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-enamide	IC50	14.0 [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-enamide	Ki	5730.0 [1]
	(E)-3-(2-Oxo-2-(pyridin-3-yl)ethylidene)indolin-2-one	IC50	8500.0 [1]
	(E)-3-(2-Oxo-2-(pyridin-3-yl)ethylidene)indolin-2-one	Ki	12000.0 [1], 86000.0 [2]
	(E)-4-Chloro-3-(2-(4-chlorophenyl)-2-oxoethylidene)indolin-2-one	IC50	90.0 [1], 800.0 [2]
	(E)-4-Chloro-3-(2-(4-chlorophenyl)-2-oxoethylidene)indolin-2-one	Ki	47000.0 [1]
	(E)-4-Chloro-3-(2-(2-methoxyphenyl)-2-oxoethylidene)indolin-2-one	IC50	740.0 [1], 900.0 [2]
	(E)-4-Chloro-3-(2-(2-methoxyphenyl)-2-oxoethylidene)indolin-2-one	Ki	3300.0 [1]
	(E)-4-Chloro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)-1-phenylindolin-2-one	IC50	570.0 [1], 800.0 [2]
	(E)-4-Chloro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)-1-phenylindolin-2-one	Ki	9100.0 [1]
	N-[(5S)-6-[4-(6-Fluoropyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamide	IC50	110.0 [1], 1100.0 [2]
	N-[(5S)-6-[4-(6-Fluoropyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamide	Ki	6280.0 [1]
	N-[(5S)-6-[4-(6-Nitropyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamide	IC50	100.0 [1], 400.0 [2]
	N-[(5S)-6-[4-(6-Nitropyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamide	Ki	2260.0 [1]
	3-(2-Oxo-propylidene)-1,3-dihydro-indol-2-one	IC50	19000.0 [1]
	3-(2-Oxo-propylidene)-1,3-dihydro-indol-2-one	Ki	10000.0 [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-enoate	IC50	30.0 [1]
	2-[[3-(3-Fluorophenyl)-4-oxo-5-phenyl-5,6,7,8-tetrahydro-[1]benzothiolo[2,3-d]pyrimidin-2-yl]sulfanyl]acetohydrazide	IC50	170.0 [1], 930.0 [2]
	Benzyl N-[4-(4-prop-2-enoylpiperazin-1-yl)sulfonylphenyl]carbamate	IC50	2900.0 [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-enoate	IC50	20.0 [1]
	2-(4-Oxo-5-phenyl-3-pyridin-3-ylthieno[2,3-d]pyrimidin-2-yl)sulfanylacetohydrazide	IC50	480.0 [1], 1200.0 [2]
	2-(4-Oxo-3,5-diphenylthieno[2,3-d]pyrimidin-2-yl)sulfanylacetohydrazide	IC50	250.0 [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-enamide	IC50	390.0 [1]
	N-[(5S)-6-[4-[6-(2-Fluoroethoxy)pyridin-2-yl]piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamide	Ki	7320.0 [1]
	N-[(5S)-6-[4-(6-Tert-butylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamide	IC50	170.0 [1]
	N-[(5S)-6-[4-(6-Tert-butylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamide	Ki	3500.0 [1]
	N-[(5S)-6-[4-(6-Iodopyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamide	IC50	140.0 [1]
	N-[(5S)-6-[4-(6-Iodopyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamide	Ki	2920.0 [1]
	N-[(5S)-6-Oxo-5-[(2-phenylacetyl)amino]-6-[4-(6-phenylpyridin-2-yl)piperazin-1-yl]hexyl]prop-2-enamide	IC50	200.0 [1]
	N-[(5S)-6-Oxo-5-[(2-phenylacetyl)amino]-6-[4-(6-phenylpyridin-2-yl)piperazin-1-yl]hexyl]prop-2-enamide	Ki	7760.0 [1]
	N-[(5S)-6-[4-(6-Chloropyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamide	IC50	180.0 [1]
	N-[(5S)-6-[4-(6-Chloropyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamide	Ki	4430.0 [1]
	N-[(5S)-6-[4-(6-Bromopyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamide	IC50	220.0 [1]
	N-[(5S)-6-[4-(6-Bromopyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamide	Ki	5650.0 [1]
	N-[(5S)-6-Oxo-5-[(2-phenylacetyl)amino]-6-(4-pyridin-2-ylpiperazin-1-yl)hexyl]prop-2-enamide	IC50	340.0 [1]
	N-[(5S)-6-Oxo-5-[(2-phenylacetyl)amino]-6-(4-pyridin-2-ylpiperazin-1-yl)hexyl]prop-2-enamide	Ki	8420.0 [1]
	N-[(5S)-6-[4-(6-Nitropyridin-3-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamide	IC50	90.0 [1]
	N-[(5S)-6-[4-(6-Nitropyridin-3-yl)piperazin-1-yl]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]prop-2-enamide	Ki	2450.0 [1]
	N-[4-(Pyrrolidine-1-sulfonyl)phenyl]prop-2-enamide	IC50	1900.0 [1], 20300.0 [2]
	2-[3-(3-Fluorophenyl)-5-(3-methoxyphenyl)-4-oxothieno[2,3-d]pyrimidin-2-yl]sulfanylacetohydrazide	IC50	140.0 [1], 210.0 [2]
	2-[3-(2-Fluorophenyl)-4-oxo-5-phenylthieno[2,3-d]pyrimidin-2-yl]sulfanylacetohydrazide	IC50	160.0 [1], 500.0 [2]
	2-[3-(3-Fluorophenyl)-4-oxo-5-phenylthieno[2,3-d]pyrimidin-2-yl]sulfanylacetohydrazide	IC50	180.0 [1], 250.0 [2]
	2-[3-(4-Fluorophenyl)-4-oxo-5-phenylthieno[2,3-d]pyrimidin-2-yl]sulfanylacetohydrazide	IC50	320.0 [1], 1300.0 [2]
	2-[3-(3-Methoxyphenyl)-4-oxo-5-phenylthieno[2,3-d]pyrimidin-2-yl]sulfanylacetohydrazide	IC50	470.0 [1], 820.0 [2]
	2-[5-(4-Fluorophenyl)-4-oxo-3-phenylthieno[2,3-d]pyrimidin-2-yl]sulfanylacetohydrazide	IC50	290.0 [1], 800.0 [2]
	N-[4-[4-(Adamantane-1-carbonyl)piperazin-1-yl]sulfonylphenyl]prop-2-enamide	IC50	10.0 [1], 770.0 [2]
	(2,3-Difluorophenyl)methyl 4-[4-(prop-2-enoylamino)phenyl]sulfonylpiperazine-1-carboxylate	IC50	46.0 [1], 1600.0 [2]
	N-[4-[4-(Piperidine-1-carbonyl)piperazin-1-yl]sulfonylphenyl]prop-2-enamide	IC50	37.0 [1], 360.0 [2]
	N-[4-[4-(Cyclopentanecarbonyl)piperazin-1-yl]sulfonylphenyl]prop-2-enamide	IC50	32.0 [1], 1200.0 [2]
	N-[4-[4-(4,4-Difluoropiperidine-1-carbonyl)piperazin-1-yl]sulfonylphenyl]prop-2-enamide	IC50	41.0 [1], 810.0 [2]
	Benzyl 4-[4-(prop-2-enoylamino)phenyl]sulfonyl-1,4-diazepane-1-carboxylate	IC50	460.0 [1], 3200.0 [2]
	4-(4-Acryloylamino-benzenesulfonyl)-piperazine-1-carboxylic acid tert-butyl ester	IC50	120.0 [1], 620.0 [2]
	[1-(4-Acryloylamino-benzenesulfonyl)-piperidin-4-yl]-carbamic acid benzyl ester	IC50	220.0 [1], 5000.0 [2]
	(2E)-3-(3-Nitrophenyl)-1-(pyridin-3-yl)prop-2-en-1-one	IC50	19600.0 [1]
	(2E)-3-(3-Nitrophenyl)-1-(pyridin-3-yl)prop-2-en-1-one	Ki	4000.0 [1]
	(E)-5-Chloro-3-(2-oxopropylidene)indolin-2-one	IC50	3700.0 [1]
	(E)-5-Chloro-3-(2-oxopropylidene)indolin-2-one	Ki	900.0 [1]
	(E)-4-Chloro-1-methyl-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-one	IC50	11000.0 [1]
	(E)-4-Chloro-1-methyl-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-one	Ki	4000.0 [1]
	(E)-Methyl 4-((4-chloro-2-oxo-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-1-yl)methyl)benzoate	IC50	660.0 [1], 1200.0 [2]
	(3E)-4-Chloro-3-[2-(4-methoxypyridin-3-yl)-2-oxoethylidene]-1H-indol-2-one	IC50	950.0 [1], 1400.0 [2]
	(E)-4-Chloro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)-1-phenethylindolin-2-one	IC50	1500.0 [1], 2900.0 [2]
	(E)-4-Chloro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)-1-(3-phenylpropyl)indolin-2-one	IC50	1000.0 [1], 1300.0 [2]
	(3E)-4-Chloro-N,N-dimethyl-2-oxo-3-(2-oxo-2-pyridin-3-ylethylidene)indole-1-carboxamide	IC50	5500.0 [1], 9200.0 [2]
	(E)-5-Methyl-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-one	IC50	4500.0 [1], 6300.0 [2]
	(E)-6-Bromo-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-one	IC50	360.0 [1], 1500.0 [2]
	(E)-4-Chloro-3-(2-oxo-2-(pyridin-2-yl)ethylidene)indolin-2-one	IC50	890.0 [1], 1100.0 [2]
	(E)-4-Chloro-3-(2-oxo-2-(pyridin-4-yl)ethylidene)indolin-2-one	IC50	1000.0 [1], 1200.0 [2]
	(E)-4-Chloro-1-isopropyl-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-one	IC50	1400.0 [1], 1500.0 [2]
	(E)-5-Chloro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-one	IC50	1200.0 [1], 6000.0 [2]
	(E)-7-Chloro-3-(2-oxopropylidene)indolin-2-one	IC50	3900.0 [1], 4700.0 [2]
	(E)-3-(2-(4-Aminophenyl)-2-oxoethylidene)-4-chloroindolin-2-one	IC50	1100.0 [1], 3000.0 [2]
	(E)-1-Benzyl-4-chloro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-one	Ki	410.0 [1], 1000.0 [2]
	(E)-5-Bromo-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-one	Ki	680.0 [1], 3000.0 [2]
	(E)-6-Fluoro-3-(2-oxopropylidene)indolin-2-one	IC50	20000.0 [1]
	(E)-6-Fluoro-3-(2-oxopropylidene)indolin-2-one	Ki	5400.0 [1]
	(E)-3-(2-Oxopropylidene)-6-(trifluoromethoxy)indolin-2-one	IC50	2600.0 [1], 3600.0 [2]
	(E)-4-Chloro-3-(2-oxo-2-phenylethylidene)indolin-2-one	IC50	20000.0 [1]
	(E)-4-Chloro-3-(2-oxo-2-phenylethylidene)indolin-2-one	Ki	3300.0 [1]
	(E)-4-Bromo-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-one	Ki	250.0 [1], 400.0 [2]
	(E)-6-Chloro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-one	IC50	20000.0 [1]
	(E)-6-Chloro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-one	Ki	5300.0 [1]
	(E)-4-Chloro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-one	IC50	1700.0 [1]
	(E)-4-Chloro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-one	Ki	1300.0 [1]
	(E)-4-Chloro-3-(2-(3-chlorophenyl)-2-oxoethylidene)indolin-2-one	IC50	700.0 [1], 2800.0 [2]
	(E)-3-(2-(3-Aminophenyl)-2-oxoethylidene)-4-chloroindolin-2-one	IC50	1400.0 [1], 1800.0 [2]
	(E)-4-Chloro-1-(cyclohexylmethyl)-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-one	IC50	2100.0 [1], 6700.0 [2]
	Ethyl (3E)-4-chloro-2-oxo-3-(2-oxo-2-pyridin-3-ylethylidene)indole-1-carboxylate	IC50	1800.0 [1], 2500.0 [2]
	(E)-5-Nitro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-one	IC50	1700.0 [1], 7900.0 [2]
	(E)-7-Bromo-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-one	IC50	2900.0 [1], 3200.0 [2]
	(E)-3-(2-(5-Bromopyridin-3-yl)-2-oxoethylidene)-4-chloroindolin-2-one	IC50	970.0 [1], 1400.0 [2]
	(E)-4-Chloro-3-(2-(3-methoxyphenyl)-2-oxoethylidene)indolin-2-one	IC50	1000.0 [1], 1100.0 [2]
	(E)-4-Chloro-1-isobutyl-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-one	IC50	1000.0 [1], 4100.0 [2]
	Methyl 3-[[(3E)-4-chloro-2-oxo-3-(2-oxo-2-pyridin-3-ylethylidene)indol-1-yl]methyl]benzoate	IC50	1100.0 [1], 5600.0 [2]
	(E)-4-Chloro-3-(2-(4-methoxyphenyl)-2-oxoethylidene)indolin-2-one	IC50	1100.0 [1], 1300.0 [2]
	(E)-7-Chloro-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-2-one	IC50	1600.0 [1], 7300.0 [2]
	4-[4-(Acryloyl-methyl-amino)-benzenesulfonyl]-piperazine-1-carboxylic acid tert-butyl ester	IC50	4500.0 [1], 32000.0 [2]
	N-[4-[4-(3-Methylpyridin-2-yl)piperazin-1-yl]sulfonylphenyl]prop-2-enamide	IC50	25.0 [1], 990.0 [2]
	N-[4-[4-[5-(Trifluoromethyl)pyridin-2-yl]piperazin-1-yl]sulfonylphenyl]prop-2-enamide	IC50	76.0 [1], 1800.0 [2]
	(3,5-Difluorophenyl)methyl 4-[4-(prop-2-enoylamino)phenyl]sulfonylpiperazine-1-carboxylate	IC50	70.0 [1], 3000.0 [2]

Entire TableStructureCompound NameStandard TypeStandard Values (in nM)

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

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References

This online tool may be cited as follows

MLA	"Quest Database™ Protein-glutamine gamma-glutamyltransferase Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 9 May. 2024, https://www.aatbio.com/data-sets/protein-glutamine-gamma-glutamyltransferase-inhibitors-ic50-ki.
APA	AAT Bioquest, Inc. (2024, May 9). 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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