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Protein farnesyltransferase 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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▼
LonafarnibIC501.9 [1]
CID 395754IC500.5 [1]
N-Ethyl-2-(2-phenyl-1H-indol-3-yl)-N-pyridin-4-ylmethyl-acetamideIC50106.0 [1]
4-[(5-{[4-(3-Chlorophenyl)-3-oxopiperazin-1-YL]methyl}-1H-imidazol-1-YL)methyl]benzonitrileIC502.0 [1]
1-[4-(13-Chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-ylidene)piperidin-1-yl]-2-pyridin-4-ylethanoneIC50250.0 [1]
TipifarnibIC500.9 [1]
Bms-214662IC501.35 [1]
1-[4-[(2S)-6-Bromo-13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl]piperazin-1-yl]-2-(1-oxidopyridin-1-ium-4-yl)ethanoneIC501500.0 [1]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2R)-2-Amino-3-sulfanylpropanoyl]amino]-3-methylbutanoyl]amino]-3-methylpentanoyl]amino]-4-methylsulfanylbutanoic acidIC50200.0 [1], 340.0 [2], 420.0 [3]
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2R)-2-Amino-3-sulfanylpropanoyl]amino]-3-methylbutanoyl]amino]-3-methylpentanoyl]amino]-4-methylsulfanylbutanoic acidKi1100.0 [1]
1-[4-(6-Bromo-13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-ylidene)piperidin-1-yl]-2-(1-oxidopyridin-1-ium-4-yl)ethanoneIC5090.0 [1]
Chaetomellic acid AIC5055.0 [1], 60.0 [2], 175.0 [3], 180.0 [4]
3-Oxo-18-oxa-2,5,9,11-tetrazahexacyclo[17.6.2.22,5.113,17.07,11.022,26]triaconta-1(25),7,9,13(28),14,16,19(27),20,22(26),23-decaene-16-carbonitrileIC500.1 [1], 0.2 [2], 0.29 [3]
1-[4-(13-Chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl)piperazin-1-yl]-2-pyridin-4-ylethanoneIC5036.0 [1], 160.0 [2], 360.0 [3], 3700.0 [4]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-Amino-3-sulfanylpropanoyl]amino]-3-methylbutanoyl]amino]-3-phenylpropanoyl]amino]-4-methylsulfanylbutanoic acidIC5025.0 [1], 37.0 [2], 600.0 [3], 1000.0 [4]
1-[4-(6-Bromo-13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl)piperazin-1-yl]-2-(1-oxidopyridin-1-ium-4-yl)ethanoneIC5047.0 [1], 450.0 [2], 1200.0 [3], 4000.0 [4]
(2S)-2-[[4-[(1H-Imidazol-5-ylmethylamino)methyl]-2-(2-methylphenyl)benzoyl]amino]-4-methylsulfanylbutanoic acidIC500.86 [1], 1.0 [2], 1.4 [3], 1.8 [4]
4-[2-[4-(6-Bromo-13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl)piperazin-1-yl]-2-oxoethyl]piperidine-1-carboxamideIC5049.0 [1], 590.0 [2]
(4E,8E)-2-[(E)-3-[5-[[[(2S)-1-[[(2S)-1-[[(1S)-1-Carboxy-3-methylsulfanylpropyl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]methyl]-1-methylimidazol-2-yl]prop-2-enyl]-2-ethoxycarbonyl-5,9,13-trimethyltetradeca-4,8,12-trienoic acidIC50640.0 [1]
(4E,8E)-2-[(E)-3-[5-[[[(2S)-1-[[(2S)-1-[[(1S)-1-Carboxy-3-methylsulfanylpropyl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]methyl]-1-methylimidazol-2-yl]prop-2-enyl]-2-ethoxycarbonyl-5,9,13-trimethyltetradeca-4,8,12-trienoic acidKi500.0 [1], 15000.0 [2], 17000.0 [3]
(4E,8E)-2-[3-[5-[[[(2S)-1-[[(2S)-1-[[(1S)-1-Carboxy-3-methylsulfanylpropyl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]methyl]-1-methylimidazol-2-yl]propyl]-2-ethoxycarbonyl-5,9,13-trimethyltetradeca-4,8,12-trienoic acidIC50240.0 [1]
(4E,8E)-2-[3-[5-[[[(2S)-1-[[(2S)-1-[[(1S)-1-Carboxy-3-methylsulfanylpropyl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]methyl]-1-methylimidazol-2-yl]propyl]-2-ethoxycarbonyl-5,9,13-trimethyltetradeca-4,8,12-trienoic acidKi230.0 [1], 5600.0 [2], 7700.0 [3]
2-[4-((R)-2-Amino-3-mercapto-propylamino)-2-naphthalen-1-yl-benzoylamino]-4-methyl-pentanoic acidIC5054.0 [1], 200.0 [2], 203.0 [3]
[4-(3-Pyridyloxymethyl)-2-(2-methylphenyl)benzoyl]methionineIC500.4 [1]
1-[4-[(2R)-6-Bromo-13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl]piperazin-1-yl]-2-(1-oxidopyridin-1-ium-4-yl)ethanoneIC5025.0 [1], 26.0 [2], 500.0 [3]
4-[[5-[[[(3S)-1-[(3-Chlorophenyl)methyl]-2-oxopyrrolidin-3-yl]amino]methyl]imidazol-1-yl]methyl]benzonitrileIC500.52 [1], 1.9 [2]
1-[4-(13-Chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-ylidene)piperidin-1-yl]-2-(1-oxidopyridin-1-ium-4-yl)ethanoneIC50530.0 [1]
2'-Methoxy-4'-[[(R)-2-amino-3-mercaptopropyl]amino]biphenyl-3-carboxylic acidIC5037.0 [1], 40.0 [2]
4-[2-[4-[(2S)-6,15-Dibromo-13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl]piperidin-1-yl]-2-oxoethyl]piperidine-1-carboxamideIC5094.0 [1], 378.0 [2], 2000.0 [3]
2-[3-(3-Ethyl-1-methyl-2-oxo-azepan-3-yl)-phenoxy]-4-imidazol-1-ylmethyl-benzonitrileIC502.9 [1], 3.0 [2]
[2-Oxo-2-[[(2E,6E,10E)-3,7,11,15-tetramethylhexadeca-2,6,10,14-tetraenoxy]amino]ethyl]phosphonic acidIC503500.0 [1], 8700.0 [2], 18500.0 [3]
1-[4-(13-Chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl)piperazin-1-yl]-2-pyridin-3-ylethanoneIC50530.0 [1], 1000.0 [2], 6220.0 [3]
4-(13-Chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl)-N-pyridin-4-ylpiperazine-1-carboxamideIC50900.0 [1], 940.0 [2], 10500.0 [3]
1-[4-(13-Chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl)piperazin-1-yl]-2-phenylethanoneIC502700.0 [1], 2730.0 [2], 12000.0 [3]
4-(13-Chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl)-N-pyridin-2-ylpiperazine-1-carboxamideIC50950.0 [1], 1300.0 [2]
4-[2-[4-[(2R)-6-Bromo-13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl]piperazin-1-yl]-2-oxoethyl]piperidine-1-carboxamideIC5043.0 [1], 350.0 [2]
1-[4-[(2R)-6,15-Dibromo-13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl]piperidin-1-yl]-2-(1-oxidopyridin-1-ium-4-yl)ethanoneIC501.3 [1], 2.0 [2], 10.0 [3]
1-[4-(13-Chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl)piperazin-1-yl]-2-pyridin-2-ylethanoneIC50360.0 [1], 5000.0 [2]
4-(13-Chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl)-N-pyridin-3-ylpiperazine-1-carboxamideIC501300.0 [1], 1340.0 [2], 4800.0 [3]
1-[4-[(2S)-6-Bromo-13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl]piperazin-1-yl]-2-(1-methylpiperidin-4-yl)ethanoneIC5050.0 [1], 900.0 [2]
4-[(1S)-1-Amino-1-(3-methylimidazol-4-yl)ethyl]-2-[3-[(3S)-3-ethyl-1-methyl-2-oxoazepan-3-yl]phenoxy]benzonitrileIC500.06 [1]
4-[2-[4-[(2S)-6,12-Dibromo-13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl]piperidin-1-yl]-2-oxoethyl]piperidine-1-carboxamideIC505.0 [1], 325.0 [2]
4-(6-Bromo-13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl)-1-N-cyclohexyl-2-N-(3-imidazol-1-ylpropyl)piperazine-1,2-dicarboxamideIC500.1 [1], 0.56 [2], 1.5 [3]
GliotoxinIC501100.0 [1], 80000.0 [2]
CID 3005532IC500.5 [1], 40.0 [2]
Methyl (2S)-2-[[4-[[(2R)-2-amino-3-sulfanylpropyl]amino]-2-phenylbenzoyl]amino]-4-methylpentanoateIC5017.0 [1], 30000.0 [2]
HalenaquinoneIC50930.0 [1]
Clavaric acidIC50350.0 [1], 1300.0 [2]
(1R,8R,9S,13S)-11-[2-(2-Methoxyphenyl)prop-2-enoyl]-1-phenyl-11-azatetracyclo[6.5.2.02,7.09,13]pentadeca-2,4,6-triene-9-carboxylic acidIC5050.0 [1]
(1R,8R,9S,13S)-11-[2-(2-Methoxyphenyl)prop-2-enoyl]-1-phenyl-11-azatetracyclo[6.5.2.02,7.09,13]pentadeca-2,4,6-triene-9-carboxylic acidKi25.0 [1]
(2S)-2-[[4-[[Butyl(2-cyclohexylethyl)amino]methyl]-2-(2-methylphenyl)benzoyl]amino]-4-methylsulfanylbutanoic acidIC501.1 [1]
3-(4-Chlorophenyl)-4-cyano-5-(isopropylthio)thiophene-2-carboxylic acidIC5016000.0 [1]
(S)-2-{[5-((R)-2-Amino-3-mercapto-propylamino)-biphenyl-2-carbonyl]-amino}-4-methyl-pentanoic acidIC5025.0 [1], 183.0 [2]
H-Cys-4-Abz-Met-OHIC5072.0 [1], 150.0 [2]
ClavarinoneIC508000.0 [1], 15000.0 [2]
1-[4-(13-Chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-ylidene)piperidin-1-yl]-2-phenylethanoneIC50800.0 [1]
[(2Z,6E)-7,11-Dimethyl-3-prop-2-enyldodeca-2,6,10-trienyl] phosphono hydrogen phosphateIC50119.0 [1], 189.0 [2]
(2S)-2-[[(3S)-2-[(2S)-2-[2-(1H-Imidazol-5-yl)ethylamino]-3-methylbutanoyl]-3,4-dihydro-1H-isoquinoline-3-carbonyl]amino]-4-methylsulfanylbutanoic acidIC500.79 [1], 0.8 [2]
[(2Z,6E)-3-Ethenyl-7,11-dimethyldodeca-2,6,10-trienyl] phosphono hydrogen phosphateIC50173.0 [1]
6-[alpha-(1-Methyl-5-imidazolyl)-4-cyanobenzyloxymethyl]biphenyl-3-carbonitrileIC501.3 [1], 1318.26 [2]
(1R,5R)-30-Oxo-19-oxa-2,6,10,12-tetrazahexacyclo[18.6.2.12,5.114,18.08,12.023,27]triaconta-8,10,14(29),15,17,20(28),21,23(27)-octaene-17-carbonitrileIC500.02 [1], 1.0 [2]
4'-[[(R)-2-Amino-3-mercaptopropyl]amino]biphenyl-3-carboxylic acidIC50114.0 [1], 150.0 [2]
[1-[[3-(1,3-Benzodioxol-5-ylmethyl)imidazol-4-yl]methyl]-4-naphthalen-1-ylpyrrol-3-yl]-(4-methylpiperazin-1-yl)methanoneIC500.9 [1], 2.4 [2]
(2S)-2-[[2-[[(2S,3R)-2-[[2-[3-[(4-Cyanophenyl)methyl]imidazol-4-yl]acetyl]amino]-3-methylpentyl]-(naphthalen-1-ylmethyl)amino]acetyl]amino]-4-methylsulfanylbutanoic acidIC500.15 [1]
4-[3-(4-Cyanophenyl)-3-hydroxy-3-(3-methylimidazol-4-yl)prop-1-ynyl]-3-(3-ethoxyphenyl)benzonitrileIC500.73 [1]
4-{5-[(1-Benzyl-2-oxo-pyrrolidin-3-ylamino)-methyl]-imidazol-1-ylmethyl}-benzonitrileIC505.7 [1], 29.0 [2]
6-[[(4-Cyano-3-naphthalen-1-ylphenyl)-(3-methylimidazol-4-yl)methoxy]methyl]pyridine-3-carbonitrileIC500.4 [1], 0.73 [2]
(1R,5R)-29-Oxo-19-oxa-2,6,10,12-tetrazahexacyclo[18.5.2.12,5.114,18.08,12.023,26]nonacosa-8,10,14(28),15,17,20(27),21,23(26)-octaene-17-carbonitrileIC500.15 [1], 1.0 [2]
1-[4-[(2S)-13-Chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl]piperazin-1-yl]-2-pyridin-4-ylethanoneIC50140.0 [1]
(5S)-30-Oxo-19-oxa-2,6,10,12-tetrazahexacyclo[18.6.2.12,5.114,18.08,12.023,27]triaconta-1(26),8,10,14(29),15,17,20(28),21,23(27),24-decaene-17-carbonitrileIC503.5 [1]
[(2Z,6E)-3-Tert-butyl-7,11-dimethyldodeca-2,6,10-trienyl] phosphono hydrogen phosphateIC5031.0 [1]
[1-(1H-Imidazol-5-ylmethyl)-7-pyridin-4-yl-3,5-dihydro-2H-1,4-benzodiazepin-4-yl]-[2-(trifluoromethoxy)phenyl]methanoneIC5024.0 [1], 24000.0 [2]
1-[(2R)-2-[(4-Cyanophenyl)methyl-methylamino]-3-(3-methylimidazol-4-yl)propanoyl]-5-naphthalen-1-yl-3,6-dihydro-2H-pyridine-4-carbonitrileIC500.92 [1]
Methyl (2S)-2-[[6-[[(2R)-2-amino-3-sulfanylpropyl]amino]naphthalene-1-carbonyl]amino]-4-methylsulfanylbutanoateIC5080.0 [1], 500.0 [2]
2-[4-(2-Amino-3-mercapto-propylamino)-benzoylamino]-4-methylsulfanyl-butyric acidIC50150.0 [1]
2-[4-(2-Amino-3-mercapto-propylamino)-benzoylamino]-4-methylsulfanyl-butyric acidKi785.0 [1]
1-[4-[(4-Chlorophenyl)-pyridin-2-ylmethyl]piperazin-1-yl]-2-pyridin-3-ylethanoneIC5038300.0 [1]
(R)-2-Amino-3-(biphenyl-4-ylamino)-propane-1-thiolIC501070.0 [1], 1200.0 [2]
(R)-2-Amino-3-[(3'-methyl-1,1'-biphenyl-4-yl)amino]-1-propanethiolIC50710.0 [1], 770.0 [2]
4'-[[(R)-2-Amino-3-mercaptopropyl]amino]biphenyl-3-carboxylic acid methyl esterIC50917.0 [1], 930.0 [2]
7-Bromo-4-(1-naphthylcarbonyl)-1-(1H-imidazole-5-ylmethyl)-2,3,4,5-tetrahydro-1H-1,4-benzodiazepineIC50228.0 [1], 228000.0 [2]
(S)-4-((5-((1-(3-Chlorobenzoyl)pyrrolidin-3-ylamino)methyl)-1H-imidazol-1-yl)methyl)benzonitrileIC5027.0 [1], 67.0 [2]
Tert-butyl N-[3-[[(3S)-1-benzyl-2-oxopyrrolidin-3-yl]-[[3-[(4-cyanophenyl)methyl]imidazol-4-yl]methyl]amino]propyl]carbamateIC5018.0 [1], 65.0 [2]
4-[[5-[[[(3S)-1-Benzyl-2-oxopyrrolidin-3-yl]-(pyridin-3-ylmethyl)amino]methyl]imidazol-1-yl]methyl]benzonitrileIC5052.0 [1], 110.0 [2]
4-(5-{[(1-Benzyl-2-oxo-pyrrolidin-3-yl)-butyl-amino]-methyl}-imidazol-1-ylmethyl)-benzonitrileIC5042.0 [1], 54.0 [2]
4-{5-[2-(2-Oxo-1-phenyl-pyrrolidin-3-ylamino)-ethyl]-imidazol-1-ylmethyl}-benzonitrileIC50150.0 [1], 280.0 [2]
(2S)-4-Methylsulfanyl-2-[[2-phenyl-4-[[3-[(4-phenylphenyl)methyl]imidazol-4-yl]methylamino]benzoyl]amino]butanoic acidIC508.0 [1], 260.0 [2]
1-[4-(13-Chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-ylidene)piperidin-1-yl]-2-pyridin-3-ylethanoneIC50470.0 [1], 600.0 [2]
[4-((R)-2-Amino-3-mercapto-propyl)-3-butyl-piperazin-1-yl]-naphthalen-1-yl-methanoneIC501.0 [1]
1-[4-(13-Chloro-6-methyl-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-ylidene)piperidin-1-yl]-2-pyridin-4-ylethanoneIC5040.0 [1], 60.0 [2]
2-(2-Naphthyloxy)-4-[5-[3-oxo-4-(3-chlorophenyl)piperazinomethyl]-1-imidazolylmethyl]benzonitrileIC5048.0 [1], 1000.0 [2]
(Z)-2-((Z)-Hexadec-7-enyl)-3-methyl-but-2-enedioic acidIC50185.0 [1], 190.0 [2]
4-(6-Bromo-13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl)-1-N-cyclohexyl-2-N-(1,3,4-thiadiazol-2-yl)piperazine-1,2-dicarboxamideIC50490.0 [1], 10000.0 [2]
4-(6-Bromo-13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl)-1-N-cyclohexyl-2-N-[(6-methylpyridin-3-yl)methyl]piperazine-1,2-dicarboxamideIC5061.0 [1], 550.0 [2]
4-[3-(4-Cyanophenyl)-3-hydroxy-3-(3-methylimidazol-4-yl)prop-1-ynyl]-3-(3-methoxyphenyl)benzonitrileIC500.37 [1]
OrhalquinoneIC50410.0 [1]
(2S)-2-[[2-[[(2S,3R)-2-[[(2R)-2-Amino-3-sulfanylpropyl]amino]-3-methylpentyl]-benzylamino]acetyl]amino]-4-methylsulfanylbutanoic acidIC501.2 [1]
4-[[5-[[[(3S)-1-Benzyl-2-oxopyrrolidin-3-yl]-(3-phenylpropyl)amino]methyl]imidazol-1-yl]methyl]benzonitrileIC5015.0 [1], 74.0 [2]
4-[[5-[[3-Aminopropyl-[(3S)-1-benzyl-2-oxopyrrolidin-3-yl]amino]methyl]imidazol-1-yl]methyl]benzonitrileIC5017.0 [1], 1100.0 [2]
4-[5-[[(3S)-1-(4-Pyridyl)-2-oxo-3-pyrrolidinyl]aminomethyl]-1H-imidazole-1-ylmethyl]benzonitrileIC5043.0 [1], 200.0 [2]
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References

This online tool may be cited as follows

MLA

"Quest Database™ Protein farnesyltransferase Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Feb. 2025, https://www.aatbio.com/data-sets/protein-farnesyltransferase-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2025, February 21). Quest Database™ Protein farnesyltransferase Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/protein-farnesyltransferase-inhibitors-ic50-ki.
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