Menin/Histone-lysine N-methyltransferase MLL Inhibitors (IC50, Ki)

Structure ▲ ▼	Compound Name ▲ ▼	Standard Type ▲ ▼	Standard Values (in nM) ▲ ▼
	4-(2-Benzyl-2,7-diazaspiro[3.4]octan-7-yl)-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidine	IC50	56.0 [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]pyrimidine	IC50	120.0 [1], 385.0 [2]
	4-(2-Benzyl-2,7-diazaspiro[4.5]decan-7-yl)-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidine	IC50	140.0 [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]methanone	IC50	92.0 [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]pyrimidine	IC50	8.0 [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]pyrimidine	IC50	110.0 [1], 190.0 [2]
	4-(4-(5,5-Dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-propylthieno[2,3-d]pyrimidine	IC50	450.0 [1]
	CID 91667931	IC50	14.0 [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-carbonitrile	IC50	21.0 [1]
	CID 72201086	IC50	46.0 [1]
	CID 90455046	IC50	15.0 [1]
	4-(3-(4-(Hydroxy(phenyl)cyclopentylmethyl)piperidine-1-yl)propyloxy)benzonitrile	IC50	390.0 [1]
	4-[3-[4-(Cyclopentyl-hydroxy-pyridin-2-ylmethyl)piperidin-1-yl]propoxy]benzenesulfonamide	IC50	114.0 [1]
	4-[3-[4-[Cyclopentyl-(3,5-difluorophenyl)-hydroxymethyl]piperidin-1-yl]propoxy]benzonitrile	IC50	437.0 [1]
	4-[3-[4-(Cyclopentyl-hydroxy-pyridin-2-ylmethyl)piperidin-1-yl]propoxy]benzonitrile	IC50	302.0 [1]
	4-[3-[4-[Cyclopentyl-(3-fluorophenyl)-hydroxymethyl]piperidin-1-yl]propoxy]benzonitrile	IC50	197.0 [1]
	4-[3-[4-[(3-Chlorophenyl)-cyclopentyl-hydroxymethyl]piperidin-1-yl]propoxy]benzonitrile	IC50	226.0 [1]
	4-[3-[4-[Cyclopentyl-hydroxy-(1,3-thiazol-2-yl)methyl]piperidin-1-yl]propoxy]benzonitrile	IC50	242.0 [1]
	5-[[4-[[6-(2,2,2-Trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrile	IC50	31.0 [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-carbonitrile	IC50	23.0 [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-carbonitrile	IC50	23.0 [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-carbonitrile	IC50	44.0 [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]acetamide	IC50	27.0 [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-carbonitrile	IC50	40.0 [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-carbonitrile	IC50	27.0 [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-carbonitrile	IC50	27.0 [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]acetamide	IC50	37.0 [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-carbonitrile	IC50	16.0 [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-carbonitrile	IC50	24.0 [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-carbonitrile	IC50	18.0 [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-carbonitrile	IC50	12.0 [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-carbonitrile	IC50	17.0 [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-carbonitrile	IC50	16.0 [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-carbonitrile	IC50	111.0 [1]
	4-[3-[4-[Hydroxy-pyridin-2-yl-(1,3-thiazol-2-yl)methyl]piperidin-1-yl]propoxy]benzonitrile	IC50	90.0 [1]
	4-[3-[4-[Hydroxy-pyridin-2-yl-(1,3-thiazol-2-yl)methyl]piperidin-1-yl]propoxy]benzenesulfonamide	IC50	246.0 [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-carbonitrile	IC50	37.0 [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)pentanamide	Ki	23.8 [1]
	4-(4-(4-Chlorobenzyl)piperazin-1-yl)-6-ethylthieno[2,3-d]pyrimidine	IC50	14000.0 [1]
	6-Ethyl-4-(4-(thiazol-2-yl)piperazin-1-yl)thieno[2,3-d]pyrimidine	IC50	46000.0 [1]
	6-Butyl-4-(4-(5,5-dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)thieno[2,3-d]pyrimidine	IC50	750.0 [1]
	4-(4-(1,3,4-Thiadiazol-2-yl)piperazin-1-yl)-6-ethylthieno[2,3-d]pyrimidine	IC50	193000.0 [1]
	4-[3-[4-[(3-Fluorophenyl)-hydroxy-(1,3-thiazol-2-yl)methyl]piperidin-1-yl]propoxy]benzenesulfonamide	IC50	354.0 [1]
	4-[3-[4-[(3-Fluorophenyl)-hydroxy-(1,3-thiazol-2-yl)methyl]piperidin-1-yl]propoxy]benzonitrile	IC50	460.0 [1]
	6-Ethyl-4-(4-pyridin-2-ylpiperazin-1-yl)thieno[2,3-d]pyrimidine	IC50	58000.0 [1]
	4-(4-Benzylpiperazin-1-yl)-6-ethylthieno[2,3-d]pyrimidine	IC50	52000.0 [1]
	6-Ethyl-4-(4-(pyrimidin-2-yl)piperazin-1-yl)thieno[2,3-d]pyrimidine	IC50	87000.0 [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-carbonitrile	IC50	96.0 [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-carbonitrile	IC50	35.0 [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-carbonitrile	IC50	20.0 [1]
	4-[3-[4-(Cyclopentyl-hydroxy-piperidin-2-ylmethyl)piperidin-1-yl]propoxy]benzonitrile	IC50	28000.0 [1]
	4-[3-[4-[Cyclopentyl-hydroxy-(3-methoxyphenyl)methyl]piperidin-1-yl]propoxy]benzonitrile	IC50	1100.0 [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]acetamide	IC50	25.0 [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-carbonitrile	IC50	22.0 [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-carbonitrile	IC50	46.0 [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-carbonitrile	IC50	37.0 [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-carbonitrile	IC50	27.0 [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-carbonitrile	IC50	47.0 [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-carbonitrile	IC50	22.0 [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-carbonitrile	IC50	42.0 [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-carbonitrile	IC50	101.0 [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-carbonitrile	IC50	40.0 [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]propanamide	IC50	244.0 [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-carbonitrile	IC50	23.0 [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-carbonitrile	IC50	109.0 [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-carbonitrile	IC50	124.0 [1]
	6-Methylsulfanyl-4-[4-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]piperazin-1-yl]thieno[2,3-d]pyrimidine	IC50	20000.0 [1]
	6-Propyl-4-[4-[5-(trifluoromethyl)-1H-1,2,4-triazol-3-yl]piperazin-1-yl]thieno[2,3-d]pyrimidine	IC50	200000.0 [1]
	6-(2-Chloroethyl)-4-[4-(5,5-dimethyl-4H-1,3-thiazol-2-yl)piperazin-1-yl]thieno[2,3-d]pyrimidine	IC50	193.0 [1]
	6-Ethyl-4-[4-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]piperazin-1-yl]thieno[2,3-d]pyrimidine	IC50	1300.0 [1]
	2-[4-[6-(2,2,2-Trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]piperazin-1-yl]-5-(trifluoromethyl)-1,3,4-oxadiazole	IC50	1400.0 [1]
	6-Cyclopropyl-4-[4-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]piperazin-1-yl]thieno[2,3-d]pyrimidine	IC50	2000.0 [1]
	6-Propyl-4-[4-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]piperazin-1-yl]thieno[2,3-d]pyrimidine	IC50	650.0 [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]pyrimidine	IC50	765.0 [1]

Entire TableStructureCompound NameStandard TypeStandard Values (in nM)

Items per page: 510All1 - 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., 9 May. 2024, https://www.aatbio.com/data-sets/menin-histone-lysine-n-methyltransferase-mll-inhibitors-ic50-ki.
APA	AAT Bioquest, Inc. (2024, May 9). 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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