phenylpropyl] N-[(2R)-1-[7-(carbamoylamino)heptylamino]-3-(2,3-difluorophenyl)-2-methyl-1-oxopropan-2-yl]carbamateIC507.0 [1], 7.3 [2]
N-[3-[[(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy]methyl]-3-phenylcyclobutyl]acetamideKi631.0 [1], 2131.0 [2]
[(1R)-2-Methyl-1-phenylpropyl] N-[(2R)-2-methyl-1-oxo-3-phenyl-1-[[(1S)-1-phenylethyl]amino]propan-2-yl]carbamateIC5074.0 [1]
[(1S)-2-Methyl-1-phenylpropyl] N-[(2R)-2-methyl-1-oxo-3-phenyl-1-[[(1S)-1-phenylethyl]amino]propan-2-yl]carbamateIC5010000.0 [1]
[(1R)-2-Methyl-1-phenylpropyl] N-[(2R)-1-(8-hydroxyoctylamino)-2-methyl-1-oxo-3-phenylpropan-2-yl]carbamateIC50350.0 [1]
[(1S)-2-Methyl-1-phenylpropyl] N-[(2R)-1-(8-hydroxyoctylamino)-2-methyl-1-oxo-3-phenylpropan-2-yl]carbamateIC5052.0 [1]
[(1S)-2-Methyl-1-phenylpropyl] N-[(2R)-1-[7-(carbamoylamino)heptylamino]-2-methyl-1-oxo-3-phenylpropan-2-yl]carbamateIC5043.0 [1], 57.0 [2]
2-[3,5-Bis(trifluoromethyl)phenyl]-N-[4-(4-fluoro-2-methylphenyl)-6-(4-methylsulfonylpiperazin-1-yl)pyridin-3-yl]-N,2-dimethylpropanamideKi0.7 [1], 2.4 [2]
2-[2-[4-(4-Fluorobenzoyl)piperazin-1-yl]pyrimidin-4-yl]-2-pyridin-2-ylacetonitrileIC50109.0 [1]
2-[2-[4-(4-Fluorobenzoyl)piperazin-1-yl]pyrimidin-4-yl]-2-pyridin-2-ylacetonitrileKi76.0 [1]
(4-Methoxyphenyl)-(3-pyridin-2-yl-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl)methanoneIC5031622.78 [1]
(4-Methoxyphenyl)-(3-pyridin-2-yl-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl)methanoneKi31622.78 [1]
(3-Fluorophenyl)-(3-pyridin-2-yl-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl)methanoneIC506309.57 [1]
(3-Fluorophenyl)-(3-pyridin-2-yl-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl)methanoneKi5011.87 [1]
(3-Methoxyphenyl)-(3-pyridin-2-yl-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl)methanoneIC5031622.78 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Neurokinin 3 receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc.21 Nov2024https://www.aatbio.com/data-sets/neurokinin-3-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024November 21). Quest Database™ Neurokinin 3 receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/neurokinin-3-receptor-inhibitors-ic50-ki.
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