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Menin/Histone-lysine N-methyltransferase MLL 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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4-(2-Benzyl-2,7-diazaspiro[3.4]octan-7-yl)-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidineIC5056.0 [1], 144.0 [2]
4-[2-(2-Methyl-4,5,6,7-tetrahydroindazol-4-yl)-2,7-diazaspiro[3.4]octan-7-yl]-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidineIC50120.0 [1], 385.0 [2]
4-(2-Benzyl-2,7-diazaspiro[4.5]decan-7-yl)-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidineIC50140.0 [1], 227.0 [2]
[(6S)-5-Azaspiro[2.4]heptan-6-yl]-[7-[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]-2,7-diazaspiro[3.4]octan-2-yl]methanoneIC5092.0 [1], 102.0 [2]
4-[2-[(1R)-1-(Azetidin-3-yl)-2-methylpropyl]-2,7-diazaspiro[3.4]octan-7-yl]-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidineIC508.0 [1], 21.0 [2]
4-[2-[(1S)-1-(Azetidin-3-yl)-2-methylpropyl]-2,7-diazaspiro[3.4]octan-7-yl]-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidineIC50110.0 [1], 190.0 [2]
4-(4-(5,5-Dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-propylthieno[2,3-d]pyrimidineIC50450.0 [1]
CID 91667931IC5014.0 [1]
6-Hydroxy-1-(1H-pyrazol-4-ylmethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5021.0 [1]
CID 72201086IC5046.0 [1]
CID 90455046IC5015.0 [1]
4-(3-(4-(Hydroxy(phenyl)cyclopentylmethyl)piperidine-1-yl)propyloxy)benzonitrileIC50390.0 [1]
4-[3-[4-(Cyclopentyl-hydroxy-pyridin-2-ylmethyl)piperidin-1-yl]propoxy]benzenesulfonamideIC50114.0 [1]
4-[3-[4-[Cyclopentyl-(3,5-difluorophenyl)-hydroxymethyl]piperidin-1-yl]propoxy]benzonitrileIC50437.0 [1]
4-[3-[4-(Cyclopentyl-hydroxy-pyridin-2-ylmethyl)piperidin-1-yl]propoxy]benzonitrileIC50302.0 [1]
4-[3-[4-[Cyclopentyl-(3-fluorophenyl)-hydroxymethyl]piperidin-1-yl]propoxy]benzonitrileIC50197.0 [1]
4-[3-[4-[(3-Chlorophenyl)-cyclopentyl-hydroxymethyl]piperidin-1-yl]propoxy]benzonitrileIC50226.0 [1]
4-[3-[4-[Cyclopentyl-hydroxy-(1,3-thiazol-2-yl)methyl]piperidin-1-yl]propoxy]benzonitrileIC50242.0 [1]
5-[[4-[[6-(2,2,2-Trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrileIC5031.0 [1]
4-Methyl-1-(2H-triazol-4-ylmethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5023.0 [1]
1-(3-Hydroxy-2-propan-2-yloxypropyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5023.0 [1]
1-(2-Hydroxyethyl)-4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5044.0 [1]
2-[2-Cyano-4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indol-1-yl]acetamideIC5027.0 [1]
6-Methoxy-4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrileIC5040.0 [1]
6-Hydroxy-1-(2-hydroxyethyl)-4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5027.0 [1]
6-Hydroxy-4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrileIC5027.0 [1]
2-[2-Cyano-6-methoxy-4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indol-1-yl]acetamideIC5037.0 [1]
1-(2-Hydroxyethyl)-6-methoxy-4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5016.0 [1]
6-Methoxy-1-(1H-pyrazol-4-ylmethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5024.0 [1]
6-Hydroxy-4-methyl-1-(1H-pyrazol-4-ylmethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5018.0 [1]
6-Methoxy-4-methyl-1-(1H-pyrazol-4-ylmethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5012.0 [1]
6-Hydroxy-4-methyl-1-(2H-triazol-4-ylmethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5017.0 [1]
6-Methoxy-4-methyl-1-(2H-triazol-4-ylmethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5016.0 [1]
3-Methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrileIC50111.0 [1]
4-[3-[4-[Hydroxy-pyridin-2-yl-(1,3-thiazol-2-yl)methyl]piperidin-1-yl]propoxy]benzonitrileIC5090.0 [1]
4-[3-[4-[Hydroxy-pyridin-2-yl-(1,3-thiazol-2-yl)methyl]piperidin-1-yl]propoxy]benzenesulfonamideIC50246.0 [1]
1-(2,3-Dihydroxypropyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5037.0 [1]
(2S)-2-Acetamido-N-[(2S)-1-[[(3S,6S,9S,15R,28S)-15-benzyl-3-[3-(diaminomethylideneamino)propyl]-6-methyl-2,5,8,14,17,27-hexaoxo-1,4,7,13,16,26-hexazatricyclo[26.3.0.09,13]hentriacontan-18-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-5-(diaminomethylideneamino)pentanamideKi23.8 [1]
4-(4-(4-Chlorobenzyl)piperazin-1-yl)-6-ethylthieno[2,3-d]pyrimidineIC5014000.0 [1]
6-Ethyl-4-(4-(thiazol-2-yl)piperazin-1-yl)thieno[2,3-d]pyrimidineIC5046000.0 [1]
6-Butyl-4-(4-(5,5-dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)thieno[2,3-d]pyrimidineIC50750.0 [1]
4-(4-(1,3,4-Thiadiazol-2-yl)piperazin-1-yl)-6-ethylthieno[2,3-d]pyrimidineIC50193000.0 [1]
4-[3-[4-[(3-Fluorophenyl)-hydroxy-(1,3-thiazol-2-yl)methyl]piperidin-1-yl]propoxy]benzenesulfonamideIC50354.0 [1]
4-[3-[4-[(3-Fluorophenyl)-hydroxy-(1,3-thiazol-2-yl)methyl]piperidin-1-yl]propoxy]benzonitrileIC50460.0 [1]
6-Ethyl-4-(4-pyridin-2-ylpiperazin-1-yl)thieno[2,3-d]pyrimidineIC5058000.0 [1]
4-(4-Benzylpiperazin-1-yl)-6-ethylthieno[2,3-d]pyrimidineIC5052000.0 [1]
6-Ethyl-4-(4-(pyrimidin-2-yl)piperazin-1-yl)thieno[2,3-d]pyrimidineIC5087000.0 [1]
3-Fluoro-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrileIC5096.0 [1]
1-(2-Hydroxyethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5035.0 [1]
6-Hydroxy-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrileIC5020.0 [1]
4-[3-[4-(Cyclopentyl-hydroxy-piperidin-2-ylmethyl)piperidin-1-yl]propoxy]benzonitrileIC5028000.0 [1]
4-[3-[4-[Cyclopentyl-hydroxy-(3-methoxyphenyl)methyl]piperidin-1-yl]propoxy]benzonitrileIC501100.0 [1]
2-[2-Cyano-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indol-1-yl]acetamideIC5025.0 [1]
6-Methoxy-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrileIC5022.0 [1]
1-[(2R)-2,3-Dihydroxypropyl]-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5046.0 [1]
1-[(2S)-3-Hydroxy-2-methoxypropyl]-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5037.0 [1]
1-(2H-Triazol-4-ylmethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5027.0 [1]
6-Ethoxy-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrileIC5047.0 [1]
4-Chloro-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrileIC5022.0 [1]
1-[(2S)-2,3-Dihydroxypropyl]-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5042.0 [1]
1-(2-Hydroxy-3-methoxypropyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC50101.0 [1]
1-[(2R)-3-Hydroxy-2-methoxypropyl]-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5040.0 [1]
2-[2-Cyano-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indol-1-yl]propanamideIC50244.0 [1]
1-(1H-Pyrazol-4-ylmethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5023.0 [1]
6-Fluoro-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrileIC50109.0 [1]
3-Amino-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrileIC50124.0 [1]
6-Methylsulfanyl-4-[4-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]piperazin-1-yl]thieno[2,3-d]pyrimidineIC5020000.0 [1]
6-Propyl-4-[4-[5-(trifluoromethyl)-1H-1,2,4-triazol-3-yl]piperazin-1-yl]thieno[2,3-d]pyrimidineIC50200000.0 [1]
6-(2-Chloroethyl)-4-[4-(5,5-dimethyl-4H-1,3-thiazol-2-yl)piperazin-1-yl]thieno[2,3-d]pyrimidineIC50193.0 [1]
6-Ethyl-4-[4-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]piperazin-1-yl]thieno[2,3-d]pyrimidineIC501300.0 [1]
2-[4-[6-(2,2,2-Trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]piperazin-1-yl]-5-(trifluoromethyl)-1,3,4-oxadiazoleIC501400.0 [1]
6-Cyclopropyl-4-[4-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]piperazin-1-yl]thieno[2,3-d]pyrimidineIC502000.0 [1]
6-Propyl-4-[4-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]piperazin-1-yl]thieno[2,3-d]pyrimidineIC50650.0 [1]
4-[4-(5,5-Dimethyl-4H-1,3-thiazol-2-yl)piperazin-1-yl]-6-(1,1,1-trifluoropropan-2-yl)thieno[2,3-d]pyrimidineIC50765.0 [1]
Items per page: 1 - 10 of 74
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References

This online tool may be cited as follows

MLA

"Quest Database™ Menin/Histone-lysine N-methyltransferase MLL Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Nov. 2024, https://www.aatbio.com/data-sets/menin-histone-lysine-n-methyltransferase-mll-inhibitors-ic50-ki.

APA

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