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Fibroblast activation protein alpha Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
SitagliptinIC50100000.0 [1]
VildagliptinIC5020000.0 [1]
LinagliptinIC5070.8 [1], 89.0 [2], 370.0 [3]
AlogliptinIC50100000.0 [1]
TalabostatIC5012.0 [1], 24.0 [2], 70.0 [3]
N-(1-Napthalenecarbonyl)-Gly-boroProIC502.3 [1], 19.0 [2]
N-(1-Napthalenecarbonyl)-Gly-boroProKi7.9 [1]
(R)-1-(2-(1-Oxoisoindolin-2-yl)acetyl)pyrrolidin-2-ylboronic acidIC5093.0 [1], 120.0 [2]
(R)-1-(2-(1-Oxoisoindolin-2-yl)acetyl)pyrrolidin-2-ylboronic acidKi7.5 [1]
Py(D)AlaboroProIC5036.0 [1]
Py(D)AlaboroProKi9.0 [1]
2-[3-[2-[2-Cyano-(S)-pyrrolidin-1-yl]-2-oxoethylamino]-3-methyl-1-oxobutyl]-1,3-dihydroisoindoleIC5020000.0 [1], 100000.0 [2]
(R)-1-(2-Acetamidoacetyl)pyrrolidin-2-ylboronic acidKi23.0 [1]
3-[[2-[(2S)-2-Cyanopyrrolidin-1-yl]-2-oxoethyl]amino]-N-(3,4-dimethoxyphenyl)-3-methylbutanamideIC5020000.0 [1], 50000.0 [2]
(R)-1-(2-(2,5-Dichlorobenzamido)acetyl)pyrrolidin-2-ylboronic acidKi29.0 [1]
(R)-1-((R)-2-Acetamidopropanoyl)pyrrolidin-2-ylboronic acidIC502900.0 [1]
(R)-1-((R)-2-Acetamidopropanoyl)pyrrolidin-2-ylboronic acidKi350.0 [1]
(2S)-1-[(2S,4S)-4-[2-(1,3-Dihydroisoindol-2-yl)-2-oxoethyl]-5-oxopyrrolidine-2-carbonyl]-4,4-difluoropyrrolidine-2-carbonitrileIC5022.0 [1]
(2S)-1-[(2S,4S)-4-[2-(1,3-Dihydroisoindol-2-yl)-2-oxoethyl]-5-oxopyrrolidine-2-carbonyl]-4,4-difluoropyrrolidine-2-carbonitrileKi1.3 [1]
N-[4-[(1R)-1-Amino-2-(2,5-difluorophenyl)ethyl]cyclohexyl]-N-methylacetamideIC5035000.0 [1]
(1R)-2-(2,5-Difluorophenyl)-1-[4-[3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]cyclohexyl]ethanamineIC5035000.0 [1]
1-[4-[(1R)-1-Amino-2-(2,5-difluorophenyl)ethyl]cyclohexyl]piperidine-3-carboxamideIC5035000.0 [1]
(1R)-2-(2,5-Difluorophenyl)-1-[4-(3,3-difluoropyrrolidin-1-yl)cyclohexyl]ethanamineIC5035000.0 [1]
cis-(R)-2-(2,5-Difluorophenyl)-1-(4-(piperidin-1-yl)cyclohexyl)ethanamineIC5035000.0 [1]
AnagliptinIC5072700.0 [1]
OmarigliptinIC5067000.0 [1]
(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-[4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]butanamide;hydrochlorideIC5040000.0 [1]
DutogliptinIC507520.0 [1]
GosogliptinIC5010300.0 [1]
Allo-Ile-IsoindolineIC50100000.0 [1]
Abt-279Ki30000.0 [1]
N-[4-((S)-1-Amino-2-oxo-2-thiazolidin-3-yl-ethyl)-cyclohexyl]-4-trifluoromethoxy-benzenesulfonamideIC5035000.0 [1]
(R)-1-(2-Aminoacetyl)pyrrolidin-2-ylboronic acidIC5052.0 [1]
(2S)-1-[(2S)-2-Amino-4-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]-4-oxobutanoyl]pyrrolidine-2-carbonitrileIC50100000.0 [1]
Val-boroAlaIC5022000.0 [1]
[(2R)-1-[(2R)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acidIC5011.0 [1]
(2S)-2-Amino-4-[(2-chlorophenyl)methylamino]-1-piperidin-1-ylbutan-1-oneIC50100000.0 [1]
DPPI 1c hydrochlorideIC5030000.0 [1]
3-[[2-[(2S)-2-Cyanopyrrolidin-1-yl]-2-oxoethyl]amino]-N-(2-phenylethyl)propanamideIC5020000.0 [1]
(2S,3S)-3-Amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxo-2-[4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]butanamide;2,2,2-trifluoroacetic acidIC5040000.0 [1]
3-[2-(2-Cyanopyrrolidin-1-yl)-2-oxo-ethylamino]-3-methyl-N-(1-methyl-1-phenylethyl)butyramideIC5020000.0 [1]
N-Benzyl-3-[[2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino]propanamideIC5020000.0 [1]
3-[2-(2-Cyano-(S)-pyrrolidin-1-yl)-2-oxoethylamino]-N-(1-methyl-1-phenylethyl)propionamideIC5020000.0 [1]
N-[2-[(2S)-2-Cyanopyrrolidin-1-yl]-2-oxoethyl]naphthalene-1-carboxamideIC50610.0 [1]
(2S)-2-Cyano-1-(4-phenyl-L-phenylalanyl)pyrrolidineIC501410.0 [1]
(2R,3S,5R)-2-(2,5-Difluorophenyl)-5-(4,6-dihydro-1H-pyrrolo[3,4-c]pyrazol-5-yl)oxan-3-amineIC5022000.0 [1]
2-[[6-[(3R)-3-Amino-3-methylpiperidin-1-yl]-1,3-dimethyl-2,4-dioxopyrrolo[3,2-d]pyrimidin-5-yl]methyl]-4-fluorobenzonitrileIC5050000.0 [1]
N-[4-[(1S)-1-Amino-2-oxo-2-(1,3-thiazolidin-3-yl)ethyl]cyclohexyl]-4-(trifluoromethoxy)benzamideIC5035000.0 [1]
[(2R)-1-[(2R)-2-Aminopropanoyl]pyrrolidin-2-yl]boronic acidIC507800.0 [1]
(2S)-1-(2-Benzyl-3-oxo-1H-isoindole-4-carbonyl)pyrrolidine-2-carbonitrileIC50100000.0 [1]
(S)-N-(2-(2-Cyano-4,4-difluoropyrrolidin-1-yl)-2-oxoethyl)quinoline-4-carboxamideIC503.3 [1]
(2S,4S)-1-[(2R)-2-Amino-3-[(4-methoxyphenyl)methylsulfonyl]-3-methylbutanoyl]-4-fluoropyrrolidine-2-carbonitrileKi23440.0 [1]
(2S,4S)-1-[(2R)-2-Amino-3-[(4-fluorophenyl)methylsulfonyl]-3-methylbutanoyl]-4-fluoropyrrolidine-2-carbonitrileKi23440.0 [1]
(2S,4S)-1-[(2R)-2-Amino-3-methyl-3-(pyridin-2-ylmethylsulfanyl)butanoyl]-4-fluoropyrrolidine-2-carbonitrileKi19076.0 [1]
(2S,4S)-1-((R)-2-Amino-3-(benzylsulfonyl)-3-methylbutanoyl)-4-fluoropyrrolidine-2-carbonitrileKi23440.0 [1]
(2S,4S)-1-[(2R)-2-Amino-3-[(4-methoxyphenyl)methylsulfinyl]-3-methylbutanoyl]-4-fluoropyrrolidine-2-carbonitrileKi23440.0 [1]
(2S,4S)-1-[(2R)-2-Amino-3-[(4-cyanophenyl)methylsulfonyl]-3-methylbutanoyl]-4-fluoropyrrolidine-2-carbonitrileKi9450.0 [1]
(2S,4S)-1-[(2R)-2-Amino-3-[(3-methoxyphenyl)methylsulfonyl]-3-methylbutanoyl]-4-fluoropyrrolidine-2-carbonitrileKi16980.0 [1]
(2S,4S)-1-[(2R)-2-Amino-3-methyl-3-[(4-phenylmethoxyphenyl)methylsulfonyl]butanoyl]-4-fluoropyrrolidine-2-carbonitrileKi20395.0 [1]
(2S,4S)-1-[(2R)-2-Amino-3-methyl-3-[(4-phenylphenyl)methylsulfonyl]butanoyl]-4-fluoropyrrolidine-2-carbonitrileKi9660.0 [1]
(2S,4S)-1-((R)-3-(4-Methoxybenzylthio)-2-amino-3-methylbutanoyl)-4-fluoropyrrolidine-2-carbonitrileKi23440.0 [1]
(2S,4S)-1-[(2R)-2-Amino-3-[3-(4-fluorophenyl)propylsulfanyl]-3-methylbutanoyl]-4-fluoropyrrolidine-2-carbonitrileKi15776.0 [1]
N-[[(2S,3As,7aS)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-2,3,3a,4,5,6,7,7a-octahydroindol-2-yl]methyl]-1,1,1-trifluoromethanesulfonamideIC5034180.0 [1]
1-(Quinazoline-2-ylmethyl)-3-methyl-7-(2-butynyl)-8-piperazinoxanthineIC501800.0 [1]
7-But-2-ynyl-1-[(4-methoxyquinazolin-2-yl)methyl]-3-methyl-8-piperazin-1-ylpurine-2,6-dioneIC501200.0 [1]
1-(Quinoline-2-ylmethyl)-3-methyl-7-(2-butynyl)-8-piperazinoxanthineIC5010300.0 [1]
(2S,4S)-1-[(2R)-2-Amino-3-methyl-3-(3-phenylpropylsulfonyl)butanoyl]-4-fluoropyrrolidine-2-carbonitrileKi23440.0 [1]
(2S,4S)-1-[(2R)-2-Amino-3-[(2-methoxyphenyl)methylsulfonyl]-3-methylbutanoyl]-4-fluoropyrrolidine-2-carbonitrileKi12380.0 [1]
(2S,4S)-1-[(2R)-2-Amino-3-methyl-3-[[4-(trifluoromethyl)phenyl]methylsulfanyl]butanoyl]-4-fluoropyrrolidine-2-carbonitrileKi23440.0 [1]
(2S,4S)-1-((R)-2-Amino-3-methyl-3-(phenethylthio)butanoyl)-4-fluoropyrrolidine-2-carbonitrileKi23440.0 [1]
(2S,4S)-1-[(2R)-2-Amino-3-methyl-3-(pyridin-4-ylmethylsulfonyl)butanoyl]-4-fluoropyrrolidine-2-carbonitrileKi23440.0 [1]
(2S,4S)-1-[(2R)-2-Amino-3-methyl-3-[(4-methylsulfonylphenyl)methylsulfonyl]butanoyl]-4-fluoropyrrolidine-2-carbonitrileKi23440.0 [1]
(2S,4S)-1-[(2R)-2-Amino-3-methyl-3-(pyridin-4-ylmethylsulfanyl)butanoyl]-4-fluoropyrrolidine-2-carbonitrileKi9660.0 [1]
(2S,4S)-1-[(2R)-2-Amino-3-methyl-3-[(4-methylphenyl)methylsulfonyl]butanoyl]-4-fluoropyrrolidine-2-carbonitrileKi23440.0 [1]
(2S,4S)-1-((R)-2-Amino-3-methyl-3-(3-phenylpropylthio)butanoyl)-4-fluoropyrrolidine-2-carbonitrileKi12176.0 [1]
(2S,4S)-1-((R)-3-(3-Phenoxybenzylthio)-2-amino-3-methylbutanoyl)-4-fluoropyrrolidine-2-carbonitrileKi12845.0 [1]
(2S,4S)-1-[(2R)-2-Amino-3-methyl-3-[(3-phenoxyphenyl)methylsulfonyl]butanoyl]-4-fluoropyrrolidine-2-carbonitrileKi6863.0 [1]
[(2S)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acidIC5011.0 [1]
6-Chloro-5-[[(2R,5S)-5-[(2S)-2-cyanopyrrolidine-1-carbonyl]pyrrolidin-2-yl]methoxy]pyridine-3-carboxylic acidKi2200.0 [1]
(2S)-1-{[(2S,5R)-5-(2-Chlorophenoxymethyl)pyrrolidin-2-yl]carbonyl}pyrrolidine-2-carbonitrileKi479.0 [1]
3-Chloro-4-{[(2R,5S)-5-{[(2S)-2-cyanopyrrolidin-1-yl]carbonyl}pyrrolidin-2-yl]methoxy}benzoic acidKi536.0 [1]
4-[[(2R,5S)-5-[(2S)-2-Cyanopyrrolidine-1-carbonyl]pyrrolidin-2-yl]methoxy]naphthalene-1-carboxylic acidKi240.0 [1]
(2S)-1-[(2S,5R)-5-[(2-Chloro-4-cyanophenoxy)methyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonitrileKi505.0 [1]
1-(4-Methylquinazoline-2-ylmethyl)-3-methyl-7-(2-butynyl)-8-piperazinoxanthineIC50740.0 [1]
4-[[(2R,5S)-5-[(2S)-2-Cyanopyrrolidine-1-carbonyl]pyrrolidin-2-yl]methoxy]-3-propan-2-ylbenzoic acidKi888.0 [1]
4-Chloro-3-{[(2R,5S)-5-{[(2S)-2-cyanopyrrolidin-1-yl]carbonyl}pyrrolidin-2-yl]methoxy}benzoic acidKi1770.0 [1]
(2S)-1-[(2S,5R)-5-[(2-Chloro-4-methylsulfonylphenoxy)methyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonitrileKi394.0 [1]
6-Chloro-5-[[(2R,5S)-5-[(2S)-2-cyanopyrrolidine-1-carbonyl]pyrrolidin-2-yl]methoxy]-1-oxidopyridin-1-ium-3-carboxylic acidKi1527.0 [1]
(2R,5S)-1-(2-(1-(Ethoxymethyl)cyclopentylamino)acetyl)pyrrolidine-2,5-dicarbonitrileIC5030000.0 [1]
(2R,5S)-1-(2-(1-(Butoxymethyl)cyclopentylamino)acetyl)pyrrolidine-2,5-dicarbonitrileIC5030000.0 [1]
(1S,2R,5S)-5-(Isoindolin-2-yl)-2-(2,4,5-trifluorophenyl)cyclohexanamineIC507000.0 [1]
(1S,2R,5S)-5-[3-(Trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-2-(2,4,5-trifluorophenyl)cyclohexan-1-amineIC5060000.0 [1]
(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-pyrazolo[1,5-a]pyrimidin-5-ylphenyl)butanamide;2,2,2-trifluoroacetic acidIC5040000.0 [1]
(2S,5R)-1-[2-(1-Adamantylamino)acetyl]pyrrolidine-2,5-dicarbonitrileIC5030000.0 [1]
(2R,5S)-1-(2-(1-(Methoxymethyl)cyclopentylamino)acetyl)pyrrolidine-2,5-dicarbonitrileIC5030000.0 [1]
(R)-1-((S)-2,4-Diaminobutanamido)pentylboronic acidIC5033000.0 [1]
(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-[4-([1,2,4]triazolo[1,5-a]pyridin-7-yl)phenyl]butanamide;2,2,2-trifluoroacetic acidIC5040000.0 [1]
(2R,5S)-1-[2-[(3-Hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2,5-dicarbonitrileIC5030000.0 [1]
(2S,5R)-1-[2-(3-Tricyclo[3.3.1.03,7]nonanylamino)acetyl]pyrrolidine-2,5-dicarbonitrileIC5030000.0 [1]
(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-[4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]butanamide;2,2,2-trifluoroacetic acidIC5040000.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Fibroblast activation protein alpha Inhibitors (IC50, Ki)." AAT Bioquest, Inc.21 Nov2024https://www.aatbio.com/data-sets/fibroblast-activation-protein-alpha-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024November 21). Quest Database™ Fibroblast activation protein alpha Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/fibroblast-activation-protein-alpha-inhibitors-ic50-ki.
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