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FK506-binding protein 1A Inhibitors (IC50, Ki)

Structure
▲
▼
Compound Name
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▼
Standard Type
▲
▼
Standard Values (in nM)
▲
▼
SirolimusIC500.45 [1], 0.6 [2], 1.1 [3], 1.6 [4]
SirolimusKi0.2 [1], 0.6 [2]
TacrolimusIC502.3 [1], 2.5 [2], 14.05 [3], 1000.0 [4]
TacrolimusKi0.4 [1]
(S)-3-(Pyridin-3-yl)propyl 1-(3,3-dimethyl-2-oxopentanoyl)pyrrolidine-2-carboxylateIC501240.0 [1]
(S)-3-(Pyridin-3-yl)propyl 1-(3,3-dimethyl-2-oxopentanoyl)pyrrolidine-2-carboxylateKi0.01 [1], 7.5 [2]
2-[3-[(1R)-3-(3,4-Dimethoxyphenyl)-1-[(2S)-1-(3,3-dimethyl-2-oxopentanoyl)piperidine-2-carbonyl]oxypropyl]phenoxy]acetic acidIC5044.0 [1], 114.0 [2], 170.0 [3]
CycloheximideIC503600.0 [1]
CycloheximideKi3400.0 [1]
AscomycinIC502.1 [1]
2-[3-[(1R)-3-(3,4-Dimethoxyphenyl)-1-[(2S)-1-[(2S)-2-(3,4,5-trimethoxyphenyl)butanoyl]piperidine-2-carbonyl]oxypropyl]phenoxy]acetic acidIC501.8 [1]
1,3-Diphenyl-1-propyl-1-(3,3-dimethyl-1,2-dioxypentyl)-2-piperidine carboxylateKi10.0 [1]
2-[3-[(1R)-3-(3,4-Dimethoxyphenyl)-1-[(2S)-1-[(2S)-2-phenylbutanoyl]piperidine-2-carbonyl]oxypropyl]phenoxy]acetic acidIC5040.0 [1]
2-[3-[(1R)-3-(3,4-Dimethoxyphenyl)-1-[(2S)-1-(2-phenylacetyl)piperidine-2-carbonyl]oxypropyl]phenoxy]acetic acidIC501530.0 [1]
3-(3,4,5-Trimethoxyphenyl)propyl (2s)-1-(Benzylsulfonyl)piperidine-2-CarboxylateIC50200.0 [1]
3-(3,4,5-Trimethoxyphenyl)propyl (2s)-1-(Benzylsulfonyl)piperidine-2-CarboxylateKi230.0 [1]
(1-Phenyl-7-pyridin-3-ylheptan-4-yl) (2S)-1-[2,2-difluoro-2-(3,4,5-trimethoxyphenyl)acetyl]piperidine-2-carboxylateKi19.0 [1]
(S)-1-(3,3-Dimethyl-2-oxo-pentanoyl)-piperidine-2-carboxylic acid 3-pyridin-3-yl-propyl esterIC502110.0 [1]
(S)-1-(3,3-Dimethyl-2-oxo-pentanoyl)-piperidine-2-carboxylic acid 3-pyridin-3-yl-propyl esterKi165.0 [1]
(2S)-1-(3,3-Dimethyl-2-oxopentanoyl)-N-(3-phenylpropyl)pyrrolidine-2-carboxamideKi1.0 [1], 1100.0 [2]
4-[(1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-1,14-Dihydroxy-12-[(E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-2,3,10,16-tetraoxo-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-en-17-yl]-N-(2-pyridin-2-ylethyl)butanamideIC5014.3 [1], 849.8 [2]
(1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-1,14-Dihydroxy-12-[(E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-17-[4-(3-morpholin-4-ylazetidin-1-yl)-4-oxobutyl]-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetroneIC509.52 [1], 1077.0 [2]
4-[(1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-1,14-Dihydroxy-12-[(E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-2,3,10,16-tetraoxo-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-en-17-yl]-N,N-bis(2-hydroxyethyl)butanamideIC5013.39 [1], 988.6 [2]
(1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-1,14-Dihydroxy-12-[(E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-17-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetroneIC5012.61 [1], 1098.0 [2]
(1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-1,14-Dihydroxy-12-[(E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-17-[4-oxo-4-[4-(pyridin-2-ylmethyl)piperazin-1-yl]butyl]-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetroneIC5011.19 [1], 1291.0 [2]
(1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-1,14-Dihydroxy-17-[4-(3-hydroxyazetidin-1-yl)-4-oxobutyl]-12-[(E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetroneIC5012.48 [1], 1111.0 [2]
4-[(1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-1,14-Dihydroxy-12-[(E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-2,3,10,16-tetraoxo-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-en-17-yl]-N-(2-morpholin-4-ylethyl)butanamideIC5011.48 [1], 824.0 [2]
[(1R,2R,4R)-4-[(E)-2-[(1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-17-Ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-2,3,10,16-tetraoxo-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-en-12-yl]prop-1-enyl]-2-methoxycyclohexyl] 4-methylpiperazine-1-carboxylateIC5010.99 [1], 1735.0 [2]
(1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-1,14-Dihydroxy-12-[(E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-17-[(E)-6-oxo-6-piperazin-1-ylhex-1-enyl]-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetroneIC5012.59 [1], 1808.0 [2]
5-[[3-[(2S)-1-(4,4-Dimethyl-2-oxopentanoyl)piperidine-2-carbonyl]oxy-6-phenylhexyl]carbamothioylamino]-2-(3-hydroxy-6-oxoxanthen-9-yl)benzoic acidIC50250.0 [1]
5-[[3-[(2S)-1-(4,4-Dimethyl-2-oxopentanoyl)piperidine-2-carbonyl]oxy-6-phenylhexyl]carbamothioylamino]-2-(3-hydroxy-6-oxoxanthen-9-yl)benzoic acidKi32.0 [1]
2-(3-Hydroxy-6-oxoxanthen-9-yl)-5-[4-[(2S)-1-[2-oxo-2-(3,4,5-trimethoxyphenyl)acetyl]piperidine-2-carbonyl]oxybutylcarbamothioylamino]benzoic acidIC50410.0 [1]
2-(3-Hydroxy-6-oxoxanthen-9-yl)-5-[4-[(2S)-1-[2-oxo-2-(3,4,5-trimethoxyphenyl)acetyl]piperidine-2-carbonyl]oxybutylcarbamothioylamino]benzoic acidKi526.0 [1]
5-[3-[(2S)-1-(4,4-Dimethyl-2-oxopentanoyl)piperidine-2-carbonyl]oxypropylcarbamothioylamino]-2-(3-hydroxy-6-oxoxanthen-9-yl)benzoic acidIC50980.0 [1]
5-[3-[(2S)-1-(4,4-Dimethyl-2-oxopentanoyl)piperidine-2-carbonyl]oxypropylcarbamothioylamino]-2-(3-hydroxy-6-oxoxanthen-9-yl)benzoic acidKi482.0 [1]
5-[3-[(2S)-1-(3,3-Dimethyl-2-oxopentanoyl)pyrrolidine-2-carbonyl]oxypropylcarbamothioylamino]-2-(3-hydroxy-6-oxoxanthen-9-yl)benzoic acidIC501650.0 [1]
5-[3-[(2S)-1-(3,3-Dimethyl-2-oxopentanoyl)pyrrolidine-2-carbonyl]oxypropylcarbamothioylamino]-2-(3-hydroxy-6-oxoxanthen-9-yl)benzoic acidKi1300.0 [1]
(1R,9S,12S,13R,14S,17R,18E,21R,23S,24R,25S,27R)-17-Ethyl-1,14,20-trihydroxy-12-[(E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetroneIC506.8 [1], 1314.0 [2]
Benzyl (2S)-1-[2-[(1S,2R,5R)-1-hydroxy-2-methyl-5-propan-2-ylcyclohexyl]-2-oxoacetyl]piperidine-2-carboxylateKi210.0 [1], 210000.0 [2]
Cyclosporin AKi20.0 [1]
BiricodarIC5017.0 [1]
(1R,9S,12S,13R,14S,17R,18Z,20S,21S,23S,24R,25S,27R)-17-Ethyl-1,14,20-trihydroxy-12-[(E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetroneKi0.7 [1]
TimcodarIC50100000.0 [1]
N~1~-Phenyl-N~2~-(2-phenylethyl)pyrrolidine-1,2-dicarboxamideKi30000.0 [1]
1-(Toluene-4-sulfonyl)-pyrrolidine-2-carboxylic acid phenethyl-amideKi33000.0 [1]
Pyrrolidine-1,2-dicarboxylic acid 2-butylamide 1-cyclohexylamideKi50000.0 [1]
N-(2-Phenylethyl)-1-(phenylsulfonyl)prolinamideKi37000.0 [1]
1-N-Benzyl-2-N-(2-phenylethyl)pyrrolidine-1,2-dicarboxamideKi30000.0 [1]
(2E,4S,6R,7S,9R,10R,18S,21S,24R,25E,27S,28R,30R,32S)-10,27-Dihydroxy-21-[1-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]propan-2-yl]-4,7,28-trimethoxy-3,9,24,26,30,32-hexamethyl-36-phenyl-20,41-dioxa-13,34,36,38-tetrazapentacyclo[31.5.2.16,10.013,18.034,38]hentetraconta-2,25,39-triene-11,12,19,23,29,35,37-heptoneKi12.0 [1]
1,7-Diphenylheptan-4-yl (2S)-1-[[(2R)-1-phenyl-3-phosphonooxypropan-2-yl]carbamoyl]piperidine-2-carboxylateKi137000.0 [1]
1-(Phenylglyoxyloyl)piperidine-2-carboxylic acid 3-(3-pyridinyl)propyl esterKi725.0 [1]
1-(3,3-Dimethyl-2-oxo-pentanoyl)-pyrrolidine-2-carboxylic acid 3-pyridin-3-yl-propyl esterKi7.5 [1]
SAFit1Ki90.0 [1]
(1S,5S,6R)-10-(3,5-Dichlorophenyl)sulfonyl-3-[2-(3,4-dimethoxyphenoxy)ethyl]-5-ethenyl-3,10-diazabicyclo[4.3.1]decan-2-oneKi8.8 [1]
Ethyl 2-[4-[(2R)-2-[(1S,3S,5S)-3,5-dimethyl-2-oxocyclohexyl]-2-hydroxyethyl]-2,6-dioxopiperidin-1-yl]acetateIC504400.0 [1]
6-Methoxy-17-piperidin-1-ylsulfonyl-11,17-diazatetracyclo[11.3.1.02,11.03,8]heptadeca-3(8),4,6-trien-12-oneKi360.0 [1]
17-[(2S,6R)-2,6-Dimethylmorpholin-4-yl]sulfonyl-6-methoxy-11,17-diazatetracyclo[11.3.1.02,11.03,8]heptadeca-3(8),4,6-trien-12-oneKi123.0 [1]
6-Methoxy-N-(6-morpholin-4-ylpyridin-3-yl)-12-oxo-11,17-diazatetracyclo[11.3.1.02,11.03,8]heptadeca-3(8),4,6-triene-17-sulfonamideKi591.0 [1]
(2S)-1-(3,3-Dimethyl-2-oxopentanoyl)-N-(3,3-diphenylpropyl)piperidine-2-carboxamideKi420.0 [1]
6-Methoxy-12-oxo-N-(2,4,5-trifluorophenyl)-11,17-diazatetracyclo[11.3.1.02,11.03,8]heptadeca-3(8),4,6-triene-17-sulfonamideKi590.0 [1]
S-(2-Phenylethyl) (2S)-1-(3,3-dimethyl-2-oxopentanoyl)pyrrolidine-2-carbothioateKi12.2 [1]
4,6-Dimethoxy-17-(3-methylphenyl)sulfonyl-11,17-diazatetracyclo[11.3.1.02,11.03,8]heptadeca-3(8),4,6-trien-12-oneKi104.0 [1]
6-Methoxy-N-(6-methoxypyridin-3-yl)-12-oxo-11,17-diazatetracyclo[11.3.1.02,11.03,8]heptadeca-3(8),4,6-triene-17-sulfonamideKi210.0 [1]
N-(3,4-Difluorophenyl)-6-methoxy-12-oxo-11,17-diazatetracyclo[11.3.1.02,11.03,8]heptadeca-3(8),4,6-triene-17-sulfonamideKi150.0 [1]
S-(3-Pyridin-3-ylpropyl) (2S)-1-(3,3-dimethyl-2-oxopentanoyl)pyrrolidine-2-carbothioateKi8.7 [1]
N-(6-Chloropyridin-3-yl)-6-methoxy-12-oxo-11,17-diazatetracyclo[11.3.1.02,11.03,8]heptadeca-3(8),4,6-triene-17-sulfonamideKi360.0 [1]
4-[(4,6-Dimethoxy-12-oxo-11,17-diazatetracyclo[11.3.1.02,11.03,8]heptadeca-3(8),4,6-trien-17-yl)sulfonyl]benzonitrileKi82.0 [1]
1-(2-Oxo-propionyl)-piperidine-2-carboxylic acid ethyl esterKi10000.0 [1]
4,6-Dimethoxy-17-(4-phenylphenyl)sulfonyl-11,17-diazatetracyclo[11.3.1.02,11.03,8]heptadeca-3(8),4,6-trien-12-oneKi88.0 [1]
17-(4-Bromophenyl)sulfonyl-4,6-dimethoxy-11,17-diazatetracyclo[11.3.1.02,11.03,8]heptadeca-3(8),4,6-trien-12-oneKi92.0 [1]
(1R,9S,12S,13R,17R,18E,21S,23S,24R,25S,27R)-17-Ethyl-1-hydroxy-12-[(E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetroneIC500.77 [1]
4,6-Dimethoxy-17-(4-methylphenyl)sulfonyl-11,17-diazatetracyclo[11.3.1.02,11.03,8]heptadeca-3(8),4,6-trien-12-oneKi84.0 [1]
6-Methoxy-12-oxo-N-(3,4,5-trimethoxyphenyl)-11,17-diazatetracyclo[11.3.1.02,11.03,8]heptadeca-3(8),4,6-triene-17-sulfonamideKi640.0 [1]
17-[4-(3,4-Dichlorophenyl)phenyl]sulfonyl-4,6-dimethoxy-11,17-diazatetracyclo[11.3.1.02,11.03,8]heptadeca-3(8),4,6-trien-12-oneKi156.0 [1]
(2S)-1-[[(1-Methylcyclohexyl)methyl]aminocarbonyl]piperidine-2-carboxylic acid benzyl esterKi550.0 [1]
2-[(1R,2R)-4-[(E)-2-[(1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-17-Ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-2,3,10,16-tetraoxo-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-en-12-yl]prop-1-enyl]-2-methoxycyclohexyl]oxy-N-methyl-N-phenylacetamideIC502.9 [1]
2-[(1R,2R)-4-[(E)-2-[(1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-17-Ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-2,3,10,16-tetraoxo-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-en-12-yl]prop-1-enyl]-2-methoxycyclohexyl]oxyacetamideIC500.6 [1]
S-(3-Phenylpropyl) (2S)-1-(3,3-dimethyl-2-oxopentanoyl)pyrrolidine-2-carbothioateKi11.0 [1]
2-[3-[(1R)-1-[(2S)-1-[(2S)-2-Cyclohexyl-2-phenylacetyl]piperidine-2-carbonyl]oxy-3-(3,4-dimethoxyphenyl)propyl]phenoxy]acetic acidKi900.0 [1]
1-Benzyl-4-[(2R)-2-[(1S,3S,5S)-3,5-dimethyl-2-oxocyclohexyl]-2-hydroxyethyl]piperidine-2,6-dioneIC50116700.0 [1]
(2S)-1-(Neopentylaminocarbonyl)piperidine-2-carboxylic acid (R)-1,3-diphenylpropyl esterKi350.0 [1]
Methyl (4aS,8S)-1-oxo-2-propyl-4,4a,5,6,7,8-hexahydro-3H-pyrido[1,2-c]pyrimidine-8-carboxylateKi83000.0 [1]
(1R,9S,12S,13R,14E,17R,18E,21S,23S,24R,25S,27R)-17-Ethyl-1-hydroxy-12-[(E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacosa-14,18-diene-2,3,10,16-tetroneIC50529.0 [1]
(2S)-1-[[(1-Methylcyclopentyl)methyl]aminocarbonyl]piperidine-2-carboxylic acid benzyl esterKi570.0 [1]
Benzyl (4aS,8S)-2-benzyl-1-oxo-4,4a,5,6,7,8-hexahydro-3H-pyrido[1,2-c]pyrimidine-8-carboxylateKi14000.0 [1]
3-(3,4,5-Trimethoxyphenyl)propyl (2S)-1-(2,2-dimethylpropylcarbamoyl)piperidine-2-carboxylateKi390.0 [1]
(2S)-1-(Neopentylaminocarbonyl)piperidine-2-carboxylic acid benzyl esterKi790.0 [1]
2-[4-[(2R)-2-[(1S,3S,5S)-3,5-Dimethyl-2-oxocyclohexyl]-2-hydroxyethyl]-2,6-dioxopiperidin-1-yl]acetamideIC5021600.0 [1]
(2S)-1-(Neopentylaminocarbonyl)piperidine-2-carboxylic acid 3-(3-methoxyphenyl)propyl esterKi370.0 [1]
4-[(2R)-2-[(1S,3S,5S)-3,5-Dimethyl-2-oxocyclohexyl]-2-hydroxyethyl]-1-methylpiperidine-2,6-dioneIC50124100.0 [1]
Cycloheximide acetateIC50200000.0 [1]
(2S)-1-(Benzylaminocarbonyl)piperidine-2-carboxylic acid benzyl esterKi6500.0 [1]
(2S)-1-(Neopentylaminocarbonyl)piperidine-2-carboxylic acid 4-phenylbutyl esterKi150.0 [1]
Ethyl 4-[4-[(2R)-2-[(1S,3S,5S)-3,5-dimethyl-2-oxocyclohexyl]-2-hydroxyethyl]-2,6-dioxopiperidin-1-yl]butanoateIC5022300.0 [1]
Ethyl 1-(phenylsulfonyl)piperidine-2-carboxylateIC503100.0 [1]
(2S)-1-[(2-Methyl-2-propenyl)aminocarbonyl]piperidine-2-carboxylic acid benzyl esterKi7200.0 [1]
(2S)-1-(Neopentylaminocarbonyl)piperidine-2-carboxylic acid 3-phenoxybenzyl esterKi220.0 [1]
Methyl (4aS,8S)-2-benzyl-1-oxo-4,4a,5,6,7,8-hexahydro-3H-pyrido[1,2-c]pyrimidine-8-carboxylateKi67000.0 [1]
Benzyl (4aS,8S)-1-oxo-2-propyl-4,4a,5,6,7,8-hexahydro-3H-pyrido[1,2-c]pyrimidine-8-carboxylateKi24000.0 [1]
(3-Phenoxyphenyl)methyl (2S)-1-[(1-methylcyclohexyl)methylcarbamoyl]piperidine-2-carboxylateKi200.0 [1]
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References

This online tool may be cited as follows

MLA

"Quest Database™ FK506-binding protein 1A Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 20 Feb. 2025, https://www.aatbio.com/data-sets/fk506-binding-protein-1a-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2025, February 20). Quest Database™ FK506-binding protein 1A Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/fk506-binding-protein-1a-inhibitors-ic50-ki.
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