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Bradykinin B1 receptor Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
CID 9916412IC500.18 [1]
N-[(1R)-6-[(Tert-butylamino)methyl]-1,2,3,4-tetrahydronaphthalen-1-yl]-2-[(2S)-1-[3-(trifluoromethyl)phenyl]sulfonylpiperidin-2-yl]acetamideIC5013.0 [1], 23.0 [2]
N-[(1R)-6-[(Tert-butylamino)methyl]-1,2,3,4-tetrahydronaphthalen-1-yl]-2-[(2S)-1-[3-(trifluoromethyl)phenyl]sulfonylpiperidin-2-yl]acetamideKi23.0 [1]
Methyl 2-chloro-6-[3-fluoro-4-[(1R)-1-[[1-[(2,2,2-trifluoroacetyl)amino]cyclopropanecarbonyl]amino]ethyl]phenyl]benzoateIC501.52 [1]
Methyl 2-chloro-6-[3-fluoro-4-[(1R)-1-[[1-[(2,2,2-trifluoroacetyl)amino]cyclopropanecarbonyl]amino]ethyl]phenyl]benzoateKi0.44 [1], 2.0 [2]
2-[(2R)-1-(4-Methylphenyl)sulfonyl-3-oxopiperazin-2-yl]-N-[(1R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]acetamideIC500.22 [1]
2-[(2R)-1-(4-Methylphenyl)sulfonyl-3-oxopiperazin-2-yl]-N-[(1R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]acetamideKi0.1 [1], 0.16 [2]
Chroman 28IC500.4 [1], 3.4 [2]
Chroman 28Ki0.7 [1], 0.77 [2]
Methyl 2-fluoro-6-[3-fluoro-4-[[[5-(4-pyridin-2-ylpiperazine-1-carbonyl)pyridin-2-yl]amino]methyl]phenyl]benzoateKi65.0 [1], 85.0 [2], 286.0 [3], 726.0 [4], 10000.0 [5]
(3R)-3-(4-Fluorophenyl)-N-[(4R)-7-(piperidin-1-ylmethyl)-3,4-dihydro-2H-chromen-4-yl]-3-[[3-(trifluoromethyl)phenyl]sulfonylamino]propanamideIC500.8 [1]
(3R)-3-(4-Fluorophenyl)-N-[(4R)-7-(piperidin-1-ylmethyl)-3,4-dihydro-2H-chromen-4-yl]-3-[[3-(trifluoromethyl)phenyl]sulfonylamino]propanamideKi0.4 [1]
1-[(3R)-2-Oxo-5-(2-phenylethyl)-1-propyl-3H-1,4-benzodiazepin-3-yl]-3-[4-(4-pyridin-4-ylpiperazin-1-yl)phenyl]ureaIC501.9 [1]
1-[(3R)-2-Oxo-5-(2-phenylethyl)-1-propyl-3H-1,4-benzodiazepin-3-yl]-3-[4-(4-pyridin-4-ylpiperazin-1-yl)phenyl]ureaKi0.59 [1]
(3R)-3-(Naphthalen-2-ylsulfonylamino)-3-phenyl-N-[(1R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]propanamideIC505.5 [1]
(3R)-3-(Naphthalen-2-ylsulfonylamino)-3-phenyl-N-[(1R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]propanamideKi0.24 [1]
(2R)-N-[(1R)-1-[5-[5-Chloro-3-fluoro-2-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl]-3-fluoropyridin-2-yl]ethyl]-3,3,3-trifluoro-2-hydroxy-2-methylpropanamideIC504.47 [1]
(2R)-N-[(1R)-1-[5-[5-Chloro-3-fluoro-2-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl]-3-fluoropyridin-2-yl]ethyl]-3,3,3-trifluoro-2-hydroxy-2-methylpropanamideKi0.5 [1], 0.66 [2], 1.85 [3]
N-[(2-Chlorophenyl)methyl]-2-[[3-methoxy-4-(2-methylpropoxy)phenyl]methyl-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]sulfonylamino]acetamideKi11.0 [1], 37.0 [2]
2-[(2R)-1-(3,4-Dichlorophenyl)sulfonyl-3-oxo-2,4-dihydroquinoxalin-2-yl]-N-[(1R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]acetamideIC500.55 [1]
2-[(2R)-1-(3,4-Dichlorophenyl)sulfonyl-3-oxo-2,4-dihydroquinoxalin-2-yl]-N-[(1R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]acetamideKi0.1 [1]
N-[(1R)-6-(Aminomethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]-2-[(2R)-1-(4-methylphenyl)sulfonyl-3-oxopiperazin-2-yl]acetamideIC50238.0 [1]
N-[(1R)-6-(Aminomethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]-2-[(2R)-1-(4-methylphenyl)sulfonyl-3-oxopiperazin-2-yl]acetamideKi60.0 [1]
Nvp-saa164IC5033.0 [1]
Nvp-saa164Ki8.0 [1], 10.0 [2]
Methyl 2-[4-[[[3-(3,3,3-trifluoropropanoylamino)pyridin-2-yl]amino]methyl]phenyl]benzoateKi11.8 [1], 12.0 [2]
N-[2-[4-(4,5-Dihydro-1H-imidazol-2-yl)phenyl]ethyl]-2-[(2R)-1-naphthalen-2-ylsulfonyl-3-oxo-2,4-dihydroquinoxalin-2-yl]acetamideIC500.04 [1]
N-[2-[4-(4,5-Dihydro-1H-imidazol-2-yl)phenyl]ethyl]-2-[(2R)-1-naphthalen-2-ylsulfonyl-3-oxo-2,4-dihydroquinoxalin-2-yl]acetamideKi0.02 [1]
(2R,3S)-2,3-Dihydroxy-N-[(1R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]-4-[3-(trifluoromethyl)phenyl]sulfonylbutanamideIC504.3 [1]
(2R,3S)-2,3-Dihydroxy-N-[(1R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]-4-[3-(trifluoromethyl)phenyl]sulfonylbutanamideKi4.1 [1]
2-[(2R)-1-(4-Methylphenyl)sulfonyl-3-oxo-2,4-dihydroquinoxalin-2-yl]-N-[(4R)-7-(piperidin-1-ylmethyl)-3,4-dihydro-2H-chromen-4-yl]acetamideIC500.14 [1]
2-[(2R)-1-(4-Methylphenyl)sulfonyl-3-oxo-2,4-dihydroquinoxalin-2-yl]-N-[(4R)-7-(piperidin-1-ylmethyl)-3,4-dihydro-2H-chromen-4-yl]acetamideKi0.24 [1]
3-(4-Oxochromen-3-yl)-N-[(1R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]benzamideIC50112.0 [1]
3-(4-Oxochromen-3-yl)-N-[(1R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]benzamideKi64.0 [1]
3-(4-Methyl-1-oxophthalazin-2-yl)-N-[(1R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]benzamideIC503405.0 [1]
3-(4-Methyl-1-oxophthalazin-2-yl)-N-[(1R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]benzamideKi6366.0 [1]
Kallidin, des-Arg(10)-IC500.87 [1]
Kallidin, des-Arg(10)-Ki0.2 [1]
FasitibantKi10000.0 [1]
SafotibantKi0.3 [1], 0.35 [2]
Methyl 2-fluoro-6-[3-fluoro-4-[[[1-[(2,2,2-trifluoroacetyl)amino]cyclopropanecarbonyl]amino]methyl]phenyl]benzoateKi1.47 [1], 1.5 [2]
N-[1-[4-[(2S)-2-Amino-6-(dimethylamino)hexanoyl]piperazin-1-yl]-2-methyl-1-oxopropan-2-yl]-2,4-dichloro-3-[(2,4-dimethylquinolin-8-yl)oxymethyl]benzenesulfonamideKi5.5 [1], 10000.0 [2]
N-[1-[4-[(2S)-2-Amino-5-(dimethylamino)pentanoyl]piperazin-1-yl]-2-methyl-1-oxopropan-2-yl]-2,4-dichloro-3-[(2,4-dimethylquinolin-8-yl)oxymethyl]benzenesulfonamideKi5.5 [1], 10000.0 [2]
N-[1-[4-[(3S)-3-Amino-6-(dimethylamino)hexanoyl]piperazin-1-yl]-2-methyl-1-oxopropan-2-yl]-2,4-dichloro-3-[(2,4-dimethylquinolin-8-yl)oxymethyl]benzenesulfonamideKi5.5 [1], 10000.0 [2]
Methyl 2-[4-[[[2-methyl-2-(3,3,3-trifluoropropanoylamino)propanoyl]amino]methyl]phenyl]benzoateKi3450.0 [1], 3500.0 [2]
Methyl 2-[4-[[[1-(3,3,3-trifluoropropanoylamino)cyclopropanecarbonyl]amino]methyl]phenyl]benzoateKi63.0 [1]
Methyl 2,4-dichloro-6-[3-fluoro-4-[(1R)-1-[[1-[(2,2,2-trifluoroacetyl)amino]cyclopropanecarbonyl]amino]ethyl]phenyl]benzoateKi0.4 [1], 0.46 [2]
4-Bromo-3-[(2-chlorobenzoyl)amino]-N-[2-(1-pyridin-4-ylpiperidin-4-yl)ethyl]-1H-pyrazole-5-carboxamideIC503.0 [1], 3.5 [2]
Tetrahydrofuran-2-ylmethyl 4-{[(2-benzoylphenyl)amino]sulfonyl}phenylcarbamateKi0.7 [1]
N-(2-Benzoyl-phenyl)-4-[3-(3-piperidin-1-yl-propyl)-ureido]-benzenesulfonamideKi0.25 [1]
N-[4-(2-Benzoyl-phenylsulfamoyl)-phenyl]-acetamideKi45.0 [1]
Methyl 2-[4-[[[3-(pentanoylamino)pyridin-2-yl]amino]methyl]phenyl]benzoateKi200.0 [1]
Methyl 2-fluoro-6-[3-fluoro-4-[(pyridin-2-ylamino)methyl]phenyl]benzoateKi815.0 [1]
(2R)-N-[3-[(4-Carbamimidoylbenzoyl)amino]propyl]-1-[2,4-dichloro-3-[(2,4-dimethylquinolin-8-yl)oxymethyl]phenyl]sulfonylpyrrolidine-2-carboxamideKi5.5 [1], 10000.0 [2]
Unii-8PY38jsg1YKi0.02 [1]
Methyl 2-fluoro-6-[3-fluoro-4-[(1R)-1-[[1-[(2,2,2-trifluoroacetyl)amino]cyclopropanecarbonyl]amino]ethyl]phenyl]benzoateIC501.9 [1]
Methyl 2-fluoro-6-[3-fluoro-4-[(1R)-1-[[1-[(2,2,2-trifluoroacetyl)amino]cyclopropanecarbonyl]amino]ethyl]phenyl]benzoateKi0.57 [1]
1-(5-Cyclohexyl-2-oxo-1-propyl-3H-1,4-benzodiazepin-3-yl)-3-[4-[4-(dimethylamino)piperidin-1-yl]phenyl]ureaIC50164.0 [1]
1-(5-Cyclohexyl-2-oxo-1-propyl-3H-1,4-benzodiazepin-3-yl)-3-[4-[4-(dimethylamino)piperidin-1-yl]phenyl]ureaKi28.0 [1]
N-[(1R)-1-[2-Fluoro-4-[3-fluoro-2-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl]phenyl]ethyl]-1-[(2,2,2-trifluoroacetyl)amino]cyclopropane-1-carboxamideIC500.89 [1]
N-[(1R)-1-[2-Fluoro-4-[3-fluoro-2-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl]phenyl]ethyl]-1-[(2,2,2-trifluoroacetyl)amino]cyclopropane-1-carboxamideKi0.51 [1]
N-[(1R)-1-[2-Fluoro-4-[3-fluoro-2-(2-methyltetrazol-5-yl)phenyl]phenyl]ethyl]-1-[(2,2,2-trifluoroacetyl)amino]cyclopropane-1-carboxamideIC500.65 [1]
N-[(1R)-1-[2-Fluoro-4-[3-fluoro-2-(2-methyltetrazol-5-yl)phenyl]phenyl]ethyl]-1-[(2,2,2-trifluoroacetyl)amino]cyclopropane-1-carboxamideKi0.6 [1]
1-[(3S)-5-Cyclohexyl-2-oxo-1-propyl-3H-1,4-benzodiazepin-3-yl]-3-[4-(4-piperidin-1-ylpiperidin-1-yl)phenyl]ureaIC502200.0 [1]
1-[(3S)-5-Cyclohexyl-2-oxo-1-propyl-3H-1,4-benzodiazepin-3-yl]-3-[4-(4-piperidin-1-ylpiperidin-1-yl)phenyl]ureaKi1023.0 [1]
1-[(3R)-5-Cyclohexyl-2-oxo-1-propyl-3H-1,4-benzodiazepin-3-yl]-3-[4-(4-pyridin-4-ylpiperazin-1-yl)phenyl]ureaIC508.0 [1]
1-[(3R)-5-Cyclohexyl-2-oxo-1-propyl-3H-1,4-benzodiazepin-3-yl]-3-[4-(4-pyridin-4-ylpiperazin-1-yl)phenyl]ureaKi1.33 [1]
1-[(3R)-5-(4-Methylphenyl)-2-oxo-1-propyl-3H-1,4-benzodiazepin-3-yl]-3-[4-(4-piperidin-1-ylpiperidin-1-yl)phenyl]ureaIC5064.5 [1]
1-[(3R)-5-(4-Methylphenyl)-2-oxo-1-propyl-3H-1,4-benzodiazepin-3-yl]-3-[4-(4-piperidin-1-ylpiperidin-1-yl)phenyl]ureaKi13.4 [1]
1-[(3R)-2-Oxo-5-(2-phenylethyl)-1-propyl-3H-1,4-benzodiazepin-3-yl]-3-[4-(4-piperidin-1-ylpiperidin-1-yl)phenyl]ureaIC504.83 [1]
1-[(3R)-2-Oxo-5-(2-phenylethyl)-1-propyl-3H-1,4-benzodiazepin-3-yl]-3-[4-(4-piperidin-1-ylpiperidin-1-yl)phenyl]ureaKi1.37 [1]
1-[(3R)-5-Cyclohexyl-2-oxo-1-propyl-3H-1,4-benzodiazepin-3-yl]-3-[4-(4-piperidin-1-ylpiperidin-1-yl)phenyl]ureaIC5024.7 [1]
1-[(3R)-5-Cyclohexyl-2-oxo-1-propyl-3H-1,4-benzodiazepin-3-yl]-3-[4-(4-piperidin-1-ylpiperidin-1-yl)phenyl]ureaKi5.73 [1]
Methyl 4-chloro-2-[4-[(1R)-1-[[4-chloro-3-[(2-cyanoacetyl)amino]pyridin-2-yl]amino]ethyl]phenyl]benzoateIC501.5 [1]
Methyl 4-chloro-2-[4-[(1R)-1-[[4-chloro-3-[(2-cyanoacetyl)amino]pyridin-2-yl]amino]ethyl]phenyl]benzoateKi0.8 [1]
2-[1-(2-Chlorophenyl)sulfonyl-3-oxopiperazin-2-yl]-N-[(1R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]acetamideIC500.55 [1]
2-[1-(2-Chlorophenyl)sulfonyl-3-oxopiperazin-2-yl]-N-[(1R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]acetamideKi0.41 [1]
N-[(1R)-6-[(Cyclopropylmethylamino)methyl]-1,2,3,4-tetrahydronaphthalen-1-yl]-2-[(2S)-1-[3-(trifluoromethyl)phenyl]sulfonylpiperidin-2-yl]acetamideIC5016.0 [1], 31.0 [2]
N-[(1R)-6-[(Tert-butylamino)methyl]-1,2,3,4-tetrahydronaphthalen-1-yl]-2-[(2S)-1-[4-methyl-3-(trifluoromethyl)phenyl]sulfonylpiperidin-2-yl]acetamideIC5011.0 [1], 16.0 [2]
2-[1-(4-Methylphenyl)sulfonyl-3-oxopiperazin-2-yl]-N-[(1R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]acetamideIC500.3 [1]
2-[1-(4-Methylphenyl)sulfonyl-3-oxopiperazin-2-yl]-N-[(1R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]acetamideKi0.3 [1]
N-[(1R)-6-[(Propan-2-ylamino)methyl]-1,2,3,4-tetrahydronaphthalen-1-yl]-2-[(2S)-1-[3-(trifluoromethyl)phenyl]sulfonylpiperidin-2-yl]acetamideIC5072.0 [1], 110.0 [2]
N-[(1R)-6-[(2-Methylpropylamino)methyl]-1,2,3,4-tetrahydronaphthalen-1-yl]-2-[(2S)-1-[3-(trifluoromethyl)phenyl]sulfonylpiperidin-2-yl]acetamideIC5013.0 [1], 42.0 [2]
2-[3-Oxo-1-[3-(trifluoromethyl)phenyl]sulfonylpiperazin-2-yl]-N-[(1R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]acetamideIC500.94 [1]
2-[3-Oxo-1-[3-(trifluoromethyl)phenyl]sulfonylpiperazin-2-yl]-N-[(1R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]acetamideKi0.15 [1]
2-[1-[(5-Chloro-1-benzothiophen-2-yl)sulfonyl]-3-oxopiperazin-2-yl]-N-[(1R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]acetamideIC503.3 [1]
2-[1-[(5-Chloro-1-benzothiophen-2-yl)sulfonyl]-3-oxopiperazin-2-yl]-N-[(1R)-6-(piperidin-1-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]acetamideKi0.1 [1]
(3R)-N-[(4R)-1-Methyl-2,2-dioxo-7-(piperidin-1-ylmethyl)-3,4-dihydro-2lambda6,1-benzothiazin-4-yl]-3-(naphthalen-2-ylsulfonylamino)-3-phenylpropanamideIC5010.7 [1]
(3R)-N-[(4R)-1-Methyl-2,2-dioxo-7-(piperidin-1-ylmethyl)-3,4-dihydro-2lambda6,1-benzothiazin-4-yl]-3-(naphthalen-2-ylsulfonylamino)-3-phenylpropanamideKi1.3 [1]
4-Bromo-5-[(2-chlorobenzoyl)amino]-N-[2-(4-pyridinyl)ethyl]-1H-pyrazole-3-carboxamideIC50490.0 [1]
4-Bromo-5-[(2-chlorobenzoyl)amino]-N-[2-(4-pyridinyl)ethyl]-1H-pyrazole-3-carboxamideKi120.0 [1]
N-[4-Chloro-2-[[(1R)-1-[4-[3-fluoro-2-(2-methyltetrazol-5-yl)phenyl]phenyl]ethyl]amino]pyridin-3-yl]-2-cyanoacetamideIC501.17 [1]
N-[4-Chloro-2-[[(1R)-1-[4-[3-fluoro-2-(2-methyltetrazol-5-yl)phenyl]phenyl]ethyl]amino]pyridin-3-yl]-2-cyanoacetamideKi0.5 [1]
N-[(1R)-6-[(Cyclobutylamino)methyl]-1,2,3,4-tetrahydronaphthalen-1-yl]-2-[(2S)-1-[3-(trifluoromethyl)phenyl]sulfonylpiperidin-2-yl]acetamideIC5054.0 [1], 58.0 [2]
2-[(2R)-1-(4-Methylphenyl)sulfonyl-3-oxopiperazin-2-yl]-N-[(1R)-6-(morpholin-4-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]acetamideIC501.2 [1]
2-[(2R)-1-(4-Methylphenyl)sulfonyl-3-oxopiperazin-2-yl]-N-[(1R)-6-(morpholin-4-ylmethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]acetamideKi3.0 [1]
4-(Benzhydryl-amino)-N,N-bis-(3-dimethylamino-propyl)-3-nitro-benzenesulfonamideIC506200.0 [1]
4-(Benzhydryl-amino)-N,N-bis-(3-dimethylamino-propyl)-3-nitro-benzenesulfonamideKi3000.0 [1]
2-[(2R)-1-(4-Methylphenyl)sulfonyl-3-oxopiperazin-2-yl]-N-[(1R)-6-[(4-methylpiperazin-1-yl)methyl]-1,2,3,4-tetrahydronaphthalen-1-yl]acetamideIC501.46 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Bradykinin B1 receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc.10 May2024https://www.aatbio.com/data-sets/bradykinin-b1-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 10). Quest Database™ Bradykinin B1 receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/bradykinin-b1-receptor-inhibitors-ic50-ki.
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