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Histone-lysine N-methyltransferase, H3 lysine-79 specific Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
PinometostatIC507.0 [1]
PinometostatKi0.01 [1], 0.07 [2], 0.08 [3]
CID 56962336IC500.4 [1]
CID 56962336Ki0.3 [1], 300.0 [2]
(2S)-2-Amino-4-[[(2S,3S,4R,5R)-3,4-dihydroxy-5-[6-(methylamino)purin-9-yl]oxolan-2-yl]methylsulfanyl]butanoic acidKi290.0 [1], 300.0 [2], 1100.0 [3]
5'-[(3-{[(4-Tert-Butylphenyl)carbamoyl]amino}propyl)(Propan-2-Yl)amino]-5'-DeoxyadenosineIC5014.0 [1], 100.0 [2]
5'-[(3-{[(4-Tert-Butylphenyl)carbamoyl]amino}propyl)(Propan-2-Yl)amino]-5'-DeoxyadenosineKi0.46 [1], 0.5 [2], 0.72 [3]
S-Adenosyl-L-homocysteineIC50600.0 [1]
S-Adenosyl-L-homocysteineKi160.0 [1]
Dot1L-IN-1IC500.1 [1], 3.0 [2], 17.0 [3]
Dot1L-IN-1Ki0.0 [1]
1-{[6-(3-Fluorophenyl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-3-yl]methyl}-1H-1,2,3-benzotriazoleIC508290.0 [1], 21910.0 [2], 28080.0 [3], 55780.0 [4]
5-IodotubercidinIC5018000.0 [1], 18200.0 [2]
S-Adenosyl-3-thiopropylamineKi100000.0 [1]
CID 56962337IC500.3 [1], 8.8 [2]
Bromo-deaza-SAHIC5077.0 [1]
CID 2231443IC508400.0 [1], 40730.0 [2]
3-(Benzotriazol-1-ylmethyl)-6-benzyl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoleIC5019390.0 [1], 48800.0 [2]
1-{[6-(3,4-Dimethylphenyl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-3-yl]methyl}-1H-benzimidazoleIC5017370.0 [1], 63970.0 [2]
(2S)-2-Amino-5-[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl-(2-iodoethyl)amino]pentanoic acidIC5038.0 [1]
(2S)-2-Amino-5-[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[6-(methylamino)purin-9-yl]oxolan-2-yl]methyl-(2-iodoethyl)amino]pentanoic acidIC50120.0 [1]
1-(4-Tert-butylphenyl)-3-[3-[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[6-(methylamino)purin-9-yl]oxolan-2-yl]methyl-propan-2-ylamino]propyl]ureaKi0.76 [1], 0.8 [2]
Benzyl N-[3-[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylamino]propyl]carbamateKi46000.0 [1]
Benzyl N-[3-[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl-propan-2-ylamino]propyl]carbamateKi22000.0 [1]
5-[[(2S,3S,4R,5R)-5-(6-Aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]-N-phenylpentanamideKi22000.0 [1]
3-[[(2S,3S,4R,5R)-5-(6-Aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]propyl N-phenylcarbamateKi16000.0 [1]
1-[3-[[(2S,3S,4R,5R)-5-(6-Aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]propyl]-3-benzylureaKi1900.0 [1]
1-[3-[[(2S,3S,4R,5R)-5-(6-Aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]propyl]-3-phenylureaKi550.0 [1]
1-[2-[[(2S,3S,4R,5R)-5-(6-Aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]ethyl]-3-phenylureaKi18000.0 [1]
1-[4-[[(2S,3S,4R,5R)-5-(6-Aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]butyl]-3-phenylureaKi1100.0 [1]
1-[3-[[(2S,3S,4R,5R)-5-(6-Aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]propyl]-3-(4-chlorophenyl)ureaKi82.0 [1]
1-[3-[[(2S,3S,4R,5R)-5-(6-Aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]propyl]-3-[4-(trifluoromethyl)phenyl]ureaKi58.0 [1]
1-[3-[[(3R,4S,5R)-3-(6-Aminopurin-9-yl)-4,5-dihydroxycyclopenten-1-yl]methyl-propan-2-ylamino]propyl]-3-(4-tert-butylphenyl)ureaKi1.3 [1]
1-[3-[[(1R,2R,3S,4R)-4-(6-Aminopurin-9-yl)-2,3-dihydroxycyclopentyl]methyl-propan-2-ylamino]propyl]-3-(4-tert-butylphenyl)ureaKi1.1 [1]
1-[3-[[(1S,2R,3S,4R)-4-(6-Aminopurin-9-yl)-2,3-dihydroxycyclopentyl]methyl-propan-2-ylamino]propyl]-3-(4-tert-butylphenyl)ureaKi50000.0 [1]
1-{[6-(3-Bromophenyl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-3-yl]methyl}-1H-benzimidazoleIC504090.0 [1], 26780.0 [2]
1-{[6-(3-Methoxyphenyl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-3-yl]methyl}-1H-benzotriazoleIC506470.0 [1], 64150.0 [2]
1-{[6-(4-Fluorophenyl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-3-yl]methyl}-1H-1,2,3-benzotriazoleIC504640.0 [1], 8000.0 [2]
6-(1,3-Benzodioxol-5-yl)-3-(benzotriazol-1-ylmethyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoleIC503960.0 [1], 6750.0 [2]
1-{[6-(4-Tert-butylphenyl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-3-yl]methyl}-1H-benzotriazoleIC504480.0 [1], 13050.0 [2]
4-{6-[(E)-2-(Furan-2-yl)ethenyl][1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-3-yl}-N,N-dimethylanilineIC5020940.0 [1]
(2R,3R,4S,5R)-2-(6-Aminopurin-9-yl)-5-[[propan-2-yl-[3-[2-[6-(trifluoromethoxy)-1H-benzimidazol-2-yl]ethyl]cyclobutyl]amino]methyl]oxolane-3,4-diolIC502.18 [1], 2.92 [2]
AdenosineIC50100000.0 [1]
SinefunginIC5033710.0 [1]
CID 71268957IC50100000.0 [1]
6,7-Dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amineIC50100000.0 [1]
3-[[(2S,3S,4R,5R)-5-(6-Aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]propanoic acidKi100000.0 [1]
(2R,3R,4S,5S)-2-(6-Aminopurin-9-yl)-5-(2-hydroxyethylsulfanylmethyl)oxolane-3,4-diolKi100000.0 [1]
5'-Deoxy-5'-[2-(amino)ethylthio]adenosineKi25000.0 [1]
(2S)-2-Amino-4-[[(2S,3S,4R,5R)-5-[6-(benzylamino)purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]butanoic acidKi1100.0 [1]
2-Amino-N-[4-(2-amino-3-cyano-1-ethylindol-5-yl)oxyphenyl]acetamideIC5099000.0 [1]
2-Amino-N-[4-(2-amino-3-cyano-1-methylindol-5-yl)oxyphenyl]acetamideIC50100000.0 [1]
(2R)-2-Amino-N-[4-[(2-amino-3-cyano-1H-indol-5-yl)oxy]phenyl]-3-hydroxypropanamideIC50100000.0 [1]
2-Amino-4-[[(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]butanoic acidIC50170.0 [1]
5'-Deoxy-5'-(Dimethylamino)adenosineKi38000.0 [1]
5'-S-Benzyl-5'-thioadenosineKi100000.0 [1]
(2s)-2-Amino-N-[4-[(2-Amino-3-Cyano-1h-Indol-5-Yl)oxy]phenyl]-3-Hydroxy-PropanamideIC50100000.0 [1]
(2S)-2-Amino-4-[[(2S,3S,4R,5R)-3,4-dihydroxy-5-[6-(propan-2-ylamino)purin-9-yl]oxolan-2-yl]methylsulfanyl]butanoic acidKi3800.0 [1]
PRMT5 Inhibitor C17IC50100000.0 [1]
(2S)-2-Amino-4-[[(2S,3S,4R,5R)-5-[6-(cyclopropylamino)purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]butanoic acidKi2000.0 [1]
(2S)-2-Amino-4-[[(2S,3S,4R,5R)-5-[6-(butylamino)purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]butanoic acidKi2800.0 [1]
(2S)-2-Amino-4-[[(2S,3S,4R,5R)-5-[6-(tert-butylamino)purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]butanoic acidKi7800.0 [1]
(2S)-2-Amino-4-[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl-(2-iodoethyl)amino]butanoic acidIC5016000.0 [1]
(2S)-2-Amino-5-[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl-[2-(3-carbamoylphenyl)ethyl]amino]pentanoic acidIC501300.0 [1]
2-[[1-(2-Chlorophenyl)indol-6-yl]carbamoylamino]-N-[3-[[(3R)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-3-yl]amino]propyl]acetamideIC503.98 [1]
2-[[1-(2-Chlorophenyl)indol-6-yl]carbamoylamino]-N-[4-[[(3R)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-3-yl]amino]butyl]acetamideIC503.98 [1]
2-[[1-(2-Chlorophenyl)indol-6-yl]carbamoylamino]-N-[3-[methyl-[(3R)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-3-yl]amino]propyl]acetamideIC500.15 [1]
(2R,3R,4S,5R)-2-(6-Aminopurin-9-yl)-5-[(1S)-1-[[3-[2-(6-tert-butyl-1H-benzimidazol-2-yl)ethyl]cyclobutyl]-cyclobutylamino]ethyl]oxolane-3,4-diolIC501430.0 [1]
1-[3-[[(1S)-1-[(2R,3S,4R,5R)-5-(6-Aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]ethyl]-propan-2-ylamino]propyl]-3-(4-tert-butylphenyl)ureaIC506.34 [1]
(2R,3R,4S,5R)-2-(6-Aminopurin-9-yl)-5-[(1S)-1-[[3-[2-(6-tert-butyl-1H-benzimidazol-2-yl)ethyl]cyclobutyl]amino]ethyl]oxolane-3,4-diolIC50690.0 [1]
2-[[1-(2-Chlorophenyl)indol-6-yl]carbamoylamino]acetamideIC507943.28 [1]
(3R)-N-Methyl-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-3-amineIC50141000.0 [1]
(2R,3R,4S,5R)-2-(6-Aminopurin-9-yl)-5-[(1S)-1-[bis[3-[2-(6-tert-butyl-1H-benzimidazol-2-yl)ethyl]cyclobutyl]amino]ethyl]oxolane-3,4-diolIC502160.0 [1]
2-Amino-N-[4-[2-amino-3-cyano-1-(cyclopropylmethyl)indol-5-yl]oxyphenyl]acetamideIC5096000.0 [1]
5-Benzyloxy-2-amino-1H-indole-3-carbonitrileIC50100000.0 [1]
5-Benzyloxy-2-amino-1-methyl-1H-indole-3-carbonitrileIC50100000.0 [1]
5-(3-Aminobenzyloxy)-2-amino-1-methyl-1H-indole-3-carbonitrileIC50100000.0 [1]
6-[(E)-2-(Furan-2-yl)ethenyl]-3-phenyl[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoleIC507010.0 [1]
6-[(E)-2-(Furan-2-yl)ethenyl]-3-(pyridin-4-yl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoleIC5013660.0 [1]
N-[(6-Methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1-propan-2-ylindazole-4-carboxamideIC50100000.0 [1]
(2S)-2-Amino-5-[[(2R,3S,4R,5R)-5-[6-(benzylamino)purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methyl-(2-iodoethyl)amino]pentanoic acidIC50110.0 [1]
5'-Deoxy-5'-(Prop-2-Yn-1-Ylamino)adenosineKi100000.0 [1]
5'-[(3-{[(4-Tert-Butylphenyl)carbamoyl]amino}propyl)(Methyl)amino]-5'-DeoxyadenosineKi13.0 [1]
5'-S-(3-Aminophenyl)-5'-thioadenosineKi100000.0 [1]
6-[2-(2-Furyl)vinyl]-3-(3-methylphenyl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoleIC509410.0 [1]
(3R)-1-(7H-Pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-3-amineIC50251188.64 [1]
N-[(4,6-Dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1-propan-2-ylindazole-4-carboxamideIC50100000.0 [1]
1-[3-[[(2S,3S,4R,5R)-5-(6-Aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]propyl]-3-(4-tert-butylphenyl)ureaKi70.0 [1]
1-[3-[[(2S,3S,4R,5R)-5-(6-Aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]propyl]-3-(2-ethylphenyl)ureaKi690.0 [1]
1-[3-[[(2S,3S,4R,5R)-5-(6-Aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]propyl]-3-(3-ethylphenyl)ureaKi130.0 [1]
1-[3-[[(2S,3S,4R,5R)-5-(6-Aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]propyl]-3-(2,4-difluorophenyl)ureaKi1000.0 [1]
1-[3-[[(2S,3S,4R,5R)-5-(6-Aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]propyl]-3-[3,5-bis(trifluoromethyl)phenyl]ureaKi80.0 [1]
1-[3-[[(2S,3S,4R,5R)-5-(6-Aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]propyl]-3-naphthalen-1-ylureaKi2700.0 [1]
1-(4-Tert-butylphenyl)-3-[3-[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[6-(prop-2-enylamino)purin-9-yl]oxolan-2-yl]methyl-propan-2-ylamino]propyl]ureaKi12.0 [1]
1-[3-[[(2R,3S,4R,5R)-5-[6-(Benzylamino)purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methyl-propan-2-ylamino]propyl]-3-(4-tert-butylphenyl)ureaKi22.0 [1]
(2R,3R,4S,5R)-2-(6-Aminopurin-9-yl)-5-[(pyridin-2-ylmethylamino)methyl]oxolane-3,4-diolKi100000.0 [1]
(2R,3R,4S,5R)-2-(6-Aminopurin-9-yl)-5-[(pyridin-4-ylmethylamino)methyl]oxolane-3,4-diolKi100000.0 [1]
(2R,3R,4S,5R)-2-(6-Aminopurin-9-yl)-5-[(thiophen-2-ylmethylamino)methyl]oxolane-3,4-diolKi100000.0 [1]
(2R,3R,4S,5R)-2-(6-Aminopurin-9-yl)-5-[(furan-2-ylmethylamino)methyl]oxolane-3,4-diolKi100000.0 [1]
(2R,3S,4R,5R)-2-[[(3-Aminophenyl)methyl-prop-2-enylamino]methyl]-5-(6-aminopurin-9-yl)oxolane-3,4-diolKi100000.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Histone-lysine N-methyltransferase, H3 lysine-79 specific Inhibitors (IC50, Ki)." AAT Bioquest, Inc.21 Nov2024https://www.aatbio.com/data-sets/histone-lysine-n-methyltransferase-h3-lysine-79-specific-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024November 21). Quest Database™ Histone-lysine N-methyltransferase, H3 lysine-79 specific Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/histone-lysine-n-methyltransferase-h3-lysine-79-specific-inhibitors-ic50-ki.
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