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Proteinase-activated receptor 2 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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N-[(2S)-3-Cyclohexyl-1-[[(2S,3S)-3-methyl-1-oxo-1-(4-phenylpiperidin-1-yl)pentan-2-yl]amino]-1-oxopropan-2-yl]-1,2-oxazole-5-carboxamideIC502200.0 [1]
N-[(2S)-3-Cyclohexyl-1-[[(2S,3S)-3-methyl-1-oxo-1-spiro[indene-1,4'-piperidine]-1'-ylpentan-2-yl]amino]-1-oxopropan-2-yl]-1,2-oxazole-5-carboxamideIC501000.0 [1], 1584.89 [2], 3600.0 [3], 9600.0 [4]
N-[(2S)-3-Cyclohexyl-1-[[(2S,3S)-1-[(2-methoxyphenyl)methylamino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-1,2-oxazole-5-carboxamideIC50400.0 [1], 500.0 [2], 1700.0 [3], 1900.0 [4]
Tert-butyl 4-[8-tert-butyl-6-(4-fluorophenyl)imidazo[1,2-b]pyridazine-2-carbonyl]-3,3-dimethylpiperazine-1-carboxylateIC504.2 [1], 4.8 [2], 50000.0 [3]
Tert-butyl 4-[6-(4-fluorophenyl)-8-propan-2-ylimidazo[1,2-b]pyridazine-2-carbonyl]-3,3-dimethylpiperazine-1-carboxylateIC502.0 [1], 5.0 [2], 51000.0 [3], 97000.0 [4]
Ethyl (2R,3S)-1-[6-(4-fluorophenyl)-8-(trifluoromethyl)imidazo[1,2-b]pyridazine-2-carbonyl]-2-methylpiperidine-3-carboxylateIC503300.0 [1], 4400.0 [2], 4800.0 [3], 5500.0 [4]
1-[(2S)-4-[6-(4-Fluorophenyl)-8-propan-2-ylimidazo[1,2-b]pyridazine-2-carbonyl]-2-methylpiperazin-1-yl]-2-thiophen-3-ylethanoneIC502.0 [1], 5.0 [2], 500.0 [3]
TriptolideIC5014.0 [1], 23.0 [2]
N-[(2S)-3-Cyclohexyl-1-[[(2S,3S)-3-methyl-1-oxo-1-spiro[1,2-dihydroindene-3,4'-piperidine]-1'-ylpentan-2-yl]amino]-1-oxopropan-2-yl]-1,2-oxazole-5-carboxamideIC502000.0 [1], 7943.28 [2]
N-[(2S)-3-Cyclohexyl-1-[[(2S,3S)-3-methyl-1-[4-(2-morpholin-4-yl-2-oxoethyl)anilino]-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-1,2-oxazole-5-carboxamideIC5057000.0 [1]
(2S)-6-Amino-N-[(2S)-1-(benzhydrylamino)-1-oxo-3-phenylpropan-2-yl]-2-[[2-[[1-[(2,6-dichlorophenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-5-yl]carbamoylamino]acetyl]amino]hexanamideIC501100.0 [1]
(2S)-6-Amino-N-[(2S)-1-(benzhydrylamino)-1-oxo-3-phenylpropan-2-yl]-2-[[2-[[1-[(2,6-dichlorophenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-5-yl]carbamoylamino]acetyl]amino]hexanamideKi600.0 [1]
(2S)-6-Amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-carbamimidamido-2-(hexadecanoylamino)pentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-4-methylpentanoyl]amino]pentanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-carboxypropanoyl]amino]-4-carboxybutanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]hexanoyl]amino]hexanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-3-methylpentanoyl]amino]hexanoic acidIC501000.0 [1], 15000.0 [2]
2-Furoyl-LIGRLO-amideIC50100.0 [1]
6-Amino-1-[4-(3-methylbutanoyl)piperazin-1-yl]hexan-1-oneIC505000000.0 [1]
2-(6-Bromo-1,3-benzodioxol-5-yl)-N-(4-cyanophenyl)-1-[(1S)-1-cyclohexylethyl]benzimidazole-5-carboxamideIC506600.0 [1]
(~{s})-(4-Fluoranyl-2-Propyl-Phenyl)-(1~{h}-Imidazol-2-Yl)methanolIC504200.0 [1]
6-Fluoro-4-N-(furan-2-ylmethyl)-2-N-pentylquinazoline-2,4-diamineIC50690.0 [1]
1,7-Bis(4-methoxyphenyl)-3,5-heptanedioneIC5067800.0 [1]
(2S)-4-Amino-N-[(2R)-1-anilino-1-oxo-3-phenylpropan-2-yl]-2-[[2-[[1-[(2,6-dichlorophenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-5-yl]carbamoylamino]acetyl]amino]butanamideKi1940.0 [1]
(2S)-6-Amino-N-[(2R)-1-(benzhydrylamino)-1-oxo-3-phenylpropan-2-yl]-2-[[2-[[1-[(2,6-dichlorophenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-5-yl]carbamoylamino]acetyl]amino]hexanamideKi627.0 [1]
2-(3,5-Dichlorophenoxy)-6-fluoro-N-[(3-methylfuran-2-yl)methyl]quinazolin-4-amineIC502800.0 [1]
2-(2,4-Dichlorophenoxy)-6-methoxy-N-[(3-methylfuran-2-yl)methyl]quinazolin-4-amineIC5010000.0 [1]
3-(Aminomethyl)-N-[(2S)-3-cyclohexyl-1-[[(2S,3S)-3-methyl-1-oxo-1-spiro[indene-1,4'-piperidine]-1'-ylpentan-2-yl]amino]-1-oxopropan-2-yl]-1,2-oxazole-5-carboxamideIC5010000.0 [1]
N-[(2S)-3-Cyclohexyl-1-[[(2S,3S)-3-methyl-1-oxo-1-spiro[indene-1,4'-piperidine]-1'-ylpentan-2-yl]amino]-1-oxopropan-2-yl]-1H-imidazole-5-carboxamideIC503162.28 [1]
(1S,3S)-5-(4-Fluorophenyl)-1-(5-phenyl-1,2-oxazol-3-yl)pentane-1,3-diolIC506000.0 [1]
N-[(2S)-1-[[(2S,3S)-1-[(2S)-2-(Tert-butylcarbamoyl)piperidin-1-yl]-3-methyl-1-oxopentan-2-yl]amino]-3-cyclohexyl-1-oxopropan-2-yl]-1,2-oxazole-5-carboxamideIC507943.28 [1]
N-[(2S)-3-Cyclohexyl-1-[[(2S,3S)-3-methyl-1-oxo-1-spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-ylpentan-2-yl]amino]-1-oxopropan-2-yl]-1,2-oxazole-5-carboxamideIC501995.26 [1]
3-Amino-N-[(2S)-3-cyclohexyl-1-[[(2S,3S)-3-methyl-1-oxo-1-spiro[indene-1,4'-piperidine]-1'-ylpentan-2-yl]amino]-1-oxopropan-2-yl]-1,2-oxazole-5-carboxamideIC501258.93 [1]
(4-(Cyclohexanecarbonyl)piperazin-1-yl)(2-methyl-3-phenyl imidazo[1,2-a]pyridin-6-yl)methanoneIC5077000.0 [1]
Methylbenzyl methylbenzimidazole piperidinylmethanoneIC50243000.0 [1]
2-Bromo-N-[2-(4-fluorophenyl)-4-oxoquinazolin-3-yl]-5-methoxybenzamideIC5034000.0 [1]
N-[(2S)-1-[[(2S,3S)-1-[(2-Butan-2-yloxyphenyl)methylamino]-3-methyl-1-oxopentan-2-yl]amino]-3-cyclohexyl-1-oxopropan-2-yl]-1,2-oxazole-5-carboxamideIC501000.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-Amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylpentanoyl]amino]-N-[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-methylpentanamideIC50700000.0 [1]
(2S)-6-Amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-carbamimidamido-2-(hexadecanoylamino)pentanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-carboxypropanoyl]amino]-4-carboxybutanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]hexanoyl]amino]hexanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-3-hydroxypropanoyl]amino]propanoyl]amino]-3-methylpentanoyl]amino]hexanoic acidIC50140.0 [1]
Items per page: 1 - 10 of 35
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References

This online tool may be cited as follows

MLA

"Quest Database™ Proteinase-activated receptor 2 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Feb. 2025, https://www.aatbio.com/data-sets/proteinase-activated-receptor-2-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2025, February 21). Quest Database™ Proteinase-activated receptor 2 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/proteinase-activated-receptor-2-inhibitors-ic50-ki.
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