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Menin 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-[4-(5,5-Dimethyl-4H-1,3-thiazol-2-yl)piperazin-1-yl]-5,6,7,8-tetrahydro-[1]benzothiolo[2,3-d]pyrimidineIC501200.0 [1], 1900.0 [2]
4-(4-(5,5-Dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-propylthieno[2,3-d]pyrimidineIC50430.0 [1], 446.0 [2]
2-[4-(4-Fluorophenyl)-1,3-thiazol-2-yl]acetamideIC50200000.0 [1], 230000.0 [2]
CID 72201086IC5046.0 [1], 190.0 [2]
N-(3-Imidazol-1-ylpropyl)-8-thia-4,6-diazatricyclo[7.5.0.02,7]tetradeca-1(9),2,4,6-tetraen-3-amineIC5035000.0 [1], 83000.0 [2]
4-(4-(5,5-Dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-ethylthieno[2,3-d]pyrimidineIC501200.0 [1]
4-(4-Benzylpiperazin-1-yl)-6-ethylthieno[2,3-d]pyrimidineIC5042000.0 [1], 85000.0 [2]
2-[4-(4-Methoxyphenyl)-1,3-thiazol-2-yl]acetamideIC5033000.0 [1], 67000.0 [2]
5-Acetyl-9-(4-tert-butylphenyl)-6-pyridin-3-yl-8,9,10,11-tetrahydro-6H-benzo[b][1,4]benzodiazepin-7-oneIC507000.0 [1], 13000.0 [2]
5-Acetyl-9-(4-tert-butylphenyl)-6-pyridin-4-yl-8,9,10,11-tetrahydro-6H-benzo[b][1,4]benzodiazepin-7-oneIC5028000.0 [1], 29000.0 [2]
LoperamideIC5069000.0 [1]
4-[4-[5-(Difluoromethyl)-1,3,4-thiadiazol-2-yl]piperazin-1-yl]-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidineIC5082.0 [1]
5-Methyl-2-phenyl-2H-1,2,3-triazole-4-carboxamideIC50380000.0 [1]
11-(1,3-Benzodioxol-5-yl)-3,3-dimethyl-2,3,4,5,10,11-hexahydro-1H-dibenzo[b,e][1,4]diazepin-1-oneIC5012000.0 [1]
MI-3 (Menin-MLL Inhibitor)IC50650.0 [1]
4-[3-(4-Benzhydrylpiperazin-1-yl)-2-hydroxypropoxy]benzonitrileIC5077000.0 [1]
4-[2-Hydroxy-3-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]propoxy]benzonitrileIC5012800.0 [1]
2-(4-Phenyl-1,3-thiazol-2-yl)acetamideIC502000000.0 [1]
CID 91667931IC5014.7 [1]
N-(1-Benzylpiperidin-4-yl)-5,6-dimethylthieno[2,3-d]pyrimidin-4-amineIC508700.0 [1]
3,3-Dimethyl-11-(3,4,5-trimethoxyphenyl)-2,3,4,5,10,11-hexahydro-1H-dibenzo[b,e][1,4]diazepin-1-oneIC5035000.0 [1]
4-(6-Ethylthiopheno[3,2-e]pyrimidin-4-yl)piperazinyl 2-furyl ketoneIC5012000.0 [1]
CID 90455046IC5032.0 [1]
4-(6-Ethylthiopheno[3,2-e]pyrimidin-4-yl)piperazinyl phenyl ketoneIC5010000.0 [1]
4-(4-Methylpiperazin-1-yl)-5,6-diphenylfuro[2,3-d]pyrimidineIC50500000.0 [1]
[1-(3-Phenoxypropyl)-4-piperidinyl]-diphenylmethanolIC50250000.0 [1]
9-(1,3-Benzodioxol-5-yl)-6-pyridin-4-yl-5,6,8,9,10,11-hexahydrobenzo[b][1,4]benzodiazepin-7-oneIC50230000.0 [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]benzonitrileIC50436.0 [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]
4-Methyl-1-(1H-pyrazol-5-ylmethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5033.0 [1]
4-Methyl-1-(2-piperidin-4-ylethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5014.0 [1]
4-Methyl-1-(2-morpholin-4-ylethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5022.0 [1]
4-[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]ethyl]-N-methylpiperazine-1-sulfonamideIC5032.0 [1]
1-[2-(4-Ethylsulfonylpiperazin-1-yl)ethyl]-4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5055.0 [1]
4-Methyl-1-(2-piperazin-1-ylethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5015.0 [1]
4-Methyl-1-[2-(4-methylpiperazin-1-yl)ethyl]-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5013.0 [1]
4-Methyl-1-[2-(1-methylsulfonylpiperidin-4-yl)ethyl]-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5040.0 [1]
4-Methyl-1-[2-(5-oxomorpholin-2-yl)ethyl]-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5028.0 [1]
4-Methyl-1-[2-(4-propanoylpiperazin-1-yl)ethyl]-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5083.0 [1]
1-[2-(1-Acetylpiperidin-4-yl)ethyl]-4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC50130.0 [1]
4-Methyl-1-[2-(4-propylpiperazin-1-yl)ethyl]-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5039.0 [1]
1-[2-(4-Acetylpiperazin-1-yl)ethyl]-4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5018.0 [1]
4-[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]ethyl]piperazine-1-sulfonamideIC5026.0 [1]
1-[2-(4-Formylpiperazin-1-yl)ethyl]-4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5013.0 [1]
1-[2-[4-(2-Cyclopentylacetyl)piperazin-1-yl]ethyl]-4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5057.0 [1]
4-Methyl-1-[(5-oxomorpholin-2-yl)methyl]-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC507.5 [1]
1-[2-[4-(3-Cyclopentylpropanoyl)piperazin-1-yl]ethyl]-4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5042.0 [1]
4-Methyl-1-[2-(4-methylsulfonylpiperazin-1-yl)ethyl]-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5013.0 [1]
6-(2,2-Difluoroethyl)-4-[4-(5,5-dimethyl-4H-1,3-thiazol-2-yl)piperazin-1-yl]thieno[2,3-d]pyrimidineIC5065.0 [1]
1-[2-[4-(2-Fluoroacetyl)piperazin-1-yl]ethyl]-4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5010.0 [1]
4-Methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1-[2-[4-(trifluoromethylsulfonyl)piperazin-1-yl]ethyl]indole-2-carbonitrileIC5071.0 [1]
4-Methyl-1-[2-[4-(2,2,2-trifluoroacetyl)piperazin-1-yl]ethyl]-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5075.0 [1]
1-[2-[4-(2,2-Difluoroacetyl)piperazin-1-yl]ethyl]-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-[4-[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]ethyl]piperazin-1-yl]propanamideIC5021.0 [1]
4-Methyl-1-[[(2S)-5-oxomorpholin-2-yl]methyl]-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC503.6 [1]
4-Methyl-1-[[(2R)-5-oxomorpholin-2-yl]methyl]-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC50123.0 [1]
4-[4-(4-Chlorophenyl)-3,6-dihydro-2H-pyridin-1-yl]-2-cyclopentyl-2-phenylbutan-1-amineIC50830.0 [1]
[4-[[2-[6-(2,2,2-Trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]-2,7-diazaspiro[4.4]nonan-7-yl]methyl]phenyl]methanesulfonamideIC504.0 [1]
2-[N-Methyl-4-[[2-[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]-2,7-diazaspiro[4.4]nonan-7-yl]methyl]anilino]ethanolIC5010.0 [1]
N-[4-[[2-[6-(2,2,2-Trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]-2,7-diazaspiro[4.4]nonan-7-yl]methyl]phenyl]prop-2-enamideIC5010.0 [1]
[4-[[2-[6-(2,2,2-Trifluoroethyl)thieno[3,2-d]pyrimidin-4-yl]-2,7-diazaspiro[4.4]nonan-7-yl]methyl]phenyl]methanesulfonamideIC5010.0 [1]
4-[4-[[2-[6-(2,2-Difluoroethyl)thieno[2,3-d]pyrimidin-4-yl]-2,7-diazaspiro[4.4]nonan-7-yl]methyl]phenyl]morpholineIC5010.0 [1]
1-[4-[[2-[6-(2,2,2-Trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]-2,7-diazaspiro[4.4]nonan-7-yl]methyl]phenyl]ethanesulfonamideIC5010.0 [1]
2-Methyl-2-[4-[[2-[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]-2,7-diazaspiro[4.4]nonan-7-yl]methyl]phenyl]propanenitrileIC5020.0 [1]
2-[4-[[2-[6-(2,2,2-Trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]-2,7-diazaspiro[4.4]nonan-7-yl]methyl]phenyl]acetonitrileIC5020.0 [1]
N-(2-Hydroxyethyl)-1-[4-[[2-[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]-2,7-diazaspiro[4.4]nonan-7-yl]methyl]phenyl]methanesulfonamideIC5010.0 [1]
(1R,9R)-11-(2-Hydroxy-5-phenylpentyl)-2,11-diazatricyclo[7.3.1.02,7]trideca-4,6-dien-3-oneIC501.0 [1]
1-[2-(1-Formylpiperidin-4-yl)ethyl]-4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrileIC5063.0 [1]
4-[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]ethyl]piperidine-1-sulfonamideIC5038.0 [1]
4-[4-(5,5-Dimethyl-4H-1,3-thiazol-2-yl)piperazin-1-yl]-6-(trifluoromethyl)thieno[2,3-d]pyrimidineIC5046.0 [1]
4-(4-(4-Chlorobenzyl)piperazin-1-yl)-6-ethylthieno[2,3-d]pyrimidineIC5030000.0 [1]
4-(3-(4-(Hydroxydiphenylmethyl)piperidin-1-yl)propoxy)benzonitrileIC5010800.0 [1]
3-(Pyridin-3-yl)benzenamineIC5050000.0 [1]
4-[3-(4-Benzhydrylpiperidin-1-yl)propoxy]benzonitrileIC50205000.0 [1]
4-[3-[4-[Hydroxy(phenyl)methyl]piperidin-1-yl]propoxy]benzonitrileIC50234000.0 [1]
4-[3-[4-(1-Hydroxy-1-phenylpentyl)piperidin-1-yl]propoxy]benzonitrileIC5015300.0 [1]
4-[3-[4-(Cyclopropyl-hydroxy-phenylmethyl)piperidin-1-yl]propoxy]benzonitrileIC5011200.0 [1]
4-[3-[4-(1-Hydroxy-1-phenylethyl)piperidin-1-yl]propoxy]benzonitrileIC50295000.0 [1]
4-[3-[4-(Cyclohexyl-hydroxy-phenylmethyl)piperidin-1-yl]propoxy]benzonitrileIC501700.0 [1]
4-(3-{4-[(S)-Cyclopentyl(Hydroxy)phenylmethyl]piperidin-1-Yl}propoxy)benzonitrileIC50529.0 [1]
4-(3-{4-[(R)-Cyclopentyl(Hydroxy)phenylmethyl]piperidin-1-Yl}propoxy)benzonitrileIC50270.0 [1]
4-[3-[4-(1-Hydroxy-2-methyl-1-phenylpropyl)piperidin-1-yl]propoxy]benzonitrileIC504100.0 [1]
4-[3-[4-(Cyclobutyl-hydroxy-phenylmethyl)piperidin-1-yl]propoxy]benzonitrileIC504000.0 [1]
6-Benzyl-4-(4-(5,5-dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)thieno[2,3-d]pyrimidineIC504600.0 [1]
6-Bromo-4-(4-(5,5-dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)thieno[2,3-d]pyrimidineIC504800.0 [1]
2-[3-[(3S,9S,15S,18S,29S)-18-Amino-15-[[3-(2-methylpropyl)phenyl]methyl]-2,5,8,14,17,28-hexaoxospiro[1,4,7,13,16,27-hexazatricyclo[27.3.0.09,13]dotriacontane-6,1'-cyclobutane]-3-yl]propyl]guanidineIC5036000.0 [1]
2-[3-[(3S,9S,15S,18S,29S)-18-Amino-15-[(4-fluorophenyl)methyl]-2,5,8,14,17,28-hexaoxospiro[1,4,7,13,16,27-hexazatricyclo[27.3.0.09,13]dotriacontane-6,1'-cyclobutane]-3-yl]propyl]guanidineIC50422.0 [1]
2-[3-[(3S,9S,15S,18S,29S)-18-Amino-15-[(3,5-difluorophenyl)methyl]-2,5,8,14,17,28-hexaoxospiro[1,4,7,13,16,27-hexazatricyclo[27.3.0.09,13]dotriacontane-6,1'-cyclobutane]-3-yl]propyl]guanidineIC5018.5 [1]
2-[3-[(3S,9S,15R,18S,29S)-18-Amino-15-[(3,5-difluorophenyl)methyl]-2,5,8,14,17,28-hexaoxospiro[1,4,7,13,16,27-hexazatricyclo[27.3.0.09,13]dotriacontane-6,1'-cyclobutane]-3-yl]propyl]guanidineKi143000.0 [1]
(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-Acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]heptanoyl]amino]-3-phenylpropanoyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]-N-ethylpyrrolidine-2-carboxamideIC507390.0 [1]
(2S)-2-Acetamido-N-[(2S)-1-[[(3S,6S,9S,15S,18S,27S)-15-benzyl-3-[3-(diaminomethylideneamino)propyl]-6-methyl-2,5,8,14,17,26-hexaoxo-1,4,7,13,16,25-hexazatricyclo[25.3.0.09,13]triacontan-18-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-5-(diaminomethylideneamino)pentanamideIC5063.3 [1]
(2S)-2-Acetamido-N-[(2S)-1-[[(3S,6S,9S,15S,18S,26S)-15-benzyl-3-[3-(diaminomethylideneamino)propyl]-6-methyl-2,5,8,14,17,25-hexaoxo-1,4,7,13,16,24-hexazatricyclo[24.3.0.09,13]nonacosan-18-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-5-(diaminomethylideneamino)pentanamideIC50514.0 [1]
(2S)-2-Acetamido-N-[(2S)-1-[[(3S,6S,9S,15S,18S,29S)-15-benzyl-3-[3-(diaminomethylideneamino)propyl]-6-methyl-2,5,8,14,17,28-hexaoxo-1,4,7,13,16,27-hexazatricyclo[27.3.0.09,13]dotriacontan-18-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-5-(diaminomethylideneamino)pentanamideIC5025.0 [1]
2-[3-[(3S,6S,9S,15S,18S,29S)-18-Amino-15-benzyl-6-methyl-2,5,8,14,17,28-hexaoxo-1,4,7,13,16,27-hexazatricyclo[27.3.0.09,13]dotriacontan-3-yl]propyl]guanidineIC50665.0 [1]
(2S)-2-Acetamido-N-[(2S)-1-[[(3S,6S,9S,15S,18S,25S)-15-benzyl-3-[3-(diaminomethylideneamino)propyl]-6-methyl-2,5,8,14,17,24-hexaoxo-1,4,7,13,16,23-hexazatricyclo[23.3.0.09,13]octacosan-18-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-5-(diaminomethylideneamino)pentanamideIC5011000.0 [1]
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References

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MLA

"Quest Database™ Menin Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 10 May. 2024, https://www.aatbio.com/data-sets/menin-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, May 10). Quest Database™ Menin Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/menin-inhibitors-ic50-ki.
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