Proton-coupled folate transporter Inhibitors (IC50, Ki)

Structure ▲ ▼	Compound Name ▲ ▼	Standard Type ▲ ▼	Standard Values (in nM) ▲ ▼
	Pemetrexed	IC50	13.2 [1]
	Pemetrexed	Ki	94.0 [1], 96.0 [2], 259.0 [3], 1540.0 [4], 2540.0 [5]
	(2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]pentanedioic acid	IC50	3.34 [1]
	(2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]pentanedioic acid	Ki	130.0 [1], 330.0 [2], 1820.0 [3]
	(2S)-2-[[5-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-2-carbonyl]amino]pentanedioic acid	IC50	43.4 [1]
	(2S)-2-[[5-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-2-carbonyl]amino]pentanedioic acid	Ki	130.0 [1], 230.0 [2], 1950.0 [3], 7230.0 [4]
	Methotrexate	IC50	120.5 [1], 121.0 [2]
	Raltitrexed	IC50	99.5 [1]
	N-{4-[4-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl}-L-glutamic Acid	IC50	213.0 [1]
	N-{4-[4-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl}-L-glutamic Acid	Ki	460.0 [1]
	(2S)-2-[[4-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-2-carbonyl]amino]pentanedioic acid	Ki	390.0 [1], 28100.0 [2]
	(2S)-2-[[5-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-3-carbonyl]amino]pentanedioic acid	Ki	420.0 [1], 30700.0 [2]
	(2S)-2-[[5-[5-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)pentyl]thiophene-2-carbonyl]amino]pentanedioic acid	Ki	100.0 [1], 2230.0 [2]
	(2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]hexanedioic acid	IC50	1000.0 [1]
	(2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]hexanedioic acid	Ki	1600.0 [1]
	(2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]pentanoic acid	IC50	1000.0 [1]
	(2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]pentanoic acid	Ki	2900.0 [1]
	(2S)-2-[[5-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]pyridine-2-carbonyl]amino]pentanedioic acid	IC50	57.6 [1]
	(2S)-2-[[5-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]pyridine-2-carbonyl]amino]pentanedioic acid	Ki	332.0 [1]
	Pralatrexate	IC50	57.0 [1]
	(2S)-2-[[5-[(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)methyl]thiophene-2-carbonyl]amino]pentanedioic acid	IC50	1000.0 [1]
	(2S)-2-[[5-[2-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)ethyl]thiophene-2-carbonyl]amino]pentanedioic acid	IC50	80.2 [1]
	(2S)-2-[[4-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]pentanedioic acid	IC50	5.39 [1]
	(2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-3-carbonyl]amino]pentanedioic acid	IC50	6.51 [1]
	(2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)propyl]thiophene-2-carbonyl]amino]pentanedioic acid	IC50	312.0 [1]
	4-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]butanoic acid	IC50	1000.0 [1]
	(2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]butanedioic acid	IC50	1000.0 [1]
	5-[3-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-propyl]-thiophene-2-carboxylic acid	IC50	1000.0 [1]
	(2S)-2-[[6-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]pyridine-3-carbonyl]amino]pentanedioic acid	IC50	1000.0 [1]
	(2S)-2-[[6-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)but-1-ynyl]pyridine-2-carbonyl]amino]pentanedioic acid	IC50	1000.0 [1]
	(2S)-2-[[6-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]pyridine-2-carbonyl]amino]pentanedioic acid	IC50	1000.0 [1]
	(2S)-2-[[6-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)but-1-ynyl]pyridine-3-carbonyl]amino]pentanedioic acid	IC50	1000.0 [1]
	(2S)-2-[[5-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)but-1-ynyl]pyridine-2-carbonyl]amino]pentanedioic acid	IC50	1000.0 [1]
	(2S)-2-[[5-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)butyl]thiophene-2-carbonyl]amino]pentanedioic acid	IC50	141.0 [1]
	(2S)-2-[[5-[5-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)pentyl]thiophene-2-carbonyl]amino]pentanedioic acid	IC50	57.4 [1]
	(2S)-2-[[5-[6-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)hexyl]thiophene-2-carbonyl]amino]pentanedioic acid	IC50	1000.0 [1]
	(S)-2-(4-(3-(2,4-Diaminofuro[2,3-d]pyrimidine-5-yl)propyl)-2-thienylcarbonylamino)glutaric acid	IC50	1000.0 [1]
	(S)-2-(2-(3-(2,4-Diaminofuro[2,3-d]pyrimidine-5-yl)propyl)-4-thienylcarbonylamino)glutaric acid	IC50	1000.0 [1]

Entire TableStructureCompound NameStandard TypeStandard Values (in nM)

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References

This online tool may be cited as follows

MLA	"Quest Database™ Proton-coupled folate transporter Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 22 Feb. 2025, https://www.aatbio.com/data-sets/proton-coupled-folate-transporter-inhibitors-ic50-ki.
APA	AAT Bioquest, Inc. (2025, February 22). Quest Database™ Proton-coupled folate transporter Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/proton-coupled-folate-transporter-inhibitors-ic50-ki.
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