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Dihydrofolate reductase Inhibitors (IC50, Ki)

Structure
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▼
Compound Name
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Standard Type
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▼
Standard Values (in nM)
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▼
MethotrexateIC5020.0 [1]
MethotrexateKi0.01 [1]
TrimethoprimIC50198000.0 [1]
TrimethoprimKi1380.0 [1]
PemetrexedIC506600.0 [1]
PemetrexedKi7.0 [1], 7.2 [2]
PyrimethamineIC50400.0 [1], 2600.0 [2], 4300.0 [3], 6000.0 [4]
PyrimethamineKi98.0 [1]
TrimetrexateIC5012.2 [1]
TrimetrexateKi1.4 [1], 13.0 [2], 83.0 [3]
AminopterinIC5025.0 [1]
AminopterinKi0.0 [1], 0.21 [2]
L-Glutamic acid, N-(4-(((2-amino-1,4-dihydro-4-oxo-6-quinazolinyl)methyl)-2-propynylamino)benzoyl)-IC501900.0 [1]
PiritreximIC502.0 [1], 3.0 [2]
PiritreximKi0.03 [1], 33.0 [2], 38.0 [3]
N-[4-[2-(2,4-Diaminofuro[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acidIC501000.0 [1]
(2S)-2-[[4-[(2-Amino-6-methyl-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]amino]pentanedioic acidIC502100.0 [1], 2200.0 [2]
IclaprimIC508.0 [1], 30000.0 [2]
IclaprimKi775.0 [1]
2,4-Diamino-5-(3-methoxybenzyl)pyrimidineKi9.6 [1], 300.0 [2], 1000.0 [3], 2300.0 [4]
2,4-Diamino-5-[3-benzyloxybenzyl]pyrimidineKi11.0 [1], 65.0 [2], 200.0 [3], 1000.0 [4]
2,4-Diamino-5-[3-octyloxybenzyl]pyrimidineKi24.0 [1], 97.0 [2], 1130.0 [3], 2400.0 [4]
2,4-Diamino-5-[3-hexyloxybenzyl]pyrimidineKi9.8 [1], 171.0 [2], 600.0 [3], 1900.0 [4]
2,4-Diamino-5-[3-butoxybenzyl]pyrimidineKi3.6 [1], 150.0 [2], 220.0 [3], 930.0 [4]
2,4-Diamino-5-[3-heptyloxybenzyl]pyrimidineKi131.0 [1], 221.0 [2], 620.0 [3], 1330.0 [4]
DpmabgIC50220.0 [1], 450.0 [2]
5-(4-Propoxybenzyl)pyrimidine-2,4-diamineKi6.4 [1], 230.0 [2], 330.0 [3], 2900.0 [4]
5-(4-Ethoxybenzyl)pyrimidine-2,4-diamineKi9.8 [1], 130.0 [2], 210.0 [3], 6000.0 [4]
5-[3-(Nonyloxy)benzyl]pyrimidine-2,4-diamineKi36.0 [1], 360.0 [2], 990.0 [3]
5-[3-(Decyloxy)benzyl]pyrimidine-2,4-diamineKi52.0 [1], 750.0 [2], 2220.0 [3], 3110.0 [4]
5-[3-(Heptyloxy)benzyl]-6-methylpyrimidine-2,4-diamineKi75.0 [1], 370.0 [2], 1000.0 [3], 1500.0 [4]
5-(3-Pentyloxy-benzyl)-pyrimidine-2,4-diamineKi7.1 [1], 140.0 [2], 210.0 [3], 1100.0 [4]
5-(3-Ethoxybenzyl)pyrimidine-2,4-diamineKi8.6 [1], 156.0 [2], 430.0 [3], 1600.0 [4]
5-(3-Propoxybenzyl)pyrimidine-2,4-diamineKi10.5 [1], 130.0 [2], 510.0 [3], 2400.0 [4]
5-(3-Isopropoxybenzyl)pyrimidine-2,4-diamineKi8.8 [1], 23.0 [2], 160.0 [3], 1400.0 [4]
5-[3-(Tetrahydro-pyran-2-yloxy)-benzyl]-pyrimidine-2,4-diamineKi13.0 [1], 93.0 [2], 360.0 [3], 1300.0 [4]
5-[3-(Heptyloxy)benzyl]-6-ethylpyrimidine-2,4-diamineKi19.0 [1], 48.0 [2], 400.0 [3], 710.0 [4]
5-[(6,7-Dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)methyl]pyrimidine-2,4-diamineIC5010.0 [1], 210.0 [2], 30000.0 [3]
CycloguanilKi55.6 [1], 410.0 [2], 43000.0 [3]
10-Propargyl-5,8-dideazafolic acidIC501900.0 [1], 11000.0 [2]
EpiroprimIC50200.0 [1], 600000.0 [2]
EpiroprimKi58.88 [1]
2-[[4-Carboxy-4-[[4-[(2,4-diaminopteridin-6-yl)methylamino]benzoyl]amino]butyl]carbamoyl]benzoic acidIC501.1 [1], 12.2 [2]
2-[[4-Carboxy-4-[[4-[(2,4-diaminopteridin-6-yl)methylamino]benzoyl]amino]butyl]carbamoyl]benzoic acidKi0.0 [1]
2,4-Diamino-5-[3-hydroxybenzyl]pyrimidineKi750.0 [1], 990.0 [2], 3300.0 [3]
2,4-Diamino-5-[2-Methoxy-5-(4-Carboxybutyloxy)benzyl]pyrimidineIC505000.0 [1], 8000.0 [2]
2-{4-[(2,4-Diamino-quinazolin-6-ylmethyl)-amino]-benzoylamino}-pentanedioic acidIC504.5 [1]
2-{4-[(2,4-Diamino-quinazolin-6-ylmethyl)-amino]-benzoylamino}-pentanedioic acidKi0.0 [1], 0.01 [2]
2-(4-((2-Amino-4-hydroxyquinazolin-6-yl) methylthio)benzamido)pentanedioic acidIC50330.0 [1]
5-[3-(3-Methoxy-5-phenyl-phenyl)but-1-ynyl]-6-methyl-pyrimidine-2,4-diamineIC501700.0 [1]
5-[3-(3-Methoxy-4-phenyl-phenyl)but-1-ynyl]-6-methyl-pyrimidine-2,4-diamineIC501420.0 [1]
2-[[4-[(2-Amino-4-oxo-3H-quinazolin-6-yl)methoxy]benzoyl]amino]pentanedioic acidIC50170.0 [1]
Furo[2,3d]pyrimidine antifolateIC50220.0 [1]
5-[3-(2,5-Dimethoxyphenyl)prop-1-Yn-1-Yl]-6-Ethylpyrimidine-2,4-DiamineIC501280.0 [1]
5-[3-[3-Methoxy-5-(p-tolyl)phenyl]but-1-ynyl]-6-methyl-pyrimidine-2,4-diamineIC501400.0 [1], 1410.0 [2]
5-Amino-2-[[4-[(2,4-diaminopteridin-6-yl)methyl-methylamino]benzoyl]amino]pentanoic acidIC501.0 [1], 2.5 [2], 160.0 [3]
2,4-Diamino-5-[3-(3-methoxy-5-(2-methylphenyl)phenyl)but-1-ynyl]-6-methylpyrimidineIC501360.0 [1]
5-[3-[3-(2,6-Dimethylphenyl)-5-methoxy-phenyl]but-1-ynyl]-6-methyl-pyrimidine-2,4-diamineIC501250.0 [1]
2,4-Diamino-5-[3-(3-methoxy-5-(2,6-diisopropylphenyl)phenyl)-but-1-ynyl]-6-methylpyrimidineIC507200.0 [1]
5-[(3r)-3-(5-Methoxybiphenyl-3-Yl)but-1-Yn-1-Yl]-6-Methylpyrimidine-2,4-DiamineIC501360.0 [1]
2-(4-{[(2,4-Diamino-furo[2,3-d]pyrimidin-5-ylmethyl)-amino]-methyl}-benzoylamino)-pentanedioic acidIC5010000.0 [1], 30500.0 [2], 200000.0 [3]
5-[(3S)-3-(3-Methoxy-5-phenylphenyl)but-1-yn-1-yl]-6-methylpyrimidine-2,4-diamineIC501380.0 [1]
5-[[(9R)-4-Methoxy-9-methyl-7,9-dihydro-6H-[1,3]dioxolo[4,5-h]isoquinolin-8-yl]methyl]pyrimidine-2,4-diamineIC502.8 [1], 9.8 [2], 1200.0 [3]
5-[[7-Methoxy-4-(3-nitrophenyl)-3,4-dihydro-1H-isoquinolin-2-yl]methyl]pyrimidine-2,4-diamineIC506.0 [1], 56.0 [2], 100000.0 [3]
5-[(4,11-Dimethyl-2,4-dihydro-1H-pyrido[4,3-a]carbazol-3-yl)methyl]pyrimidine-2,4-diamineIC504.0 [1], 10.0 [2], 85.0 [3]
5-[(6,7-Dimethoxy-1-methyl-3,4-dihydro-1H-isoquinolin-2-yl)methyl]pyrimidine-2,4-diamineIC5044.0 [1], 53.0 [2], 670.0 [3]
5-[(7-Chloro-10-methylsulfanyl-3,4-dihydro-1H-pyrazino[1,2-a]indol-2-yl)methyl]pyrimidine-2,4-diamineIC502.0 [1], 31.0 [2], 5200.0 [3]
5-[(7-Benzyl-1-methyl-6-phenyl-3,4-dihydro-1H-pyrrolo[1,2-a]pyrazin-2-yl)methyl]pyrimidine-2,4-diamineIC50450.0 [1], 550.0 [2], 18000.0 [3]
5-[[(9S)-4-Methoxy-9-methyl-7,9-dihydro-6H-[1,3]dioxolo[4,5-h]isoquinolin-8-yl]methyl]pyrimidine-2,4-diamineIC5021.0 [1], 29.0 [2], 520.0 [3]
5-[[4-(2,4-Dichlorophenyl)-6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl]methyl]pyrimidine-2,4-diamineIC507.0 [1], 31.0 [2], 1700.0 [3]
5-(1,3,4,9-Tetrahydropyrido[3,4-b]indol-2-ylmethyl)pyrimidine-2,4-diamineIC504.0 [1], 47.0 [2], 180000.0 [3]
2,4-Pyrimidinediamine, 5-[(3,4-dihydro-2(1H)-isoquinolinyl)methyl]-IC501100.0 [1], 5500.0 [2], 100000.0 [3]
5-[(4-Methoxy-9-methyl-7,9-dihydro-6H-[1,3]dioxolo[4,5-h]isoquinolin-8-yl)methyl]pyrimidine-2,4-diamineIC5012.0 [1], 24.0 [2], 1400.0 [3]
RaltitrexedIC5021000.0 [1]
EdatrexatoIC502.6 [1], 4.4 [2]
1,3,5-Triazine-2,4-diamine, 1-(3-chlorophenyl)-1,6-dihydro-6,6-dimethyl-Ki93.33 [1], 100.0 [2]
7H-Pyrrolo[3,2-f]quinazoline-1,3-diamineKi1.0 [1], 1000.0 [2]
N6-(2,5-Dimethoxy-benzyl)-N6-methyl-pyrido[2,3-D]pyrimidine-2,4,6-triamineIC508500.0 [1]
5-Methyl-6-(1-naphthylaminomethyl)pyrido[2,3-d]pyrimidine-2,4-diamineIC504.3 [1], 100.0 [2]
6-Methyl-5-[3-(3,4,5-trimethoxyphenyl)but-1-ynyl]pyrimidine-2,4-diamineIC501380.0 [1]
2-[[4-[[(2-Amino-4-oxo-3H-quinazolin-6-yl)amino]methyl]benzoyl]amino]pentanedioic acidIC50110.0 [1]
3-(2,4-Diamino-6-methylpyrimidin-5-yl)-1-(3,4,5-trimethoxyphenyl)prop-2-yn-1-olIC505710.0 [1]
2,4-Diamino-5-(3-(3,4,5-trimethoxyphenyl)prop-1-ynyl)-6-methylpyrimidineIC50400.0 [1]
2,4-Diamino-5-(3-methoxy-3-(3,4,5-trimethoxyphenyl)prop-1-ynyl)-6-methylpyrimidineIC501220.0 [1]
5-[(4-Methylphenyl)sulfanyl]-2,4-quinazolinediamineIC50940.0 [1]
2,4-Diamino-5-(3-(3,4,5-trimethoxyphenyl)prop-1-ynyl)pyrimidineIC501460.0 [1]
2,4-Diamino-5-(3-methoxy-3-(3,4,5-trimethoxyphenyl)prop-1-ynyl)pyrimidineIC501160.0 [1]
2,4-Diamino-5-(3-(3,4,5-trimethoxyphenyl)but-1-ynyl)pyrimidineIC501460.0 [1]
3-(2,4-Diaminopyrimidin-5-yl)-1-(3,4,5-trimethoxyphenyl)prop-2-yn-1-olIC5014300.0 [1]
1,3-Diamino-7-(1-ethylpropyl)-8-methyl-7H-pyrrolo(3,2-f)quinazolineKi0.0 [1], 0.3 [2]
6-Ethyl-5-[3-(3,4,5-Trimethoxyphenyl)prop-1-Yn-1-Yl]pyrimidine-2,4-DiamineIC5057.0 [1]
5-Phenylsulfanyl-2,4-quinazolinediamineIC50620.0 [1]
6-N-[(2,5-Dimethoxyphenyl)methyl]pyrido[2,3-d]pyrimidine-2,4,6-triamineIC5013000.0 [1]
5-[3-[(2,4-Diaminopyrimidin-5-yl)methyl]-4-methoxy-phenyl]pent-4-ynoic acidIC505000.0 [1], 30000.0 [2]
6-Methyl-5-[(3R)-3-(3,4,5-trimethoxyphenyl)but-1-ynyl]pyrimidine-2,4-diamineIC501380.0 [1]
5-[3-(2,5-Dimethoxyphenyl)prop-1-ynyl]-6-methyl-pyrimidine-2,4-diamineIC501300.0 [1]
2-[[4-[(2,4-Diamino-5-chloroquinazolin-6-yl)methylamino]benzoyl]amino]pentanedioic acidIC503.8 [1]
6-N-[(3,4,5-Trimethoxyphenyl)methyl]pyrido[2,3-d]pyrimidine-2,4,6-triamineIC5076000.0 [1]
(2S)-2-[[4-[(2,4-Diamino-5-methyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl)sulfanyl]benzoyl]amino]pentanedioic acidIC50210.0 [1]
5-Amino-2-[[4-[(2-amino-5-chloro-4-oxo-3H-quinazolin-6-yl)methylamino]benzoyl]amino]pentanoic acidIC50430.0 [1]
Items per page: 1 - 10 of 100
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References

This online tool may be cited as follows

MLA

"Quest Database™ Dihydrofolate reductase Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 20 Feb. 2025, https://www.aatbio.com/data-sets/dihydrofolate-reductase-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2025, February 20). Quest Database™ Dihydrofolate reductase Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/dihydrofolate-reductase-inhibitors-ic50-ki.
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