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Bradykinin B2 receptor 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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▼
IcatibantIC500.49 [1], 3.3 [2]
IcatibantKi0.03 [1], 0.06 [2], 0.18 [3]
4-[(E)-3-[[2-[2,4-Dichloro-N-methyl-3-[(2-methylquinolin-8-yl)oxymethyl]anilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N-methylbenzamide;hydrochlorideIC501.1 [1]
BradykininIC501.8 [1]
BradykininKi0.07 [1], 0.11 [2], 0.65 [3], 0.68 [4]
Arg-3-hyp-7-phe-bradykininIC507.0 [1], 10.0 [2], 14.0 [3]
4-[(E)-3-[[2-[3-[(3-Bromo-2-methylimidazo[1,2-a]pyridin-8-yl)oxymethyl]-2,4-dichloro-N-methylanilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N-methylbenzamide;hydrochlorideIC501.5 [1], 9.0 [2]
(E)-3-(6-Acetamidopyridin-3-yl)-N-[2-[2,4-dichloro-N-methyl-3-[(2-methylquinolin-8-yl)oxymethyl]anilino]-2-oxoethyl]prop-2-enamideIC501.4 [1]
4-[(E)-3-[[2-[3-[(3-Bromo-2-methylimidazo[1,2-a]pyridin-8-yl)oxymethyl]-2,4-dichloro-N-methylanilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N,N-dimethylbenzamideIC501.4 [1], 2.2 [2]
4-[(E)-3-[[2-[2,4-Dichloro-N-methyl-3-[(2-methyl-1,3-benzoxazol-4-yl)oxymethyl]anilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N-methylbenzamideIC50860.0 [1], 1100.0 [2]
4-[(E)-3-[[2-[2,4-Dichloro-N-methyl-3-[(2-methylquinazolin-8-yl)oxymethyl]anilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N-methylbenzamideIC5056.0 [1], 59.0 [2]
4-[(E)-3-[[2-[2,4-Dichloro-N-methyl-3-[(2-methylquinoxalin-5-yl)oxymethyl]anilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N-methylbenzamideIC502900.0 [1], 4300.0 [2]
4-[(E)-3-[[2-[2,4-Dichloro-N-methyl-3-[(3-methylquinoxalin-5-yl)oxymethyl]anilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N-methylbenzamide;hydrochlorideIC503.1 [1], 5.2 [2]
4-[(E)-3-[[2-[2,4-Dichloro-3-[(1,2-dimethylbenzimidazol-4-yl)oxymethyl]-N-methylanilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N-methylbenzamideIC5043.0 [1], 67.0 [2]
N-[2-[3-(Dimethylamino)propyl-methylamino]ethyl]-1-[3-nitro-4-[2-(2-tricyclo[9.4.0.03,8]pentadeca-1(15),3,5,7,11,13-hexaenylcarbamoyl)hydrazinyl]phenyl]sulfonylpyrrole-2-carboxamideIC5012.0 [1], 55.0 [2]
N-[2-[3-(Dimethylamino)propyl-methylamino]ethyl]-1-[3-nitro-4-[2-(2-tricyclo[9.4.0.03,8]pentadeca-1(15),3,5,7,11,13-hexaenylcarbamoyl)hydrazinyl]phenyl]sulfonylpyrrole-2-carboxamideKi2.79 [1]
2-[5-Chloro-4-[[2-methyl-4-(2-methylpyrazol-3-yl)quinolin-8-yl]oxymethyl]pyridin-3-yl]sulfanyl-1,3-thiazoleIC5029.0 [1], 50.0 [2], 470.0 [3]
(2S)-N-[2-[3-(Dimethylamino)propyl-methylamino]ethyl]-1-[3-nitro-4-[2-(2-tricyclo[9.4.0.03,8]pentadeca-1(15),3,5,7,11,13-hexaenylcarbamoyl)hydrazinyl]phenyl]sulfonylpyrrolidine-2-carboxamideIC5017.0 [1], 91.0 [2]
(2S)-N-[2-[3-(Dimethylamino)propyl-methylamino]ethyl]-1-[3-nitro-4-[2-(2-tricyclo[9.4.0.03,8]pentadeca-1(15),3,5,7,11,13-hexaenylcarbamoyl)hydrazinyl]phenyl]sulfonylpyrrolidine-2-carboxamideKi0.79 [1]
4-[(E)-3-[[2-[2,4-Dichloro-N-methyl-3-[[2-methyl-4-(pyridin-2-ylmethoxy)quinolin-8-yl]oxymethyl]anilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N-methylbenzamideIC500.41 [1]
FasitibantKi0.05 [1]
(2R)-2-[[(2S)-2-[[(2S)-2-[(2S)-2-[[(2S)-2-[[2-[[(2S)-1-[(2S)-1-[(2S)-2-[[(2R)-2-[[(2S)-2-Amino-5-(diaminomethylideneamino)pentanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]pyrrolidine-1-carbonyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoic acidKi12.59 [1], 20.0 [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]benzenesulfonamideKi0.63 [1]
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]benzenesulfonamideKi0.4 [1]
4-[(E)-3-[[2-[2,4-Dichloro-N-methyl-3-[(2-methylquinolin-8-yl)oxymethyl]anilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N-methylbenzamideIC501.1 [1]
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]benzenesulfonamideKi0.63 [1]
4-[(E)-3-[[2-[2,4-Dichloro-3-[(2,3-dimethyl-1-benzofuran-7-yl)oxymethyl]-N-methylanilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N-methylbenzamideIC50270.0 [1]
4-[(E)-3-[[2-[3-[[2-(Dimethylamino)-1-methylbenzimidazol-4-yl]oxymethyl]-N,2,4-trimethylanilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N-methylbenzamideIC50160.0 [1]
4-[(E)-3-[[2-[3-[(2-Acetyl-1-methylbenzimidazol-4-yl)oxymethyl]-N,2,4-trimethylanilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N-methylbenzamideIC5094.0 [1]
Ethyl 2-[4-[[2,6-dimethyl-3-[methyl-[2-[[(E)-3-[4-(methylcarbamoyl)phenyl]prop-2-enoyl]amino]acetyl]amino]phenyl]methoxy]-1-methylbenzimidazol-2-yl]acetateIC508400.0 [1]
4-[(E)-3-[[2-[3-[[2-(Methoxymethyl)-1-methylbenzimidazol-4-yl]oxymethyl]-N,2,4-trimethylanilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N-methylbenzamideIC509100.0 [1]
4-[(E)-3-[[2-[2,4-Dichloro-3-[(1-ethyl-2-methylbenzimidazol-4-yl)oxymethyl]-N-methylanilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N-methylbenzamideIC5048.0 [1]
(E)-3-(6-Acetamidopyridin-3-yl)-N-[2-[2,4-dichloro-3-[(2-methoxy-1-methylbenzimidazol-4-yl)oxymethyl]-N-methylanilino]-2-oxoethyl]prop-2-enamideIC504.2 [1]
4-[(E)-3-[[2-[3-[(2-Methoxy-1-methylbenzimidazol-4-yl)oxymethyl]-N,2,4-trimethylanilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N-methylbenzamideIC507.2 [1]
4-[(E)-3-[[2-[2,4-Dichloro-3-[(2-methoxy-1-methylbenzimidazol-4-yl)oxymethyl]-N-methylanilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N-methylbenzamideIC502.2 [1]
N-Methyl-4-[(E)-3-oxo-3-[[2-oxo-2-[N,2,4-trimethyl-3-[(1-methyl-2-methylsulfanylbenzimidazol-4-yl)oxymethyl]anilino]ethyl]amino]prop-1-enyl]benzamideIC5079.0 [1]
N-Methyl-4-[(E)-3-oxo-3-[[2-oxo-2-[N,2,4-trimethyl-3-[[1-methyl-2-(methylamino)benzimidazol-4-yl]oxymethyl]anilino]ethyl]amino]prop-1-enyl]benzamideIC50670.0 [1]
4-[(E)-3-[[2-[3-[(2-Ethoxy-1-methylbenzimidazol-4-yl)oxymethyl]-N,2,4-trimethylanilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N-methylbenzamideIC50730.0 [1]
4-[(E)-3-[[2-[2,4-Dichloro-N-methyl-3-[(2-methylquinolin-8-yl)oxymethyl]anilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N,N-dimethylbenzamide;hydrochlorideIC503.9 [1]
(2R)-N-[3-[(4-Carbamimidoylbenzoyl)amino]propyl]-1-[2,4-dichloro-3-[(2,4-dimethylquinolin-8-yl)oxymethyl]phenyl]sulfonylpyrrolidine-2-carboxamideKi0.4 [1], 0.79 [2]
4-[(E)-3-[[2-[2,4-Dichloro-3-[(2-ethyl-1-methylbenzimidazol-4-yl)oxymethyl]-N-methylanilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N-methylbenzamide;hydrochlorideIC5022.0 [1]
N-Methyl-4-[(E)-3-oxo-3-[[2-oxo-2-[N,2,4-trimethyl-3-[(2-methylquinolin-8-yl)oxymethyl]anilino]ethyl]amino]prop-1-enyl]benzamide;hydrochlorideIC504.8 [1]
Unii-8PY38jsg1YKi9.16 [1], 9.2 [2]
4-[(E)-3-[[2-[2,4-Dichloro-3-[[4-(dimethylamino)-2-methylquinolin-8-yl]oxymethyl]-N-methylanilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N-methylbenzamide;dihydrochlorideIC503.2 [1]
4-[(E)-3-[[2-[2,4-Dichloro-3-[[4-(dimethylamino)-2-methylquinolin-8-yl]oxymethyl]-N-methylanilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N,N-dimethylbenzamide;dihydrochlorideIC502.1 [1]
4-[(E)-3-[[2-[2,4-Dichloro-3-[[2-(2,5-dimethylpyrrol-1-yl)pyridin-3-yl]oxymethyl]-N-methylanilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N-methylbenzamideIC502000.0 [1], 3500.0 [2]
4-[(E)-3-[[2-[2,4-Dichloro-N-methyl-3-[(6-methylpyridin-2-yl)methoxymethyl]anilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N-methylbenzamideIC5010000.0 [1]
4-[(E)-3-[[2-[2,4-Dichloro-3-[(4-ethoxy-2-methylquinolin-8-yl)oxymethyl]-N-methylanilino]-2-oxoethyl]amino]-3-oxoprop-1-enyl]-N-methylbenzamideIC5034.0 [1]
Unii-1Q3KX3563SIC501.1 [1], 8.7 [2]
8-(3,5-Dichloro-pyridin-4-ylmethoxy)-2-methyl-4-(2-methyl-2H-pyrazol-3-yl)-quinolineIC5050.0 [1], 180.0 [2]
8-((3,5-Dichloropyridin-4-yl)methoxy)-2-methyl-4-(4-methyl-1H-pyrazol-3-yl)quinolineIC50110.0 [1], 390.0 [2]
8-((3,5-Dichloropyridin-4-yl)methoxy)-2-methyl-4-(5-methyl-1H-pyrazol-4-yl)quinolineIC503600.0 [1], 6300.0 [2]
5-(8-((3,5-Dichloropyridin-4-yl)methoxy)-2-methylquinolin-4-yl)thiazoleIC50135.0 [1], 420.0 [2]
8-[(3,5-Dichloropyridin-4-yl)methoxy]-2-methyl-4-(2-methyl-1,2,4-triazol-3-yl)quinolineIC5068.0 [1], 2400.0 [2]
8-(3,5-Dichloro-pyridin-4-ylmethoxy)-2-methyl-4-thiazol-2-yl-quinolineIC50420.0 [1], 480.0 [2]
8-(3,5-Dichloro-pyridin-4-ylmethoxy)-2-methyl-4-(4-methyl-thiazol-5-yl)-quinolineIC5067.0 [1], 110.0 [2]
8-(3,5-Dichloro-pyridin-4-ylmethoxy)-2-methyl-4-(5-methyl-thiazol-4-yl)-quinolineIC5064.0 [1], 400.0 [2]
4-(8-((3,5-Dichloropyridin-4-yl)methoxy)-2-methylquinolin-4-yl)-3-methylisothiazoleIC50200.0 [1], 330.0 [2]
5-[8-[(3,5-Dichloropyridin-4-yl)methoxy]-2-methylquinolin-4-yl]-4-methyl-1,3-oxazoleIC505000.0 [1], 6050.0 [2]
N-[[4-Methyl-3-[[2-methyl-4-(2-methylpyrazol-3-yl)quinolin-8-yl]oxymethyl]pyridin-2-yl]methyl]cyclohexanecarboxamideIC501.8 [1], 10.0 [2]
4-(4-Chloro-thiazol-5-yl)-8-(3,5-dichloro-pyridin-4-ylmethoxy)-2-methyl-quinolineIC50980.0 [1], 2500.0 [2]
8-(3,5-Dichloro-pyridin-4-ylmethoxy)-2-methyl-4-thiazol-4-yl-quinolineIC5080.0 [1], 300.0 [2]
4-(5-Chloro-thiazol-4-yl)-8-(3,5-dichloro-pyridin-4-ylmethoxy)-2-methyl-quinolineIC50210.0 [1], 730.0 [2]
8-(3,5-Dichloro-pyridin-4-ylmethoxy)-2-methyl-4-(4-methyl-isothiazol-3-yl)-quinolineIC5020.0 [1], 70.0 [2]
8-(3,5-Dichloro-pyridin-4-ylmethoxy)-2-methyl-4-(3-methyl-isoxazol-4-yl)-quinolineIC50430.0 [1], 3800.0 [2]
2-Methyl-N-[[4-methyl-3-[[2-methyl-4-(2-methylpyrazol-3-yl)quinolin-8-yl]oxymethyl]pyridin-2-yl]methyl]propanamideIC503.8 [1], 5.4 [2]
8-[(3-Chloropyridin-4-yl)methoxy]-2-methyl-4-(2-methylpyrazol-3-yl)quinolineIC50517.0 [1], 1600.0 [2]
8-[[3-Chloro-5-(1-methylimidazol-2-yl)sulfanylpyridin-4-yl]methoxy]-2-methyl-4-(2-methylpyrazol-3-yl)quinolineIC5018.0 [1], 43.0 [2]
2-[5-Chloro-4-[[2-methyl-4-(2-methylpyrazol-3-yl)quinolin-8-yl]oxymethyl]pyridin-3-yl]sulfanyl-N,N-dimethylacetamideIC507.5 [1], 24.0 [2]
2-[5-Chloro-4-[[2-methyl-4-(2-methylpyrazol-3-yl)quinolin-8-yl]oxymethyl]pyridin-3-yl]sulfinyl-N,N-dimethylacetamideIC5037.0 [1], 76.0 [2]
2-[5-Chloro-4-[[2-methyl-4-(2-methylpyrazol-3-yl)quinolin-8-yl]oxymethyl]pyridin-3-yl]oxy-N,N-dimethylacetamideIC506.5 [1], 91.0 [2]
3-[5-Chloro-4-[[2-methyl-4-(2-methylpyrazol-3-yl)quinolin-8-yl]oxymethyl]pyridin-3-yl]-N,N-dimethylpropanamideIC5036.0 [1], 73.0 [2]
N-[[5-Chloro-4-[[2-methyl-4-(2-methylpyrazol-3-yl)quinolin-8-yl]oxymethyl]pyridin-3-yl]methyl]-2-methylpropanamideIC502.3 [1], 7.8 [2]
3-[[5-Chloro-4-[[2-methyl-4-(2-methylpyrazol-3-yl)quinolin-8-yl]oxymethyl]pyridin-3-yl]methyl]-1,1-dimethylureaIC502.8 [1], 6.6 [2]
[5-Chloro-4-[[2-methyl-4-(2-methylpyrazol-3-yl)quinolin-8-yl]oxymethyl]pyridin-3-yl]methyl N,N-dimethylcarbamateIC508.3 [1], 12.0 [2]
3-[5-Chloro-4-[[2-methyl-4-(2-methylpyrazol-3-yl)quinolin-8-yl]oxymethyl]pyridin-3-yl]propanamideIC5033.0 [1], 190.0 [2]
N-[[5-Chloro-4-[[2-methyl-4-(2-methylpyrazol-3-yl)quinolin-8-yl]oxymethyl]pyridin-3-yl]methyl]acetamideIC5012.0 [1], 24.0 [2]
N-[[5-Chloro-4-[[2-methyl-4-(2-methylpyrazol-3-yl)quinolin-8-yl]oxymethyl]pyridin-3-yl]methyl]methanesulfonamideIC5014.0 [1], 110.0 [2]
1-[[5-Chloro-4-[[2-methyl-4-(2-methylpyrazol-3-yl)quinolin-8-yl]oxymethyl]pyridin-3-yl]methyl]pyridin-2-oneIC503.6 [1], 5.1 [2]
8-[[3-Chloro-5-(pyridin-2-yloxymethyl)pyridin-4-yl]methoxy]-2-methyl-4-(2-methylpyrazol-3-yl)quinolineIC50140.0 [1], 260.0 [2]
1-[[5-Chloro-4-[[2-methyl-4-(2-methylpyrazol-3-yl)quinolin-8-yl]oxymethyl]pyridin-3-yl]methyl]-3-(trifluoromethyl)pyridin-2-oneIC501.4 [1], 4.0 [2]
1-[[4-Methyl-3-[[2-methyl-4-(2-methylpyrazol-3-yl)quinolin-8-yl]oxymethyl]pyridin-2-yl]methyl]-3-(trifluoromethyl)pyridin-2-oneIC500.54 [1], 8.8 [2]
8-(3,5-Dichloro-pyridin-4-ylmethoxy)-4-imidazol-1-yl-2-methyl-quinolineIC50580.0 [1], 2500.0 [2]
8-(3,5-Dichloro-pyridin-4-ylmethoxy)-2-methyl-4-(2-methyl-imidazol-1-yl)-quinolineIC50200.0 [1], 1300.0 [2]
8-(3,5-Dichloro-pyridin-4-ylmethoxy)-2-methyl-4-(1-methyl-1H-imidazol-2-yl)-quinolineIC5090.0 [1], 760.0 [2]
8-(3,5-Dichloro-pyridin-4-ylmethoxy)-4-(1,5-dimethyl-1H-imidazol-2-yl)-2-methylquinolineIC50200.0 [1], 3400.0 [2]
8-(3,5-Dichloro-pyridin-4-ylmethoxy)-2-methyl-4-pyrazol-1-yl-quinolineIC5032.0 [1], 920.0 [2]
8-(3,5-Dichloro-pyridin-4-ylmethoxy)-2-methyl-4-(2H-pyrazol-3-yl)-quinolineIC50310.0 [1], 350.0 [2]
[5-Chloro-4-[2-methyl-4-(2-methylpyrazol-3-yl)quinoline-8-carbonyl]pyridin-3-yl]methyl acetateIC506.0 [1], 260.0 [2]
1-[[3-[[4-(5-Chloro-1,3-thiazol-4-yl)-2-methylquinolin-8-yl]oxymethyl]-4-methylpyridin-2-yl]methyl]-3-(trifluoromethyl)pyridin-2-oneIC501.3 [1], 10.0 [2]
Tributyl-[[4-[[(2S)-2-[(N,N'-dicyclohexylcarbamimidoyl)amino]-3-naphthalen-2-ylpropanoyl]amino]phenyl]methyl]phosphanium;dihydrochlorideKi60.0 [1]
4,4'-Bis[(tripentylphosphonio)methyl]benzophenoneKi770.0 [1]
TamoxifenKi12048.0 [1]
AmiodaroneKi7674.0 [1]
[Leu8,des-Arg9]bradykininKi10.0 [1]
LabradimilKi19.0 [1]
CipargaminIC5030000.0 [1]
Fasitibant chlorideIC500.05 [1]
BradyzideKi772.0 [1]
CID 9916412Ki10000.0 [1]
Items per page: 1 - 10 of 100
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References

This online tool may be cited as follows

MLA

"Quest Database™ Bradykinin B2 receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Dec. 2024, https://www.aatbio.com/data-sets/bradykinin-b2-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, December 21). Quest Database™ Bradykinin B2 receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/bradykinin-b2-receptor-inhibitors-ic50-ki.
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