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Proton-coupled folate transporter Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
PemetrexedIC5013.2 [1]
PemetrexedKi94.0 [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 acidIC503.34 [1]
(2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]pentanedioic acidKi130.0 [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 acidIC5043.4 [1]
(2S)-2-[[5-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-2-carbonyl]amino]pentanedioic acidKi130.0 [1], 230.0 [2], 1950.0 [3], 7230.0 [4]
MethotrexateIC50120.5 [1], 121.0 [2]
RaltitrexedIC5099.5 [1]
N-{4-[4-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl}-L-glutamic AcidIC50213.0 [1]
N-{4-[4-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl}-L-glutamic AcidKi460.0 [1]
(2S)-2-[[4-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-2-carbonyl]amino]pentanedioic acidKi390.0 [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 acidKi420.0 [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 acidKi100.0 [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 acidIC501000.0 [1]
(2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]hexanedioic acidKi1600.0 [1]
(2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]pentanoic acidIC501000.0 [1]
(2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]pentanoic acidKi2900.0 [1]
(2S)-2-[[5-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]pyridine-2-carbonyl]amino]pentanedioic acidIC5057.6 [1]
(2S)-2-[[5-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]pyridine-2-carbonyl]amino]pentanedioic acidKi332.0 [1]
PralatrexateIC5057.0 [1]
(2S)-2-[[5-[(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)methyl]thiophene-2-carbonyl]amino]pentanedioic acidIC501000.0 [1]
(2S)-2-[[5-[2-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)ethyl]thiophene-2-carbonyl]amino]pentanedioic acidIC5080.2 [1]
(2S)-2-[[4-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]pentanedioic acidIC505.39 [1]
(2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-3-carbonyl]amino]pentanedioic acidIC506.51 [1]
(2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)propyl]thiophene-2-carbonyl]amino]pentanedioic acidIC50312.0 [1]
4-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]butanoic acidIC501000.0 [1]
(2S)-2-[[5-[3-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]butanedioic acidIC501000.0 [1]
5-[3-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-propyl]-thiophene-2-carboxylic acidIC501000.0 [1]
(2S)-2-[[6-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]pyridine-3-carbonyl]amino]pentanedioic acidIC501000.0 [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 acidIC501000.0 [1]
(2S)-2-[[6-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]pyridine-2-carbonyl]amino]pentanedioic acidIC501000.0 [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 acidIC501000.0 [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 acidIC501000.0 [1]
(2S)-2-[[5-[4-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)butyl]thiophene-2-carbonyl]amino]pentanedioic acidIC50141.0 [1]
(2S)-2-[[5-[5-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)pentyl]thiophene-2-carbonyl]amino]pentanedioic acidIC5057.4 [1]
(2S)-2-[[5-[6-(2-Amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)hexyl]thiophene-2-carbonyl]amino]pentanedioic acidIC501000.0 [1]
(S)-2-(4-(3-(2,4-Diaminofuro[2,3-d]pyrimidine-5-yl)propyl)-2-thienylcarbonylamino)glutaric acidIC501000.0 [1]
(S)-2-(2-(3-(2,4-Diaminofuro[2,3-d]pyrimidine-5-yl)propyl)-4-thienylcarbonylamino)glutaric acidIC501000.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Proton-coupled folate transporter Inhibitors (IC50, Ki)." AAT Bioquest, Inc.8 May2024https://www.aatbio.com/data-sets/proton-coupled-folate-transporter-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 8). 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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