Fibroblast activation protein alpha Inhibitors (IC50, Ki)

Structure ▲ ▼	Compound Name ▲ ▼	Standard Type ▲ ▼	Standard Values (in nM) ▲ ▼
	Sitagliptin	IC50	100000.0 [1]
	Vildagliptin	IC50	20000.0 [1]
	Linagliptin	IC50	70.8 [1], 89.0 [2], 370.0 [3]
	Alogliptin	IC50	100000.0 [1]
	Talabostat	IC50	12.0 [1], 24.0 [2], 70.0 [3]
	N-(1-Napthalenecarbonyl)-Gly-boroPro	IC50	2.3 [1], 19.0 [2]
	N-(1-Napthalenecarbonyl)-Gly-boroPro	Ki	7.9 [1]
	(R)-1-(2-(1-Oxoisoindolin-2-yl)acetyl)pyrrolidin-2-ylboronic acid	IC50	93.0 [1], 120.0 [2]
	(R)-1-(2-(1-Oxoisoindolin-2-yl)acetyl)pyrrolidin-2-ylboronic acid	Ki	7.5 [1]
	Py(D)AlaboroPro	IC50	36.0 [1]
	Py(D)AlaboroPro	Ki	9.0 [1]
	2-[3-[2-[2-Cyano-(S)-pyrrolidin-1-yl]-2-oxoethylamino]-3-methyl-1-oxobutyl]-1,3-dihydroisoindole	IC50	20000.0 [1], 100000.0 [2]
	(R)-1-(2-Acetamidoacetyl)pyrrolidin-2-ylboronic acid	Ki	23.0 [1]
	3-[[2-[(2S)-2-Cyanopyrrolidin-1-yl]-2-oxoethyl]amino]-N-(3,4-dimethoxyphenyl)-3-methylbutanamide	IC50	20000.0 [1], 50000.0 [2]
	(R)-1-(2-(2,5-Dichlorobenzamido)acetyl)pyrrolidin-2-ylboronic acid	Ki	29.0 [1]
	(R)-1-((R)-2-Acetamidopropanoyl)pyrrolidin-2-ylboronic acid	IC50	2900.0 [1]
	(R)-1-((R)-2-Acetamidopropanoyl)pyrrolidin-2-ylboronic acid	Ki	350.0 [1]
	(2S)-1-[(2S,4S)-4-[2-(1,3-Dihydroisoindol-2-yl)-2-oxoethyl]-5-oxopyrrolidine-2-carbonyl]-4,4-difluoropyrrolidine-2-carbonitrile	IC50	22.0 [1]
	(2S)-1-[(2S,4S)-4-[2-(1,3-Dihydroisoindol-2-yl)-2-oxoethyl]-5-oxopyrrolidine-2-carbonyl]-4,4-difluoropyrrolidine-2-carbonitrile	Ki	1.3 [1]
	N-[4-[(1R)-1-Amino-2-(2,5-difluorophenyl)ethyl]cyclohexyl]-N-methylacetamide	IC50	35000.0 [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]ethanamine	IC50	35000.0 [1]
	1-[4-[(1R)-1-Amino-2-(2,5-difluorophenyl)ethyl]cyclohexyl]piperidine-3-carboxamide	IC50	35000.0 [1]
	(1R)-2-(2,5-Difluorophenyl)-1-[4-(3,3-difluoropyrrolidin-1-yl)cyclohexyl]ethanamine	IC50	35000.0 [1]
	cis-(R)-2-(2,5-Difluorophenyl)-1-(4-(piperidin-1-yl)cyclohexyl)ethanamine	IC50	35000.0 [1]
	Anagliptin	IC50	72700.0 [1]
	Omarigliptin	IC50	67000.0 [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;hydrochloride	IC50	40000.0 [1]
	Dutogliptin	IC50	7520.0 [1]
	Gosogliptin	IC50	10300.0 [1]
	Allo-Ile-Isoindoline	IC50	100000.0 [1]
	Abt-279	Ki	30000.0 [1]
	N-[4-((S)-1-Amino-2-oxo-2-thiazolidin-3-yl-ethyl)-cyclohexyl]-4-trifluoromethoxy-benzenesulfonamide	IC50	35000.0 [1]
	(R)-1-(2-Aminoacetyl)pyrrolidin-2-ylboronic acid	IC50	52.0 [1]
	(2S)-1-[(2S)-2-Amino-4-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]-4-oxobutanoyl]pyrrolidine-2-carbonitrile	IC50	100000.0 [1]
	Val-boroAla	IC50	22000.0 [1]
	[(2R)-1-[(2R)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid	IC50	11.0 [1]
	(2S)-2-Amino-4-[(2-chlorophenyl)methylamino]-1-piperidin-1-ylbutan-1-one	IC50	100000.0 [1]
	DPPI 1c hydrochloride	IC50	30000.0 [1]
	3-[[2-[(2S)-2-Cyanopyrrolidin-1-yl]-2-oxoethyl]amino]-N-(2-phenylethyl)propanamide	IC50	20000.0 [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 acid	IC50	40000.0 [1]
	3-[2-(2-Cyanopyrrolidin-1-yl)-2-oxo-ethylamino]-3-methyl-N-(1-methyl-1-phenylethyl)butyramide	IC50	20000.0 [1]
	N-Benzyl-3-[[2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino]propanamide	IC50	20000.0 [1]
	3-[2-(2-Cyano-(S)-pyrrolidin-1-yl)-2-oxoethylamino]-N-(1-methyl-1-phenylethyl)propionamide	IC50	20000.0 [1]
	N-[2-[(2S)-2-Cyanopyrrolidin-1-yl]-2-oxoethyl]naphthalene-1-carboxamide	IC50	610.0 [1]
	(2S)-2-Cyano-1-(4-phenyl-L-phenylalanyl)pyrrolidine	IC50	1410.0 [1]
	(2R,3S,5R)-2-(2,5-Difluorophenyl)-5-(4,6-dihydro-1H-pyrrolo[3,4-c]pyrazol-5-yl)oxan-3-amine	IC50	22000.0 [1]
	2-[[6-[(3R)-3-Amino-3-methylpiperidin-1-yl]-1,3-dimethyl-2,4-dioxopyrrolo[3,2-d]pyrimidin-5-yl]methyl]-4-fluorobenzonitrile	IC50	50000.0 [1]
	N-[4-[(1S)-1-Amino-2-oxo-2-(1,3-thiazolidin-3-yl)ethyl]cyclohexyl]-4-(trifluoromethoxy)benzamide	IC50	35000.0 [1]
	[(2R)-1-[(2R)-2-Aminopropanoyl]pyrrolidin-2-yl]boronic acid	IC50	7800.0 [1]
	(2S)-1-(2-Benzyl-3-oxo-1H-isoindole-4-carbonyl)pyrrolidine-2-carbonitrile	IC50	100000.0 [1]
	(S)-N-(2-(2-Cyano-4,4-difluoropyrrolidin-1-yl)-2-oxoethyl)quinoline-4-carboxamide	IC50	3.3 [1]
	(2S,4S)-1-[(2R)-2-Amino-3-[(4-methoxyphenyl)methylsulfonyl]-3-methylbutanoyl]-4-fluoropyrrolidine-2-carbonitrile	Ki	23440.0 [1]
	(2S,4S)-1-[(2R)-2-Amino-3-[(4-fluorophenyl)methylsulfonyl]-3-methylbutanoyl]-4-fluoropyrrolidine-2-carbonitrile	Ki	23440.0 [1]
	(2S,4S)-1-[(2R)-2-Amino-3-methyl-3-(pyridin-2-ylmethylsulfanyl)butanoyl]-4-fluoropyrrolidine-2-carbonitrile	Ki	19076.0 [1]
	(2S,4S)-1-((R)-2-Amino-3-(benzylsulfonyl)-3-methylbutanoyl)-4-fluoropyrrolidine-2-carbonitrile	Ki	23440.0 [1]
	(2S,4S)-1-[(2R)-2-Amino-3-[(4-methoxyphenyl)methylsulfinyl]-3-methylbutanoyl]-4-fluoropyrrolidine-2-carbonitrile	Ki	23440.0 [1]
	(2S,4S)-1-[(2R)-2-Amino-3-[(4-cyanophenyl)methylsulfonyl]-3-methylbutanoyl]-4-fluoropyrrolidine-2-carbonitrile	Ki	9450.0 [1]
	(2S,4S)-1-[(2R)-2-Amino-3-[(3-methoxyphenyl)methylsulfonyl]-3-methylbutanoyl]-4-fluoropyrrolidine-2-carbonitrile	Ki	16980.0 [1]
	(2S,4S)-1-[(2R)-2-Amino-3-methyl-3-[(4-phenylmethoxyphenyl)methylsulfonyl]butanoyl]-4-fluoropyrrolidine-2-carbonitrile	Ki	20395.0 [1]
	(2S,4S)-1-[(2R)-2-Amino-3-methyl-3-[(4-phenylphenyl)methylsulfonyl]butanoyl]-4-fluoropyrrolidine-2-carbonitrile	Ki	9660.0 [1]
	(2S,4S)-1-((R)-3-(4-Methoxybenzylthio)-2-amino-3-methylbutanoyl)-4-fluoropyrrolidine-2-carbonitrile	Ki	23440.0 [1]
	(2S,4S)-1-[(2R)-2-Amino-3-[3-(4-fluorophenyl)propylsulfanyl]-3-methylbutanoyl]-4-fluoropyrrolidine-2-carbonitrile	Ki	15776.0 [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-trifluoromethanesulfonamide	IC50	34180.0 [1]
	1-(Quinazoline-2-ylmethyl)-3-methyl-7-(2-butynyl)-8-piperazinoxanthine	IC50	1800.0 [1]
	7-But-2-ynyl-1-[(4-methoxyquinazolin-2-yl)methyl]-3-methyl-8-piperazin-1-ylpurine-2,6-dione	IC50	1200.0 [1]
	1-(Quinoline-2-ylmethyl)-3-methyl-7-(2-butynyl)-8-piperazinoxanthine	IC50	10300.0 [1]
	(2S,4S)-1-[(2R)-2-Amino-3-methyl-3-(3-phenylpropylsulfonyl)butanoyl]-4-fluoropyrrolidine-2-carbonitrile	Ki	23440.0 [1]
	(2S,4S)-1-[(2R)-2-Amino-3-[(2-methoxyphenyl)methylsulfonyl]-3-methylbutanoyl]-4-fluoropyrrolidine-2-carbonitrile	Ki	12380.0 [1]
	(2S,4S)-1-[(2R)-2-Amino-3-methyl-3-[[4-(trifluoromethyl)phenyl]methylsulfanyl]butanoyl]-4-fluoropyrrolidine-2-carbonitrile	Ki	23440.0 [1]
	(2S,4S)-1-((R)-2-Amino-3-methyl-3-(phenethylthio)butanoyl)-4-fluoropyrrolidine-2-carbonitrile	Ki	23440.0 [1]
	(2S,4S)-1-[(2R)-2-Amino-3-methyl-3-(pyridin-4-ylmethylsulfonyl)butanoyl]-4-fluoropyrrolidine-2-carbonitrile	Ki	23440.0 [1]
	(2S,4S)-1-[(2R)-2-Amino-3-methyl-3-[(4-methylsulfonylphenyl)methylsulfonyl]butanoyl]-4-fluoropyrrolidine-2-carbonitrile	Ki	23440.0 [1]
	(2S,4S)-1-[(2R)-2-Amino-3-methyl-3-(pyridin-4-ylmethylsulfanyl)butanoyl]-4-fluoropyrrolidine-2-carbonitrile	Ki	9660.0 [1]
	(2S,4S)-1-[(2R)-2-Amino-3-methyl-3-[(4-methylphenyl)methylsulfonyl]butanoyl]-4-fluoropyrrolidine-2-carbonitrile	Ki	23440.0 [1]
	(2S,4S)-1-((R)-2-Amino-3-methyl-3-(3-phenylpropylthio)butanoyl)-4-fluoropyrrolidine-2-carbonitrile	Ki	12176.0 [1]
	(2S,4S)-1-((R)-3-(3-Phenoxybenzylthio)-2-amino-3-methylbutanoyl)-4-fluoropyrrolidine-2-carbonitrile	Ki	12845.0 [1]
	(2S,4S)-1-[(2R)-2-Amino-3-methyl-3-[(3-phenoxyphenyl)methylsulfonyl]butanoyl]-4-fluoropyrrolidine-2-carbonitrile	Ki	6863.0 [1]
	[(2S)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid	IC50	11.0 [1]
	6-Chloro-5-[[(2R,5S)-5-[(2S)-2-cyanopyrrolidine-1-carbonyl]pyrrolidin-2-yl]methoxy]pyridine-3-carboxylic acid	Ki	2200.0 [1]
	(2S)-1-{[(2S,5R)-5-(2-Chlorophenoxymethyl)pyrrolidin-2-yl]carbonyl}pyrrolidine-2-carbonitrile	Ki	479.0 [1]
	3-Chloro-4-{[(2R,5S)-5-{[(2S)-2-cyanopyrrolidin-1-yl]carbonyl}pyrrolidin-2-yl]methoxy}benzoic acid	Ki	536.0 [1]
	4-[[(2R,5S)-5-[(2S)-2-Cyanopyrrolidine-1-carbonyl]pyrrolidin-2-yl]methoxy]naphthalene-1-carboxylic acid	Ki	240.0 [1]
	(2S)-1-[(2S,5R)-5-[(2-Chloro-4-cyanophenoxy)methyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonitrile	Ki	505.0 [1]
	1-(4-Methylquinazoline-2-ylmethyl)-3-methyl-7-(2-butynyl)-8-piperazinoxanthine	IC50	740.0 [1]
	4-[[(2R,5S)-5-[(2S)-2-Cyanopyrrolidine-1-carbonyl]pyrrolidin-2-yl]methoxy]-3-propan-2-ylbenzoic acid	Ki	888.0 [1]
	4-Chloro-3-{[(2R,5S)-5-{[(2S)-2-cyanopyrrolidin-1-yl]carbonyl}pyrrolidin-2-yl]methoxy}benzoic acid	Ki	1770.0 [1]
	(2S)-1-[(2S,5R)-5-[(2-Chloro-4-methylsulfonylphenoxy)methyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonitrile	Ki	394.0 [1]
	6-Chloro-5-[[(2R,5S)-5-[(2S)-2-cyanopyrrolidine-1-carbonyl]pyrrolidin-2-yl]methoxy]-1-oxidopyridin-1-ium-3-carboxylic acid	Ki	1527.0 [1]
	(2R,5S)-1-(2-(1-(Ethoxymethyl)cyclopentylamino)acetyl)pyrrolidine-2,5-dicarbonitrile	IC50	30000.0 [1]
	(2R,5S)-1-(2-(1-(Butoxymethyl)cyclopentylamino)acetyl)pyrrolidine-2,5-dicarbonitrile	IC50	30000.0 [1]
	(1S,2R,5S)-5-(Isoindolin-2-yl)-2-(2,4,5-trifluorophenyl)cyclohexanamine	IC50	7000.0 [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-amine	IC50	60000.0 [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 acid	IC50	40000.0 [1]
	(2S,5R)-1-[2-(1-Adamantylamino)acetyl]pyrrolidine-2,5-dicarbonitrile	IC50	30000.0 [1]
	(2R,5S)-1-(2-(1-(Methoxymethyl)cyclopentylamino)acetyl)pyrrolidine-2,5-dicarbonitrile	IC50	30000.0 [1]
	(R)-1-((S)-2,4-Diaminobutanamido)pentylboronic acid	IC50	33000.0 [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 acid	IC50	40000.0 [1]
	(2R,5S)-1-[2-[(3-Hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2,5-dicarbonitrile	IC50	30000.0 [1]
	(2S,5R)-1-[2-(3-Tricyclo[3.3.1.03,7]nonanylamino)acetyl]pyrrolidine-2,5-dicarbonitrile	IC50	30000.0 [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 acid	IC50	40000.0 [1]

Entire TableStructureCompound NameStandard TypeStandard Values (in nM)

Items per page: 510All1 - 10 of 100 ⟨⟩

---

---

References

This online tool may be cited as follows

MLA	"Quest Database™ Fibroblast activation protein alpha Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 9 May. 2024, https://www.aatbio.com/data-sets/fibroblast-activation-protein-alpha-inhibitors-ic50-ki.
APA	AAT Bioquest, Inc. (2024, May 9). Quest Database™ Fibroblast activation protein alpha Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/fibroblast-activation-protein-alpha-inhibitors-ic50-ki.
BibTeX	EndNote	RefMan