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Protein-glutamine gamma-glutamyltransferase Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
N-[(5S)-6-[4-(6-Methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamideIC5014.0 [1], 310.0 [2], 790.0 [3]
N-[(5S)-6-[4-(6-Methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamideKi5730.0 [1]
(E)-3-(2-Oxo-2-(pyridin-3-yl)ethylidene)indolin-2-oneIC508500.0 [1]
(E)-3-(2-Oxo-2-(pyridin-3-yl)ethylidene)indolin-2-oneKi12000.0 [1], 86000.0 [2]
(E)-4-Chloro-3-(2-(4-chlorophenyl)-2-oxoethylidene)indolin-2-oneIC5090.0 [1], 800.0 [2]
(E)-4-Chloro-3-(2-(4-chlorophenyl)-2-oxoethylidene)indolin-2-oneKi47000.0 [1]
(E)-4-Chloro-3-(2-(2-methoxyphenyl)-2-oxoethylidene)indolin-2-oneIC50740.0 [1], 900.0 [2]
(E)-4-Chloro-3-(2-(2-methoxyphenyl)-2-oxoethylidene)indolin-2-oneKi3300.0 [1]
(E)-4-Chloro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)-1-phenylindolin-2-oneIC50570.0 [1], 800.0 [2]
(E)-4-Chloro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)-1-phenylindolin-2-oneKi9100.0 [1]
N-[(5S)-6-[4-(6-Fluoropyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamideIC50110.0 [1], 1100.0 [2]
N-[(5S)-6-[4-(6-Fluoropyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamideKi6280.0 [1]
N-[(5S)-6-[4-(6-Nitropyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamideIC50100.0 [1], 400.0 [2]
N-[(5S)-6-[4-(6-Nitropyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamideKi2260.0 [1]
3-(2-Oxo-propylidene)-1,3-dihydro-indol-2-oneIC5019000.0 [1]
3-(2-Oxo-propylidene)-1,3-dihydro-indol-2-oneKi10000.0 [1]
Ethyl (E,6S)-7-[[(2S)-1-[(2S)-2-[[(2S)-1-methoxy-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino]-7-oxo-6-(phenylmethoxycarbonylamino)hept-2-enoateIC5030.0 [1]
2-[[3-(3-Fluorophenyl)-4-oxo-5-phenyl-5,6,7,8-tetrahydro-[1]benzothiolo[2,3-d]pyrimidin-2-yl]sulfanyl]acetohydrazideIC50170.0 [1], 930.0 [2]
Benzyl N-[4-(4-prop-2-enoylpiperazin-1-yl)sulfonylphenyl]carbamateIC502900.0 [1]
Ethyl (E,6S)-7-[[(2S)-5-amino-1-[(2S)-2-[[(2S)-1-methoxy-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-1,5-dioxopentan-2-yl]amino]-7-oxo-6-(phenylmethoxycarbonylamino)hept-2-enoateIC5020.0 [1]
2-(4-Oxo-5-phenyl-3-pyridin-3-ylthieno[2,3-d]pyrimidin-2-yl)sulfanylacetohydrazideIC50480.0 [1], 1200.0 [2]
2-(4-Oxo-3,5-diphenylthieno[2,3-d]pyrimidin-2-yl)sulfanylacetohydrazideIC50250.0 [1], 800.0 [2]
N-[(5S)-6-[4-[6-(2-Fluoroethoxy)pyridin-2-yl]piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamideIC50390.0 [1]
N-[(5S)-6-[4-[6-(2-Fluoroethoxy)pyridin-2-yl]piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamideKi7320.0 [1]
N-[(5S)-6-[4-(6-Tert-butylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamideIC50170.0 [1]
N-[(5S)-6-[4-(6-Tert-butylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamideKi3500.0 [1]
N-[(5S)-6-[4-(6-Iodopyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamideIC50140.0 [1]
N-[(5S)-6-[4-(6-Iodopyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamideKi2920.0 [1]
N-[(5S)-6-Oxo-5-[(2-phenylacetyl)amino]-6-[4-(6-phenylpyridin-2-yl)piperazin-1-yl]hexyl]prop-2-enamideIC50200.0 [1]
N-[(5S)-6-Oxo-5-[(2-phenylacetyl)amino]-6-[4-(6-phenylpyridin-2-yl)piperazin-1-yl]hexyl]prop-2-enamideKi7760.0 [1]
N-[(5S)-6-[4-(6-Chloropyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamideIC50180.0 [1]
N-[(5S)-6-[4-(6-Chloropyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamideKi4430.0 [1]
N-[(5S)-6-[4-(6-Bromopyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamideIC50220.0 [1]
N-[(5S)-6-[4-(6-Bromopyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamideKi5650.0 [1]
N-[(5S)-6-Oxo-5-[(2-phenylacetyl)amino]-6-(4-pyridin-2-ylpiperazin-1-yl)hexyl]prop-2-enamideIC50340.0 [1]
N-[(5S)-6-Oxo-5-[(2-phenylacetyl)amino]-6-(4-pyridin-2-ylpiperazin-1-yl)hexyl]prop-2-enamideKi8420.0 [1]
N-[(5S)-6-[4-(6-Nitropyridin-3-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamideIC5090.0 [1]
N-[(5S)-6-[4-(6-Nitropyridin-3-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamideKi2450.0 [1]
N-[4-(Pyrrolidine-1-sulfonyl)phenyl]prop-2-enamideIC501900.0 [1], 20300.0 [2]
2-[3-(3-Fluorophenyl)-5-(3-methoxyphenyl)-4-oxothieno[2,3-d]pyrimidin-2-yl]sulfanylacetohydrazideIC50140.0 [1], 210.0 [2]
2-[3-(2-Fluorophenyl)-4-oxo-5-phenylthieno[2,3-d]pyrimidin-2-yl]sulfanylacetohydrazideIC50160.0 [1], 500.0 [2]
2-[3-(3-Fluorophenyl)-4-oxo-5-phenylthieno[2,3-d]pyrimidin-2-yl]sulfanylacetohydrazideIC50180.0 [1], 250.0 [2]
2-[3-(4-Fluorophenyl)-4-oxo-5-phenylthieno[2,3-d]pyrimidin-2-yl]sulfanylacetohydrazideIC50320.0 [1], 1300.0 [2]
2-[3-(3-Methoxyphenyl)-4-oxo-5-phenylthieno[2,3-d]pyrimidin-2-yl]sulfanylacetohydrazideIC50470.0 [1], 820.0 [2]
2-[5-(4-Fluorophenyl)-4-oxo-3-phenylthieno[2,3-d]pyrimidin-2-yl]sulfanylacetohydrazideIC50290.0 [1], 800.0 [2]
N-[4-[4-(Adamantane-1-carbonyl)piperazin-1-yl]sulfonylphenyl]prop-2-enamideIC5010.0 [1], 770.0 [2]
(2,3-Difluorophenyl)methyl 4-[4-(prop-2-enoylamino)phenyl]sulfonylpiperazine-1-carboxylateIC5046.0 [1], 1600.0 [2]
N-[4-[4-(Piperidine-1-carbonyl)piperazin-1-yl]sulfonylphenyl]prop-2-enamideIC5037.0 [1], 360.0 [2]
N-[4-[4-(Cyclopentanecarbonyl)piperazin-1-yl]sulfonylphenyl]prop-2-enamideIC5032.0 [1], 1200.0 [2]
N-[4-[4-(4,4-Difluoropiperidine-1-carbonyl)piperazin-1-yl]sulfonylphenyl]prop-2-enamideIC5041.0 [1], 810.0 [2]
Benzyl 4-[4-(prop-2-enoylamino)phenyl]sulfonyl-1,4-diazepane-1-carboxylateIC50460.0 [1], 3200.0 [2]
4-(4-Acryloylamino-benzenesulfonyl)-piperazine-1-carboxylic acid tert-butyl esterIC50120.0 [1], 620.0 [2]
[1-(4-Acryloylamino-benzenesulfonyl)-piperidin-4-yl]-carbamic acid benzyl esterIC50220.0 [1], 5000.0 [2]
(2E)-3-(3-Nitrophenyl)-1-(pyridin-3-yl)prop-2-en-1-oneIC5019600.0 [1]
(2E)-3-(3-Nitrophenyl)-1-(pyridin-3-yl)prop-2-en-1-oneKi4000.0 [1]
(E)-5-Chloro-3-(2-oxopropylidene)indolin-2-oneIC503700.0 [1]
(E)-5-Chloro-3-(2-oxopropylidene)indolin-2-oneKi900.0 [1]
(E)-4-Chloro-1-methyl-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-oneIC5011000.0 [1]
(E)-4-Chloro-1-methyl-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-oneKi4000.0 [1]
(E)-Methyl 4-((4-chloro-2-oxo-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-1-yl)methyl)benzoateIC50660.0 [1], 1200.0 [2]
(3E)-4-Chloro-3-[2-(4-methoxypyridin-3-yl)-2-oxoethylidene]-1H-indol-2-oneIC50950.0 [1], 1400.0 [2]
(E)-4-Chloro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)-1-phenethylindolin-2-oneIC501500.0 [1], 2900.0 [2]
(E)-4-Chloro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)-1-(3-phenylpropyl)indolin-2-oneIC501000.0 [1], 1300.0 [2]
(3E)-4-Chloro-N,N-dimethyl-2-oxo-3-(2-oxo-2-pyridin-3-ylethylidene)indole-1-carboxamideIC505500.0 [1], 9200.0 [2]
(E)-5-Methyl-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-oneIC504500.0 [1], 6300.0 [2]
(E)-6-Bromo-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-oneIC50360.0 [1], 1500.0 [2]
(E)-4-Chloro-3-(2-oxo-2-(pyridin-2-yl)ethylidene)indolin-2-oneIC50890.0 [1], 1100.0 [2]
(E)-4-Chloro-3-(2-oxo-2-(pyridin-4-yl)ethylidene)indolin-2-oneIC501000.0 [1], 1200.0 [2]
(E)-4-Chloro-1-isopropyl-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-oneIC501400.0 [1], 1500.0 [2]
(E)-5-Chloro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-oneIC501200.0 [1], 6000.0 [2]
(E)-7-Chloro-3-(2-oxopropylidene)indolin-2-oneIC503900.0 [1], 4700.0 [2]
(E)-3-(2-(4-Aminophenyl)-2-oxoethylidene)-4-chloroindolin-2-oneIC501100.0 [1], 3000.0 [2]
(E)-1-Benzyl-4-chloro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-oneKi410.0 [1], 1000.0 [2]
(E)-5-Bromo-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-oneKi680.0 [1], 3000.0 [2]
(E)-6-Fluoro-3-(2-oxopropylidene)indolin-2-oneIC5020000.0 [1]
(E)-6-Fluoro-3-(2-oxopropylidene)indolin-2-oneKi5400.0 [1]
(E)-3-(2-Oxopropylidene)-6-(trifluoromethoxy)indolin-2-oneIC502600.0 [1], 3600.0 [2]
(E)-4-Chloro-3-(2-oxo-2-phenylethylidene)indolin-2-oneIC5020000.0 [1]
(E)-4-Chloro-3-(2-oxo-2-phenylethylidene)indolin-2-oneKi3300.0 [1]
(E)-4-Bromo-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-oneKi250.0 [1], 400.0 [2]
(E)-6-Chloro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-oneIC5020000.0 [1]
(E)-6-Chloro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-oneKi5300.0 [1]
(E)-4-Chloro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-oneIC501700.0 [1]
(E)-4-Chloro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-oneKi1300.0 [1]
(E)-4-Chloro-3-(2-(3-chlorophenyl)-2-oxoethylidene)indolin-2-oneIC50700.0 [1], 2800.0 [2]
(E)-3-(2-(3-Aminophenyl)-2-oxoethylidene)-4-chloroindolin-2-oneIC501400.0 [1], 1800.0 [2]
(E)-4-Chloro-1-(cyclohexylmethyl)-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-oneIC502100.0 [1], 6700.0 [2]
Ethyl (3E)-4-chloro-2-oxo-3-(2-oxo-2-pyridin-3-ylethylidene)indole-1-carboxylateIC501800.0 [1], 2500.0 [2]
(E)-5-Nitro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-oneIC501700.0 [1], 7900.0 [2]
(E)-7-Bromo-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-oneIC502900.0 [1], 3200.0 [2]
(E)-3-(2-(5-Bromopyridin-3-yl)-2-oxoethylidene)-4-chloroindolin-2-oneIC50970.0 [1], 1400.0 [2]
(E)-4-Chloro-3-(2-(3-methoxyphenyl)-2-oxoethylidene)indolin-2-oneIC501000.0 [1], 1100.0 [2]
(E)-4-Chloro-1-isobutyl-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-oneIC501000.0 [1], 4100.0 [2]
Methyl 3-[[(3E)-4-chloro-2-oxo-3-(2-oxo-2-pyridin-3-ylethylidene)indol-1-yl]methyl]benzoateIC501100.0 [1], 5600.0 [2]
(E)-4-Chloro-3-(2-(4-methoxyphenyl)-2-oxoethylidene)indolin-2-oneIC501100.0 [1], 1300.0 [2]
(E)-7-Chloro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-oneIC501600.0 [1], 7300.0 [2]
4-[4-(Acryloyl-methyl-amino)-benzenesulfonyl]-piperazine-1-carboxylic acid tert-butyl esterIC504500.0 [1], 32000.0 [2]
N-[4-[4-(3-Methylpyridin-2-yl)piperazin-1-yl]sulfonylphenyl]prop-2-enamideIC5025.0 [1], 990.0 [2]
N-[4-[4-[5-(Trifluoromethyl)pyridin-2-yl]piperazin-1-yl]sulfonylphenyl]prop-2-enamideIC5076.0 [1], 1800.0 [2]
(3,5-Difluorophenyl)methyl 4-[4-(prop-2-enoylamino)phenyl]sulfonylpiperazine-1-carboxylateIC5070.0 [1], 3000.0 [2]



References

This online tool may be cited as follows

MLA

"Quest Database™ Protein-glutamine gamma-glutamyltransferase Inhibitors (IC50, Ki)." AAT Bioquest, Inc.21 Nov2024https://www.aatbio.com/data-sets/protein-glutamine-gamma-glutamyltransferase-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024November 21). Quest Database™ Protein-glutamine gamma-glutamyltransferase Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/protein-glutamine-gamma-glutamyltransferase-inhibitors-ic50-ki.
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