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Proteinase-activated receptor 1 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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VorapaxarIC501.5 [1], 25.0 [2], 47.0 [3], 64.0 [4], 120.0 [5]
VorapaxarKi1.1 [1], 8.0 [2], 8.1 [3], 8.5 [4], 13.0 [5]
(3R,3As,4S,4aR,8aS,9aR)-3-methyl-4-[(E)-2-[5-[3-(trifluoromethyl)phenyl]pyridin-2-yl]ethenyl]-3a,4,4a,5,6,7,8,8a,9,9a-decahydro-3H-benzo[f][2]benzofuran-1-oneIC5011.0 [1], 24.0 [2]
(3R,3As,4S,4aR,8aS,9aR)-3-methyl-4-[(E)-2-[5-[3-(trifluoromethyl)phenyl]pyridin-2-yl]ethenyl]-3a,4,4a,5,6,7,8,8a,9,9a-decahydro-3H-benzo[f][2]benzofuran-1-oneKi2.7 [1]
(2S)-N-Benzyl-5-(diaminomethylideneamino)-2-[[(2S)-2-[[1-[(2,6-dichlorophenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-6-yl]carbamoylamino]-3-(4-methoxyphenyl)propanoyl]amino]pentanamideIC50300.0 [1], 900.0 [2], 1300.0 [3]
(2S)-N-Benzyl-5-(diaminomethylideneamino)-2-[[(2S)-2-[[1-[(4-fluorophenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-6-yl]carbamoylamino]-3-(4-methoxyphenyl)propanoyl]amino]pentanamideIC50270.0 [1], 2200.0 [2], 2320.0 [3]
(3R,3As,4S,4aR,8aS,9aR)-4-[(E)-2-(6-ethylpyridin-2-yl)ethenyl]-3-methyl-3a,4,4a,5,6,7,8,8a,9,9a-decahydro-3H-benzo[f][2]benzofuran-1-oneIC5070.0 [1], 85.0 [2]
(3R,3As,4S,4aR,8aS,9aR)-4-[(E)-2-(6-ethylpyridin-2-yl)ethenyl]-3-methyl-3a,4,4a,5,6,7,8,8a,9,9a-decahydro-3H-benzo[f][2]benzofuran-1-oneKi12.0 [1]
(2S)-N-Benzyl-5-(diaminomethylideneamino)-2-[[(2S)-2-[[1-[(2,6-dichlorophenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-6-yl]carbamoylamino]-3-(3,4-difluorophenyl)propanoyl]amino]pentanamideIC50180.0 [1], 570.0 [2], 820.0 [3]
3-{5-[(3-Azepan-1-yl-propyl)-benzo[1,3]dioxol-5-ylmethyl-amino]-isoxazol-3-yl}-benzonitrileIC50350.0 [1], 600.0 [2], 1970.0 [3]
(3-Azepan-1-yl-propyl)-benzo[1,3]dioxol-5-ylmethyl-[3-(3-nitro-phenyl)-isoxazol-5-yl]-amineIC50830.0 [1], 1020.0 [2], 10000.0 [3]
(3-Azepan-1-yl-propyl)-benzo[1,3]dioxol-5-ylmethyl-[3-(3-methoxy-phenyl)-isoxazol-5-yl]-amineIC50130.0 [1], 260.0 [2], 2240.0 [3]
(3-Azepan-1-yl-propyl)-benzo[1,3]dioxol-5-ylmethyl-[3-(3-chloro-phenyl)-isoxazol-5-yl]-amineIC50270.0 [1], 910.0 [2], 1160.0 [3]
(3-Azepan-1-yl-propyl)-benzo[1,3]dioxol-5-ylmethyl-[3-(4-chloro-phenyl)-isoxazol-5-yl]-amineIC50990.0 [1], 1240.0 [2], 4250.0 [3]
(3-Azepan-1-yl-propyl)-benzo[1,3]dioxol-5-ylmethyl-[3-(3-fluoro-phenyl)-isoxazol-5-yl]-amineIC50140.0 [1], 770.0 [2], 1180.0 [3]
(2S)-N-Benzyl-2-[[(2S)-3-(4-cyanophenyl)-2-[[1-[(2-methylphenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-6-yl]carbamoylamino]propanoyl]amino]-5-(diaminomethylideneamino)pentanamideIC50600.0 [1], 620.0 [2], 6400.0 [3]
(2S)-N-Benzyl-5-(diaminomethylideneamino)-2-[[(2S)-2-[[1-[(2-methylphenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-6-yl]carbamoylamino]-3-(4-nitrophenyl)propanoyl]amino]pentanamideIC50150.0 [1], 800.0 [2], 1300.0 [3]
(2S)-N-Benzyl-5-(diaminomethylideneamino)-2-[[(2S)-2-[[1-[(4-fluorophenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-6-yl]carbamoylamino]-3-(4-nitrophenyl)propanoyl]amino]pentanamideIC50130.0 [1], 1100.0 [2], 6100.0 [3]
(2S)-5-(Diaminomethylideneamino)-2-[[(2S)-3-(4-methoxyphenyl)-2-[[1-[(2-methylphenyl)methyl]-3-(piperidin-1-ylmethyl)indol-6-yl]carbamoylamino]propanoyl]amino]-N-(3-phenylpropyl)pentanamideIC50310.0 [1], 730.0 [2], 4800.0 [3]
(2S)-5-(Diaminomethylideneamino)-2-[[(2S)-2-[[3-(diethylaminomethyl)-1-[(2-methylphenyl)methyl]indol-6-yl]carbamoylamino]-3-(4-methoxyphenyl)propanoyl]amino]-N-(3-phenylpropyl)pentanamideIC50230.0 [1], 2500.0 [2], 3000.0 [3]
(2S)-5-(Diaminomethylideneamino)-2-[[(2S)-3-(4-methoxyphenyl)-2-[[1-[(2-methylphenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-6-yl]carbamoylamino]propanoyl]amino]-N-(3-phenylpropyl)pentanamideIC50200.0 [1], 1000.0 [2]
(2S)-5-(Diaminomethylideneamino)-2-[[(2S)-2-[[3-(diethylaminomethyl)-1-[(3-methylphenyl)methyl]indol-6-yl]carbamoylamino]-3-(4-methoxyphenyl)propanoyl]amino]-N-(3-phenylpropyl)pentanamideIC50210.0 [1], 1300.0 [2], 2600.0 [3]
(2S)-2-[[(2S)-2-[[1-[(2-Chlorophenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-6-yl]carbamoylamino]-3-(4-methoxyphenyl)propanoyl]amino]-5-(diaminomethylideneamino)-N-(3-phenylpropyl)pentanamideIC50140.0 [1], 380.0 [2], 2600.0 [3]
(2S)-N-Benzyl-2-[[(2S)-3-(4-cyanophenyl)-2-[[1-[(2,6-dichlorophenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-6-yl]carbamoylamino]propanoyl]amino]-5-(diaminomethylideneamino)pentanamideIC5070.0 [1], 480.0 [2], 5300.0 [3]
(2S)-N-(Cyclohexylmethyl)-5-(diaminomethylideneamino)-2-[[(2S)-2-[[1-[(4-fluorophenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-6-yl]carbamoylamino]-3-(4-methoxyphenyl)propanoyl]amino]pentanamideIC50640.0 [1], 2600.0 [2], 4400.0 [3]
(2S)-5-Amino-N-benzyl-2-[[(2S)-2-[[1-[(2,6-dichlorophenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-6-yl]carbamoylamino]-3-(3,4-difluorophenyl)propanoyl]amino]pentanamideIC50100.0 [1], 500.0 [2], 600.0 [3]
(2S)-2-[[(2S)-2-[[3-(Azetidin-1-ylmethyl)-1-[(4-fluorophenyl)methyl]indol-6-yl]carbamoylamino]-3-(4-methoxyphenyl)propanoyl]amino]-N-benzyl-5-(diaminomethylideneamino)pentanamideIC50400.0 [1], 3300.0 [2], 9700.0 [3]
(2S)-N-(Cyclohexylmethyl)-5-(diaminomethylideneamino)-2-[[(2S)-3-(4-methoxyphenyl)-2-[[3-(piperidin-1-ylmethyl)-1-[[4-(trifluoromethoxy)phenyl]methyl]indol-6-yl]carbamoylamino]propanoyl]amino]pentanamideIC505600.0 [1], 6400.0 [2], 36500.0 [3]
(2S)-N-(Cyclohexylmethyl)-5-(diaminomethylideneamino)-2-[[(2S)-3-(4-methoxyphenyl)-2-[[3-(pyrrolidin-1-ylmethyl)-1-[[4-(trifluoromethoxy)phenyl]methyl]indol-6-yl]carbamoylamino]propanoyl]amino]pentanamideIC502500.0 [1], 4800.0 [2], 40300.0 [3]
N-Benzyl-2-[[(2S)-2-[[1-[(2,6-dichlorophenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-6-yl]carbamoylamino]-3-(3,4-difluorophenyl)propanoyl]amino]-4-methylsulfanylbutanamideIC50400.0 [1], 10700.0 [2], 11200.0 [3]
(2S)-N-(Cyclohexylmethyl)-5-(diaminomethylideneamino)-2-[[(2S)-2-[[3-(diethylaminomethyl)-1-[(4-fluorophenyl)methyl]indol-6-yl]carbamoylamino]-3-(4-methoxyphenyl)propanoyl]amino]pentanamideIC50900.0 [1], 3100.0 [2], 11100.0 [3]
N-Benzyl-2-[[(2S)-2-[[1-[(2,6-dichlorophenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-6-yl]carbamoylamino]-3-(3,4-difluorophenyl)propanoyl]amino]pentanediamideIC501800.0 [1], 2000.0 [2], 7900.0 [3]
N-Benzyl-5-(carbamoylamino)-2-[[(2S)-2-[[1-[(2,6-dichlorophenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-6-yl]carbamoylamino]-3-(3,4-difluorophenyl)propanoyl]amino]pentanamideIC50240.0 [1], 300.0 [2], 1900.0 [3]
(2S)-N-[1-(Benzylamino)-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-2-[[1-[(2,6-dichlorophenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-6-yl]carbamoylamino]-3-(3,4-difluorophenyl)propanamideIC50200.0 [1], 460.0 [2], 1300.0 [3]
(2S)-5-(Diaminomethylideneamino)-2-[[(2S)-2-[[1-[(4-fluorophenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-6-yl]carbamoylamino]-3-(4-methoxyphenyl)propanoyl]amino]-N-(3-phenylpropyl)pentanamideIC50600.0 [1], 1300.0 [2], 8500.0 [3]
(2S)-N-[3-Amino-1-(benzylamino)-1-oxopropan-2-yl]-2-[[1-[(2,6-dichlorophenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-6-yl]carbamoylamino]-3-(3,4-difluorophenyl)propanamideIC50500.0 [1], 900.0 [2], 920.0 [3]
4-Amino-N-benzyl-2-[[(2S)-2-[[1-[(2,6-dichlorophenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-6-yl]carbamoylamino]-3-(3,4-difluorophenyl)propanoyl]amino]butanamideIC50160.0 [1], 340.0 [2], 440.0 [3]
(2S)-6-Amino-N-benzyl-2-[[(2S)-2-[[1-[(2,6-dichlorophenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-6-yl]carbamoylamino]-3-(3,4-difluorophenyl)propanoyl]amino]hexanamideIC50100.0 [1], 300.0 [2], 700.0 [3]
(2S)-N-(Cyclohexylmethyl)-5-(diaminomethylideneamino)-2-[[(2S)-3-(4-methoxyphenyl)-2-[[1-[(3-methylphenyl)methyl]-3-(piperidin-1-ylmethyl)indol-6-yl]carbamoylamino]propanoyl]amino]pentanamideIC50900.0 [1], 3200.0 [2], 11700.0 [3]
(2S)-N-(Cyclohexylmethyl)-5-(diaminomethylideneamino)-2-[[(2S)-2-[[1-[(4-fluorophenyl)methyl]-3-(piperidin-1-ylmethyl)indol-6-yl]carbamoylamino]-3-(4-methoxyphenyl)propanoyl]amino]pentanamideIC501000.0 [1], 2300.0 [2], 23800.0 [3]
N-[3-(Azepan-1-yl)propyl]-N-(1,3-benzodioxol-5-ylmethyl)-3-(3,4-difluorophenyl)-1,2-oxazol-5-amineIC50500.0 [1], 2140.0 [2], 2400.0 [3]
(3-Azepan-1-yl-propyl)-benzo[1,3]dioxol-5-ylmethyl-[3-(4-iodo-phenyl)-isoxazol-5-yl]-amineIC5090.0 [1], 470.0 [2], 880.0 [3]
N-[3-(Azepan-1-yl)propyl]-N-(1,3-benzodioxol-5-ylmethyl)-3-(3,5-dimethoxyphenyl)-1,2-oxazol-5-amineIC50130.0 [1], 520.0 [2], 1200.0 [3]
N-[3-(Azepan-1-yl)propyl]-N-(1,3-benzodioxol-5-ylmethyl)-3-(3,4-dimethoxyphenyl)-1,2-oxazol-5-amineIC50400.0 [1], 1200.0 [2], 4670.0 [3]
(3-Azepan-1-yl-propyl)-benzo[1,3]dioxol-5-ylmethyl-(3-p-tolyl-isoxazol-5-yl)-amineIC50140.0 [1], 290.0 [2], 3200.0 [3]
N-[(1R,3As,7aS)-1-[(E)-2-[5-(3-fluorophenyl)pyridin-2-yl]ethenyl]-2,3,3a,4,5,6,7,7a-octahydro-1H-inden-2-yl]-N-methylmethanesulfonamideIC501.3 [1], 2.2 [2], 97.0 [3]
N-[(1R,3As,7aS)-1-[(E)-2-[5-(3-fluorophenyl)pyridin-2-yl]ethenyl]-2,3,3a,4,5,6,7,7a-octahydro-1H-inden-2-yl]-N-methylacetamideIC505.4 [1], 210.0 [2], 8900.0 [3]
(1R,3As,7aS)-1-[(E)-2-[5-(3-fluorophenyl)pyridin-2-yl]ethenyl]spiro[1,3,3a,4,5,6,7,7a-octahydroindene-2,5'-1,3-oxazolidine]-2'-oneIC507.2 [1], 8.6 [2], 210.0 [3]
2-[(E)-2-[(1R,3As,7aS)-spiro[1,3,3a,4,5,6,7,7a-octahydroindene-2,2'-1,3-dioxolane]-1-yl]ethenyl]-5-(3-fluorophenyl)pyridineIC5026.0 [1], 410.0 [2], 4100.0 [3]
N-[(1R,3As,7aS)-1-[(E)-2-[5-(3-fluorophenyl)pyridin-2-yl]ethenyl]-2,3,3a,4,5,6,7,7a-octahydro-1H-inden-2-yl]methanesulfonamideIC5050.0 [1], 140.0 [2], 3900.0 [3]
[(1R,3As,7aS)-1-[(E)-2-[5-(3-fluorophenyl)pyridin-2-yl]ethenyl]-2-methyl-1,3,3a,4,5,6,7,7a-octahydroinden-2-yl] carbamateIC502.7 [1], 2.9 [2], 100.0 [3]
N-[3-(Azepan-1-yl)propyl]-N-(1,3-benzodioxol-5-ylmethyl)-3-(3,5-difluorophenyl)-1,2-oxazol-5-amineIC5090.0 [1], 150.0 [2], 510.0 [3]
N3-Cyclopropyl-7-[(4-propan-2-ylphenyl)methyl]pyrrolo[3,2-f]quinazoline-1,3-diamineIC5056.0 [1]
(2S)-N-[(2S)-1-[[(2S)-1-Amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-[[(2S)-3-[4-(diaminomethylideneamino)phenyl]-2-[[(2S)-3-(4-fluorophenyl)-2-[[(E)-3-phenylprop-2-enoyl]amino]propanoyl]amino]propanoyl]amino]-4-methylpentanamideIC507.5 [1], 300.0 [2]
TRAP-6 amideIC50550.0 [1], 73000.0 [2]
Unii-7467O90MW3IC50180.0 [1]
Unii-7467O90MW3Ki19.0 [1]
3-N-Cyclopropyl-3-N-methyl-7-[(4-propan-2-ylphenyl)methyl]pyrrolo[3,2-f]quinazoline-1,3-diamineIC5052.0 [1]
(3R,3As,4S,4aR,8aS,9aR)-3-methyl-4-[(E)-2-(6-methylpyridin-2-yl)ethenyl]-3a,4,4a,5,6,7,8,8a,9,9a-decahydro-3H-benzo[f][2]benzofuran-1-oneIC50150.0 [1], 300.0 [2]
7-(4-Isopropylbenzyl)-7H-pyrrolo[3,2-f]quinazoline-1,3-diamineIC50300.0 [1]
(3R,3As,4S,4aR,8aS,9aR)-3-methyl-4-[(E)-2-quinolin-2-ylethenyl]-3a,4,4a,5,6,7,8,8a,9,9a-decahydro-3H-benzo[f][2]benzofuran-1-oneIC5060.0 [1], 100.0 [2]
(3R,3As,4S,4aR,8aS,9aR)-4-[(E)-2-(6-methoxyquinolin-2-yl)ethenyl]-3-methyl-3a,4,4a,5,6,7,8,8a,9,9a-decahydro-3H-benzo[f][2]benzofuran-1-oneIC5015.0 [1], 620.0 [2]
(1R,3Ar,8aS,9S,9aS)-1-methyl-9-[(E)-2-quinolin-2-ylethenyl]-3a,5,6,7,8,8a,9,9a-octahydro-1H-benzo[f][2]benzofuran-3-oneIC50150.0 [1]
(3R,3As,4S,4aR,8aS,9aR)-3-methyl-4-[(E)-2-(5-phenylpyridin-2-yl)ethenyl]-3a,4,4a,5,6,7,8,8a,9,9a-decahydro-3H-benzo[f][2]benzofuran-1-oneIC5027.0 [1]
(3-Azepan-1-yl-propyl)-benzo[1,3]dioxol-5-ylmethyl-[3-(4-methylsulfanyl-phenyl)-isoxazol-5-yl]-amineIC50430.0 [1], 4000.0 [2]
N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-Amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-[4-(diaminomethylideneamino)phenyl]-1-oxopropan-2-yl]amino]-3-(4-fluorophenyl)-1-oxopropan-2-yl]-1H-indole-3-carboxamideIC5019.0 [1], 2000.0 [2]
(2S)-N-[(2S)-1-Amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-[[(2S)-3-[4-(diaminomethylideneamino)phenyl]-2-[[(2S)-3-(4-fluorophenyl)-2-(thiophen-2-ylsulfonylamino)propanoyl]amino]propanoyl]amino]-4-methylpentanamideIC508950.0 [1], 193000.0 [2]
2-Methoxy-6-[1-methyl-5-(trifluoromethoxy)indol-2-yl]imidazo[2,1-b][1,3,4]thiadiazoleIC5010000.0 [1]
Methyl 4-[[6-[[(2S)-1-[[(2S)-1-(cyclohexylmethylamino)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-(4-methoxyphenyl)-1-oxopropan-2-yl]carbamoylamino]-3-(pyrrolidin-1-ylmethyl)indol-1-yl]methyl]benzoateIC503500.0 [1], 38700.0 [2]
N-[3-(Azepan-1-yl)propyl]-N-(1,3-benzodioxol-5-ylmethyl)-3-(3-fluoro-4-methoxyphenyl)-1,2-oxazol-5-amineIC5070.0 [1], 2140.0 [2]
(3-Azepan-1-yl-propyl)-benzo[1,3]dioxol-5-ylmethyl-[3-(2-methoxy-phenyl)-isoxazol-5-yl]-amineIC502210.0 [1], 2220.0 [2]
(3-Azepan-1-yl-propyl)-benzo[1,3]dioxol-5-ylmethyl-(3-m-tolyl-isoxazol-5-yl)-amineIC50120.0 [1], 890.0 [2]
(3-Azepan-1-yl-propyl)-benzo[1,3]dioxol-5-ylmethyl-[3-(4-fluoro-phenyl)-isoxazol-5-yl]-amineIC501310.0 [1], 10000.0 [2]
(3-Azepan-1-yl-propyl)-benzo[1,3]dioxol-5-ylmethyl-[3-(4-methoxy-phenyl)-isoxazol-5-yl]-amineIC50130.0 [1], 250.0 [2]
[(1R,3As,7aS)-1-[(E)-2-[5-(3-fluorophenyl)pyridin-2-yl]ethenyl]-2,3,3a,4,5,6,7,7a-octahydro-1H-inden-2-yl] methanesulfonateIC506.0 [1], 6.4 [2]
N-Acetyl-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-[4-(diaminomethylideneamino)phenyl]-1-oxopropan-2-yl]amino]-3-(4-fluorophenyl)-1-oxopropan-2-yl]-2-prop-1-ynylbenzamideIC5023.0 [1], 280.0 [2]
(2S)-2-[[(2S)-2-[[(2S)-2-[Acetyl-[(E)-3-(4-fluorophenyl)prop-2-enoyl]amino]-3-(4-fluorophenyl)propanoyl]amino]-3-[4-(diaminomethylideneamino)phenyl]propanoyl]amino]-N-[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-methylpentanamideIC5020.0 [1], 90.0 [2]
N-Acetyl-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-[4-(diaminomethylideneamino)phenyl]-1-oxopropan-2-yl]amino]-3-(4-fluorophenyl)-1-oxopropan-2-yl]-4-phenylbenzamideIC5046.0 [1], 430.0 [2]
(2S)-2-[[(2S)-2-[[(2S)-2-[Acetyl-[(E)-3-(4-methoxyphenyl)prop-2-enoyl]amino]-3-(4-fluorophenyl)propanoyl]amino]-3-[4-(diaminomethylideneamino)phenyl]propanoyl]amino]-N-[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-methylpentanamideIC5040.0 [1], 390.0 [2]
(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[Acetyl-[(E)-3-phenylprop-2-enoyl]amino]-3-(4-fluorophenyl)propanoyl]amino]-3-[4-(diaminomethylideneamino)phenyl]propanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-8-amino-4-oxooctanamideIC5021.9 [1], 85.0 [2]
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[Acetyl-[(E)-3-phenylprop-2-enoyl]amino]-3-(4-fluorophenyl)propanoyl]amino]-3-[4-(diaminomethylideneamino)phenyl]propanoyl]amino]-4-methylpentanoyl]amino]-7-amino-3-oxoheptanamideIC5044.0 [1], 250.0 [2]
(2S)-2-[[(2S)-2-[[(2S)-2-[Acetyl-[(E)-3-phenylprop-2-enoyl]amino]-3-(4-fluorophenyl)propanoyl]amino]-3-[4-(diaminomethylideneamino)phenyl]propanoyl]amino]-N-[(2S)-1,5-diamino-1-oxopentan-2-yl]-4-methylpentanamideIC5017.0 [1], 190.0 [2]
(2S)-2-[[(2S)-2-[[(2S)-2-[Acetyl-[(E)-3-phenylprop-2-enoyl]amino]-3-(4-fluorophenyl)propanoyl]amino]-3-[4-(diaminomethylideneamino)phenyl]propanoyl]amino]-5-aminopentanamideIC50870.0 [1], 141000.0 [2]
(2S)-2-[[(2S)-2-[[(2S)-2-[Acetyl(thiophen-2-yl)amino]-3-(4-fluorophenyl)propanoyl]amino]-3-[4-(diaminomethylideneamino)phenyl]propanoyl]amino]-N-[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-methylpentanamideIC50260.0 [1], 32000.0 [2]
(2S)-2-[[(2S)-2-[[(2S)-2-[Acetyl-[(E)-3-(3-chlorophenyl)prop-2-enoyl]amino]-3-(4-fluorophenyl)propanoyl]amino]-3-[4-(diaminomethylideneamino)phenyl]propanoyl]amino]-N-[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-methylpentanamideIC5041.0 [1], 80.0 [2]
(2S)-2-[[(2S)-2-[[(2S)-2-[Acetyl(1H-indol-3-yl)amino]-3-(4-fluorophenyl)propanoyl]amino]-3-[4-(diaminomethylideneamino)phenyl]propanoyl]amino]-N-[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-methylpentanamideIC50500.0 [1], 54000.0 [2]
(2S)-2-[[(2S)-2-[[(2S)-2-[Acetyl(cyclopentyl)amino]-3-(4-fluorophenyl)propanoyl]amino]-3-[4-(diaminomethylideneamino)phenyl]propanoyl]amino]-N-[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-methylpentanamideIC50370.0 [1], 85000.0 [2]
(2S)-2-[[(2S)-2-[[(2S)-2-[Acetyl-[(E)-3-phenylprop-2-enoyl]amino]-3-(4-fluorophenyl)propanoyl]amino]-3-[4-(diaminomethylideneamino)phenyl]propanoyl]amino]-4-methylpentanamideIC50110.0 [1], 4050.0 [2]
(2S)-2-[[(2S)-2-[Acetyl-[(E)-3-phenylprop-2-enoyl]amino]-3-(4-fluorophenyl)propanoyl]amino]-3-[4-(diaminomethylideneamino)phenyl]propanamideIC50780.0 [1], 64000.0 [2]
(2S)-2-[[(2S)-2-[[(2S)-2-[Acetyl-[(E)-3-(4-methylphenyl)prop-2-enoyl]amino]-3-(4-fluorophenyl)propanoyl]amino]-3-[4-(diaminomethylideneamino)phenyl]propanoyl]amino]-N-[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-methylpentanamideIC5043.0 [1], 8330.0 [2]
(2S)-2-[[(2S)-2-[[(2S)-2-[Acetyl-[(E)-3-(4-chlorophenyl)prop-2-enoyl]amino]-3-(4-fluorophenyl)propanoyl]amino]-3-[4-(diaminomethylideneamino)phenyl]propanoyl]amino]-N-[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-methylpentanamideIC5099.0 [1], 240.0 [2]
(E)-N-Acetyl-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-[4-(diaminomethylideneamino)phenyl]-1-oxopropan-2-yl]amino]-3-(4-fluorophenyl)-1-oxopropan-2-yl]non-3-enamideIC5035.0 [1], 7600.0 [2]
(2S)-2-[[(2S)-2-[[(2S)-2-[Acetyl-[(E)-3-phenylprop-2-enoyl]amino]-3-(4-fluorophenyl)propanoyl]amino]-3-(4-methoxyphenyl)propanoyl]amino]-N-[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-methylpentanamideIC501180.0 [1], 300000.0 [2]
(2S)-2-[[(2R)-2-[[(2S)-2-[Acetyl-[(E)-3-phenylprop-2-enoyl]amino]-3-(4-fluorophenyl)propanoyl]amino]-5-[bis(dimethylamino)methylideneamino]pentanoyl]amino]-N-[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-methylpentanamideIC50320.0 [1], 16000.0 [2]
(2S)-2-[[(2S)-2-[[(2S)-2-[Acetyl-[(E)-3-phenylprop-2-enoyl]amino]-3-(4-fluorophenyl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-N-[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-methylpentanamideIC5028.0 [1], 1130.0 [2]
(2S)-2-[[(2S)-2-[[(2S)-2-[Acetyl-[(E)-3-phenylprop-2-enoyl]amino]-3-(4-fluorophenyl)propanoyl]amino]-3-[4-(diaminomethylideneamino)phenyl]propanoyl]amino]-N-[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-methylpentanamideIC507.8 [1], 200.0 [2]
(2S)-2-[[(2S)-2-[[(2S)-2-(N-Acetyl-3-prop-2-ynoylanilino)-3-(4-fluorophenyl)propanoyl]amino]-3-[4-(diaminomethylideneamino)phenyl]propanoyl]amino]-N-[(2S)-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-methylpentanamideIC504.0 [1], 40.0 [2]
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[Acetyl-[(E)-3-phenylprop-2-enoyl]amino]-3-(4-fluorophenyl)propanoyl]amino]-3-[4-(diaminomethylideneamino)phenyl]propanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-7-amino-3-oxoheptanamideIC5016.6 [1], 40.0 [2]
(2S)-2-[[(2S)-2-[[(2S)-2-[Acetyl-[(E)-3-phenylprop-2-enoyl]amino]-3-(4-fluorophenyl)propanoyl]amino]-3-[4-(diaminomethylideneamino)phenyl]propanoyl]amino]-N-[(2S)-5-(diaminomethylideneamino)-1-[[(2S)-1,5-diamino-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]-4-methylpentanamideIC506.6 [1], 47.0 [2]
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[Acetyl-[(E)-3-(4-fluorophenyl)prop-2-enoyl]amino]-3-(4-fluorophenyl)propanoyl]amino]-3-[4-(diaminomethylideneamino)phenyl]propanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-7-amino-3-oxoheptanamideIC5025.0 [1], 60.0 [2]
Items per page: 1 - 10 of 100
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References

This online tool may be cited as follows

MLA

"Quest Database™ Proteinase-activated receptor 1 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 10 May. 2024, https://www.aatbio.com/data-sets/proteinase-activated-receptor-1-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, May 10). Quest Database™ Proteinase-activated receptor 1 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/proteinase-activated-receptor-1-inhibitors-ic50-ki.
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