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N-lysine methyltransferase SETD8 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
(E)-3-[(1R,2R,4Ar,5R,7R,8R,8aS)-5,7-dihydroxy-3,4a,8-trimethyl-2-[(5S,7R,8S,9S)-5,7,9-trihydroxy-8,10-dimethylundec-2-en-2-yl]-2,5,6,7,8,8a-hexahydro-1H-naphthalen-1-yl]-2-methylprop-2-enoic acidIC506500.0 [1]
(E)-3-[(1R,2R,4Ar,5R,7R,8R,8aS)-5,7-dihydroxy-3,4a,8-trimethyl-2-[(5S,7R,8S,9S)-5,7,9-trihydroxy-8,10-dimethylundec-2-en-2-yl]-2,5,6,7,8,8a-hexahydro-1H-naphthalen-1-yl]-2-methylprop-2-enoic acidKi2000.0 [1]
6,7-Dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amineIC507300.0 [1], 9000.0 [2], 37700.0 [3]
(2S)-2-[[(2S)-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-Acetamido-6-aminohexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoylamino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoic acidIC50330.0 [1]
(2S)-2-[[(2S)-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-Acetamido-6-aminohexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoylamino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoic acidKi50.0 [1]
6-Chloro-7-{[2-(morpholin-4-yl)ethyl]amino}quinoline-5,8-dioneIC50210.0 [1]
CID 46901937IC5040000.0 [1]
CID 44251522IC5040000.0 [1]
CID 53315882IC5010000.0 [1]
4-Hydroxy-3,3-dimethyl-2H-benzo[g]indole-2,5(3H)-dioneIC50700.0 [1]
7-Methoxy-2-pyrrolidin-1-yl-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amineIC50250000.0 [1]
6-Methoxy-2-pyrrolidin-1-yl-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amineIC5052000.0 [1]
6-Ethoxy-7-methoxy-2-pyrrolidin-1-yl-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amineIC509500.0 [1]
7-Methoxy-6-propan-2-yloxy-2-pyrrolidin-1-yl-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amineIC5061000.0 [1]
6-Chloro-7-methoxy-2-pyrrolidin-1-yl-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amineIC5046000.0 [1]
7-Ethoxy-6-methoxy-2-pyrrolidin-1-yl-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amineIC5011000.0 [1]
N-[5-(Azepan-1-yl)pentyl]-6,7-dimethoxy-2-pyrrolidin-1-ylquinazolin-4-amineIC507900.0 [1]
6-Methoxy-7-propan-2-yloxy-2-pyrrolidin-1-yl-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amineIC5048000.0 [1]
2-Pyrrolidin-1-yl-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amineIC50250000.0 [1]
6-Methoxy-7-phenylmethoxy-2-pyrrolidin-1-yl-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amineIC50130000.0 [1]
6-Methoxy-7-(2-methoxyethoxy)-2-pyrrolidin-1-yl-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amineIC508000.0 [1]
6-Methoxy-7-(3-methoxypropoxy)-2-pyrrolidin-1-yl-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amineIC5040000.0 [1]
N-[2-[6-Methoxy-2-pyrrolidin-1-yl-4-(5-pyrrolidin-1-ylpentylamino)quinazolin-7-yl]oxyethyl]formamideIC508700.0 [1]
6,7-Dimethoxy-2-pyrrolidin-1-yl-N-(2-pyrrolidin-1-ylethyl)quinazolin-4-amineIC5067000.0 [1]
6,7-Dimethoxy-2-pyrrolidin-1-yl-N-(3-pyrrolidin-1-ylpropyl)quinazolin-4-amineIC5036000.0 [1]
6,7-Dimethoxy-2-pyrrolidin-1-yl-N-(4-pyrrolidin-1-ylbutyl)quinazolin-4-amineIC5043000.0 [1]
6,7-Dimethoxy-N-(5-piperidin-1-ylpentyl)-2-pyrrolidin-1-ylquinazolin-4-amineIC507900.0 [1]
N-(6,7-Dimethoxy-2-pyrrolidin-1-ylquinazolin-4-yl)-N',N'-dimethylpentane-1,5-diamineIC507900.0 [1]
N-(6,7-Dimethoxy-2-pyrrolidin-1-ylquinazolin-4-yl)-N',N'-diethylpentane-1,5-diamineIC5021000.0 [1]
Tert-butyl 4-[5-[(6,7-dimethoxy-2-pyrrolidin-1-ylquinazolin-4-yl)amino]pentyl]piperazine-1-carboxylateIC5035000.0 [1]
6,7-Dimethoxy-N-(5-piperazin-1-ylpentyl)-2-pyrrolidin-1-ylquinazolin-4-amineIC5032000.0 [1]
6,7-Dimethoxy-N-[5-(4-methylpiperazin-1-yl)pentyl]-2-pyrrolidin-1-ylquinazolin-4-amineIC5029000.0 [1]
N-[5-(4-Ethylpiperazin-1-yl)pentyl]-6,7-dimethoxy-2-pyrrolidin-1-ylquinazolin-4-amineIC5025000.0 [1]
6,7-Dimethoxy-N-[5-(4-propan-2-ylpiperazin-1-yl)pentyl]-2-pyrrolidin-1-ylquinazolin-4-amineIC5034000.0 [1]
5-[(6,7-Dimethoxy-2-pyrrolidin-1-ylquinazolin-4-yl)amino]-1-pyrrolidin-1-ylpentan-1-oneIC5058000.0 [1]
6,7-Dimethoxy-N-methyl-2-pyrrolidin-1-yl-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amineIC50250000.0 [1]
6,7-Dimethoxy-2-piperidin-1-yl-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amineIC5094000.0 [1]
2-(Azepan-1-yl)-6,7-dimethoxy-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amineIC50250000.0 [1]
6,7-Dimethoxy-2-N,2-N-dimethyl-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamineIC509200.0 [1]
6,7-Dimethoxy-2-piperazin-1-yl-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amineIC50250000.0 [1]
6,7-Dimethoxy-2-(4-methylpiperazin-1-yl)-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amineIC50250000.0 [1]
2-N-Cyclopentyl-6,7-dimethoxy-2-N-methyl-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamineIC5037000.0 [1]
2-N-Cyclohexyl-6,7-dimethoxy-2-N-methyl-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamineIC5037000.0 [1]
2-N-Cyclopentyl-6,7-dimethoxy-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamineIC50250000.0 [1]
2-N-Cyclohexyl-6,7-dimethoxy-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamineIC50250000.0 [1]
2-Chloro-6,7-dimethoxy-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amineIC50250000.0 [1]
3-[6-Methoxy-2-pyrrolidin-1-yl-4-(5-pyrrolidin-1-ylpentylamino)quinazolin-7-yl]oxypropan-1-olIC5024000.0 [1]
2-[(6,7-Dimethoxy-2-pyrrolidin-1-ylquinazolin-4-yl)amino]-N-[2-(4-methylpiperazin-1-yl)ethyl]acetamideIC50250000.0 [1]
N-(6,7-Dimethoxy-2-pyrrolidin-1-ylquinazolin-4-yl)-N',N'-dimethylhexane-1,6-diamineIC5026000.0 [1]
N'-(6,7-Dimethoxy-2-pyrrolidin-1-ylquinazolin-4-yl)hexane-1,6-diamineIC5040000.0 [1]
6,7-Dimethoxy-N-(3-piperidin-4-ylpropyl)-2-pyrrolidin-1-ylquinazolin-4-amineIC5040000.0 [1]
N-[2-(4-Aminocyclohexyl)ethyl]-6,7-dimethoxy-2-pyrrolidin-1-ylquinazolin-4-amineIC5043000.0 [1]
4-N-(6,7-Dimethoxy-2-pyrrolidin-1-ylquinazolin-4-yl)cyclohexane-1,4-diamineIC50250000.0 [1]
N-[4-(Aminomethyl)cyclohexyl]-6,7-dimethoxy-2-pyrrolidin-1-ylquinazolin-4-amineIC50250000.0 [1]
N-[2-[(6,7-Dimethoxy-2-pyrrolidin-1-ylquinazolin-4-yl)amino]ethyl]-2-pyrrolidin-1-ylacetamideIC5063000.0 [1]
2-[(6,7-Dimethoxy-2-pyrrolidin-1-ylquinazolin-4-yl)amino]-N-(2-pyrrolidin-1-ylethyl)acetamideIC50250000.0 [1]
2-[(6,7-Dimethoxy-2-pyrrolidin-1-ylquinazolin-4-yl)amino]-N-(2-piperazin-1-ylethyl)acetamideIC50250000.0 [1]
2-(3,3-Difluoroazetidin-1-yl)-6,7-dimethoxy-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amineIC50110000.0 [1]
6,7-Dimethoxy-2-[(3S)-3-methylpyrrolidin-1-yl]-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amineIC5015000.0 [1]
6,7-Dimethoxy-2-N-methyl-2-N-(2-pyrrolidin-1-ylethyl)-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamineIC50250000.0 [1]
6,7-Dimethoxy-2-N-methyl-4-N-(5-pyrrolidin-1-ylpentyl)-2-N-(3-pyrrolidin-1-ylpropyl)quinazoline-2,4-diamineIC50250000.0 [1]
6,7-Dimethoxy-2-N-methyl-2-N-(4-pyrrolidin-1-ylbutyl)-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamineIC50250000.0 [1]
6,7-Dimethoxy-2-N-methyl-2-N,4-N-bis(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamineIC50250000.0 [1]
6,7-Dimethoxy-2-N-methyl-2-N-phenyl-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamineIC50250000.0 [1]
6,7-Dimethoxy-2-N-(4-methoxyphenyl)-2-N-methyl-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamineIC50250000.0 [1]
6,7-Dimethoxy-2-N-methyl-2-N-(4-nitrophenyl)-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamineIC50250000.0 [1]
6,7-Dimethoxy-2-N-phenyl-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamineIC50250000.0 [1]
6,7-Dimethoxy-2-N-(4-methoxyphenyl)-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamineIC50250000.0 [1]
6,7-Dimethoxy-4-N-(5-pyrrolidin-1-ylpentyl)-2-N-[4-(trifluoromethyl)phenyl]quinazoline-2,4-diamineIC50250000.0 [1]
6,7-Dimethoxy-2-N-(4-nitrophenyl)-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamineIC50250000.0 [1]
6,7-Dimethoxy-2-phenyl-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amineIC50250000.0 [1]
6,7-Dimethoxy-2-(4-methoxyphenyl)-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amineIC50250000.0 [1]
6,7-Dimethoxy-N-(5-pyrrolidin-1-ylpentyl)-2-[4-(trifluoromethyl)phenyl]quinazolin-4-amineIC50250000.0 [1]
2-N-(4-Fluorophenyl)-6,7-dimethoxy-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamineIC50250000.0 [1]
6-Methoxy-2-pyrrolidin-1-yl-4-(5-pyrrolidin-1-ylpentylamino)quinazolin-7-olIC50250000.0 [1]
2-Methyl-5-(4-methylphenyl)imino-1,3-benzothiazole-4,7-dioneIC50500.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ N-lysine methyltransferase SETD8 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.8 May2024https://www.aatbio.com/data-sets/n-lysine-methyltransferase-setd8-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 8). Quest Database™ N-lysine methyltransferase SETD8 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/n-lysine-methyltransferase-setd8-inhibitors-ic50-ki.
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