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Subtilisin/kexin type 9 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
N-(3-Chloropyridin-2-yl)-N-[(3R)-piperidin-3-yl]-4-(triazolo[4,5-b]pyridin-3-yl)benzamideIC50520.0 [1], 800.0 [2]
4-[4-[(3-Chloropyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]-2-methyl-N-methylsulfonylpyrazole-3-carboxamideIC5014300.0 [1], 20000.0 [2]
N-(3-Methylpyridin-2-yl)-N-[(3R)-piperidin-3-yl]-4-pyrazolo[1,5-a]pyrimidin-3-ylbenzamideIC50440.0 [1], 3200.0 [2]
[2-Methyl-1-[5-[2-methyl-4-[4-[(3-methylpyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]pyrazol-3-yl]tetrazol-2-yl]propyl] propanoateIC5015400.0 [1], 20000.0 [2]
Ethyl 1-[5-[2-methyl-4-[4-[(3-methylpyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]pyrazol-3-yl]tetrazol-2-yl]propyl carbonateIC5020000.0 [1], 23700.0 [2]
4-[4-[(3-Chloropyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]-2-methyl-N-(2H-tetrazol-5-yl)pyrazole-3-carboxamideIC5020000.0 [1], 25300.0 [2]
4-[4-[(3-Chloropyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]-N-hydroxy-2-methylpyrazole-3-carboxamideIC502970.0 [1], 20000.0 [2]
1-[5-[2-Methyl-4-[4-[(3-methylpyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]pyrazol-3-yl]tetrazol-2-yl]ethyl propan-2-yl carbonateIC50592.0 [1], 19400.0 [2]
[2,2-Dimethyl-1-[5-[2-methyl-4-[4-[(3-methylpyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]pyrazol-3-yl]tetrazol-2-yl]propyl] ethyl carbonateIC5020000.0 [1], 22900.0 [2]
1-[5-[2-Methyl-4-[4-[(3-methylpyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]pyrazol-3-yl]tetrazol-2-yl]propyl 2-methylpropanoateIC5020000.0 [1], 31800.0 [2]
1-[5-[2-Methyl-4-[4-[(3-methylpyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]pyrazol-3-yl]tetrazol-2-yl]propyl propan-2-yl carbonateIC5015400.0 [1], 19400.0 [2]
[2-Methyl-1-[5-[2-methyl-4-[4-[(3-methylpyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]pyrazol-3-yl]tetrazol-2-yl]propyl] propan-2-yl carbonateIC5020000.0 [1], 31900.0 [2]
1-[5-[2-Methyl-4-[4-[(3-methylpyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]pyrazol-3-yl]tetrazol-2-yl]ethyl propanoateIC5020000.0 [1], 25100.0 [2]
Ethyl [2-methyl-1-[5-[2-methyl-4-[4-[(3-methylpyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]pyrazol-3-yl]tetrazol-2-yl]propyl] carbonateIC506200.0 [1], 20000.0 [2]
1-[5-[2-Methyl-4-[4-[(3-methylpyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]pyrazol-3-yl]tetrazol-2-yl]propyl propanoateIC5020000.0 [1], 33400.0 [2]
4-[1-Methyl-5-(5-oxo-4H-1,2,4-oxadiazol-3-yl)pyrazol-4-yl]-N-(3-methylpyridin-2-yl)-N-[(3R)-piperidin-3-yl]benzamideIC505610.0 [1], 20000.0 [2]
N-(3-Chloropyridin-2-yl)-N-[(3R)-piperidin-3-yl]-4-pyrazolo[1,5-a]pyrimidin-3-ylbenzamideIC50690.0 [1], 1700.0 [2]
4-[4-[Isoquinolin-1-yl-[(3R)-piperidin-3-yl]carbamoyl]phenyl]-2-methylpyrazole-3-carboxylic acidIC503800.0 [1], 20000.0 [2]
Ethyl 4-[4-[(3-chloropyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]-2-methylpyrazole-3-carboxylateIC501500.0 [1], 1700.0 [2]
4-[4-[(3-Chloropyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]-2-methylpyrazole-3-carboxylic acidIC5018000.0 [1], 20000.0 [2]
1-Ethoxycarbonyloxyethyl 4-[4-[(3-chloropyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]-2-methylpyrazole-3-carboxylateIC503700.0 [1], 9500.0 [2]
[(1S)-1-Ethoxycarbonyloxyethyl] 4-[4-[(3-chloropyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]-2-methylpyrazole-3-carboxylateIC503100.0 [1], 7300.0 [2]
[(1R)-1-Ethoxycarbonyloxyethyl] 4-[4-[(3-chloropyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]-2-methylpyrazole-3-carboxylateIC505000.0 [1], 10700.0 [2]
Methyl 4-[4-[(3-chloropyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]-2-methylpyrazole-3-carboxylateIC50640.0 [1], 1500.0 [2]
1-Ethoxycarbonyloxyethyl 4-[4-[isoquinolin-1-yl-[(3R)-piperidin-3-yl]carbamoyl]phenyl]-2-methylpyrazole-3-carboxylateIC502100.0 [1], 11700.0 [2]
2-Methyl-4-[4-[(1-methylpyrrolo[2,3-c]pyridin-7-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]pyrazole-3-carboxylic acidIC501700.0 [1], 20000.0 [2]
Methyl 2-methyl-4-[4-[(3-methylpyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]pyrazole-3-carboxylateIC50800.0 [1], 2300.0 [2]
4-[4-[(3-Chloropyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]-2-methyl-N-(trifluoromethylsulfonyl)pyrazole-3-carboxamideIC505800.0 [1], 20000.0 [2]
N-(3-Chloropyridin-2-yl)-4-[1-methyl-5-(2H-tetrazol-5-yl)pyrazol-4-yl]-N-[(3R)-piperidin-3-yl]benzamideIC505750.0 [1], 20000.0 [2]
2-Methyl-4-[4-[(3-methylpyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]-N-methylsulfonylpyrazole-3-carboxamideIC5016800.0 [1], 20000.0 [2]
N-(3-Methylpyridin-2-yl)-4-[1-methyl-5-(2H-tetrazol-5-yl)pyrazol-4-yl]-N-[(3R)-piperidin-3-yl]benzamideIC503050.0 [1], 20000.0 [2]
1-[5-[2-Methyl-4-[4-[(3-methylpyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]pyrazol-3-yl]tetrazol-2-yl]ethyl 2-methylpropanoateIC503560.0 [1], 20000.0 [2]
[2-Methyl-1-[5-[2-methyl-4-[4-[(3-methylpyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]pyrazol-3-yl]tetrazol-2-yl]propyl] 2-methylpropanoateIC5019200.0 [1], 19800.0 [2]
Phenylboronic acidKi470000.0 [1]
Diphenylborinic acidKi30000.0 [1]
1-Methyl-2-[3-methyl-2-(3-methylimidazol-4-yl)imidazol-4-yl]-5-(1-methyl-5-phenylimidazol-2-yl)imidazoleIC5011200.0 [1]
(4S)-5-[[(2S)-1-[[(2S)-1-[(2S)-2-[[2-[[(2S)-1-[[(2S)-4-Amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-carbamimidamido-1-[[(2S,3S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(1S)-4-carbamimidamido-1-carboxybutyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]carbamoyl]pyrrolidin-1-yl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-[[(2S)-2-amino-4-methylsulfanylbutanoyl]amino]-5-oxopentanoic acidIC508300.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-Amino-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]butanedioic acidIC501600.0 [1]
(S)-2-Acetylamino-3-[4-(oxiran-2-ylmethoxy)phenyl]propionic acid ethyl esterKi200000.0 [1]
N-(3-Chloropyridin-2-yl)-4-(6-methyltriazolo[4,5-b]pyridin-3-yl)-N-[(3R)-piperidin-3-yl]benzamideIC50800.0 [1]
N-(3-Chloropyridin-2-yl)-N-[(3R)-piperidin-3-yl]-5-(triazolo[4,5-b]pyridin-3-yl)pyridine-2-carboxamideIC501500.0 [1]
N-(3-Chloropyridin-2-yl)-5-(6-methyltriazolo[4,5-b]pyridin-3-yl)-N-[(3R)-piperidin-3-yl]pyridine-2-carboxamideIC501800.0 [1]
Phenyl butyl borinic acidKi1000.0 [1]
1-Ethoxycarbonyloxyethyl 2-methyl-4-[4-[(1-methylpyrrolo[2,3-c]pyridin-7-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]pyrazole-3-carboxylateIC504500.0 [1]
Ethyl 1-[[2-methyl-4-[4-[(3-methylpyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]pyrazole-3-carbonyl]-methylsulfonylamino]ethyl carbonateIC5020000.0 [1]
Ethyl [(1S)-1-[5-[2-methyl-4-[4-[(3-methylpyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]pyrazol-3-yl]tetrazol-2-yl]ethyl] carbonateIC5016700.0 [1]
Ethyl 1-[5-[2-methyl-4-[4-[(3-methylpyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]pyrazol-3-yl]tetrazol-1-yl]ethyl carbonateIC5020000.0 [1]
Ethyl [(1R)-1-[5-[2-methyl-4-[4-[(3-methylpyridin-2-yl)-[(3R)-piperidin-3-yl]carbamoyl]phenyl]pyrazol-3-yl]tetrazol-2-yl]ethyl] carbonateIC5020000.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Subtilisin/kexin type 9 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.9 May2024https://www.aatbio.com/data-sets/subtilisin-kexin-type-9-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 9). Quest Database™ Subtilisin/kexin type 9 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/subtilisin-kexin-type-9-inhibitors-ic50-ki.
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