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TargetCathepsin K(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50098576(5-(2-MORPHOLIN-4-YLETHOXY)BENZOFURAN-2-CARBOXYLIC ...)
Affinity DataKi:  0.00480nMAssay Description:Inhibition of Human cathepsin KMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetCathepsin K(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM19770((2S)-2-(1-benzofuran-2-ylformamido)-4-methyl-N-[(4...)
Affinity DataKi:  0.00990nM ΔG°:  -62.2kJ/molepH: 5.5 T: 2°CAssay Description:Potential inhibitors were evaluated using the progress curve method. Assays were carried out in the presence of variable concentrations of test compo...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/5/2008
Entry Details Article
PubMed
TargetRAC-alpha serine/threonine-protein kinase(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50278693((+/-)-N-(1-amino-3-phenylpropan-2-yl)-4-bromo-5-(1...)
Affinity DataKi:  0.0400nMAssay Description:Inhibition of AKT1More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetProcathepsin L(Human)
Gsk

LigandPNGBDBM19770((2S)-2-(1-benzofuran-2-ylformamido)-4-methyl-N-[(4...)
Affinity DataKi:  0.0400nM ΔG°:  -58.8kJ/molepH: 5.5 T: 2°CAssay Description:Potential inhibitors were evaluated using the progress curve method. Assays were carried out in the presence of variable concentrations of test compo...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/5/2008
Entry Details Article
PubMed
TargetCathepsin K(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM19778((2S)-2-(1-benzofuran-2-ylformamido)-4-methyl-N-[(4...)
Affinity DataKi:  0.0410nM ΔG°:  -58.7kJ/molepH: 5.5 T: 2°CAssay Description:Potential inhibitors were evaluated using the progress curve method. Assays were carried out in the presence of variable concentrations of test compo...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/5/2008
Entry Details Article
PubMed
TargetRAC-alpha serine/threonine-protein kinase(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50278098(N-((S)-1-amino-3-(2-(trifluoromethyl)phenyl)propan...)
Affinity DataKi:  0.0500nMAssay Description:Inhibition of AKT1More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetRAC-alpha serine/threonine-protein kinase(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50278837(N-((S)-1-amino-3-(4-fluorophenyl)propan-2-yl)-4-br...)
Affinity DataKi:  0.0600nMAssay Description:Inhibition of AKT1More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetCathepsin L2(Human)
Gsk

LigandPNGBDBM19778((2S)-2-(1-benzofuran-2-ylformamido)-4-methyl-N-[(4...)
Affinity DataKi:  0.0630nMAssay Description:Potential inhibitors were evaluated using the progress curve method. Assays were carried out in the presence of variable concentrations of test compo...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/5/2008
Entry Details Article
PubMed
TargetProcathepsin L(Human)
Gsk

LigandPNGBDBM19778((2S)-2-(1-benzofuran-2-ylformamido)-4-methyl-N-[(4...)
Affinity DataKi:  0.0680nM ΔG°:  -57.4kJ/molepH: 5.5 T: 2°CAssay Description:Potential inhibitors were evaluated using the progress curve method. Assays were carried out in the presence of variable concentrations of test compo...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/5/2008
Entry Details Article
PubMed
TargetRAC-alpha serine/threonine-protein kinase(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50278099(N-((S)-1-amino-3-(3-(trifluoromethyl)phenyl)propan...)
Affinity DataKi:  0.100nMAssay Description:Inhibition of AKT1More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetRAC-alpha serine/threonine-protein kinase(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50278099(N-((S)-1-amino-3-(3-(trifluoromethyl)phenyl)propan...)
Affinity DataKi:  0.100nMAssay Description:Inhibition of AKT1More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetCathepsin K(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM19775((2S)-2-(1-benzofuran-2-ylformamido)-4-methyl-N-[(4...)
Affinity DataKi:  0.140nM ΔG°:  -55.7kJ/molepH: 5.5 T: 2°CAssay Description:Potential inhibitors were evaluated using the progress curve method. Assays were carried out in the presence of variable concentrations of test compo...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/5/2008
Entry Details Article
PubMed
TargetCathepsin K(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM19769(CHEMBL286364 | (2S)-2-(1-benzofuran-2-ylformamido)...)
Affinity DataKi:  0.160nM ΔG°:  -55.3kJ/molepH: 5.5 T: 2°CAssay Description:Potential inhibitors were evaluated using the progress curve method. Assays were carried out in the presence of variable concentrations of test compo...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/5/2008
Entry Details Article
PubMed
TargetCathepsin K(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM19769(CHEMBL286364 | (2S)-2-(1-benzofuran-2-ylformamido)...)
Affinity DataKi:  0.160nMAssay Description:Inhibition of Human cathepsin KMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetCathepsin K(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM19769(CHEMBL286364 | (2S)-2-(1-benzofuran-2-ylformamido)...)
Affinity DataKi:  0.160nMAssay Description:Apparent inhibitory constant against human cathepsin KMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetCathepsin S(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50084650({1-[1-Formyl-2-(4-hydroxy-phenyl)-ethylcarbamoyl]-...)
Affinity DataKi:  0.260nMAssay Description:Apparent inhibitory constant against human cathepsin SMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetProcathepsin L(Human)
Gsk

LigandPNGBDBM50002402(CHEMBL194643)
Affinity DataKi:  0.430nMAssay Description:Apparent inhibitory constant against human cathepsin LMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetProcathepsin L(Human)
Gsk

LigandPNGBDBM50084650({1-[1-Formyl-2-(4-hydroxy-phenyl)-ethylcarbamoyl]-...)
Affinity DataKi:  0.470nMAssay Description:Apparent inhibitory constant against human cathepsin LMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetProcathepsin L(Human)
Gsk

LigandPNGBDBM50098576(5-(2-MORPHOLIN-4-YLETHOXY)BENZOFURAN-2-CARBOXYLIC ...)
Affinity DataKi:  0.490nMAssay Description:Inhibitory activity against Human cathepsin LMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetCathepsin S(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50349197(CHEMBL1807647)
Affinity DataIC50: 0.5nMAssay Description:Inhibition of human recombinant cathepsin S using Ac-KQLR-AMC as substrate by fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2012
Entry Details Article
PubMed
TargetCathepsin S(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50349203(CHEMBL1807698)
Affinity DataIC50: 0.5nMAssay Description:Inhibition of human recombinant cathepsin S using Ac-KQLR-AMC as substrate by fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2012
Entry Details Article
PubMed
TargetCathepsin K(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50066647({3-Methyl-1-[3-oxo-1-(4-phenoxy-benzenesulfonyl)-p...)
Affinity DataKi:  0.5nMAssay Description:Inhibition of cathepsin KMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetProcathepsin L(Human)
Gsk

LigandPNGBDBM50349198(CHEMBL1807649)
Affinity DataIC50: 0.530nMAssay Description:Inhibition of human recombinant cathepsin L using Z-LR-AMC as substrate by fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2012
Entry Details Article
PubMed
TargetCathepsin S(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50002399(CHEMBL197958)
Affinity DataKi:  0.560nMAssay Description:Apparent inhibitory constant against human cathepsin SMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetProcathepsin L(Human)
Gsk

LigandPNGBDBM50002374(CHEMBL194861)
Affinity DataKi:  0.570nMAssay Description:Apparent inhibitory constant against human cathepsin LMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetCathepsin S(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50349205(CHEMBL1807700)
Affinity DataIC50: 0.580nMAssay Description:Inhibition of human recombinant cathepsin S using Ac-KQLR-AMC as substrate by fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2012
Entry Details Article
PubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Human)
Smithkline Beecham Pharmaceuticals

LigandPNGBDBM36608(Rapamycin C-7, analog 1)
Affinity DataKi:  0.600nM EC50:  1nMAssay Description:FKBP12 assay using rapamycin analogs.More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/15/2011
Entry Details Article
PubMed
TargetRAC-beta serine/threonine-protein kinase(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50278836(N-((S)-1-amino-3-(3-fluorophenyl)propan-2-yl)-4-br...)
Affinity DataKi:  0.630nMAssay Description:Inhibition of AKT2More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetProcathepsin L(Human)
Gsk

LigandPNGBDBM19775((2S)-2-(1-benzofuran-2-ylformamido)-4-methyl-N-[(4...)
Affinity DataKi:  0.630nM ΔG°:  -52.0kJ/molepH: 5.5 T: 2°CAssay Description:Potential inhibitors were evaluated using the progress curve method. Assays were carried out in the presence of variable concentrations of test compo...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/5/2008
Entry Details Article
PubMed
TargetCathepsin K(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50084650({1-[1-Formyl-2-(4-hydroxy-phenyl)-ethylcarbamoyl]-...)
Affinity DataKi:  0.740nMAssay Description:Apparent inhibitory constant against human cathepsin KMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetCathepsin S(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50349196(CHEMBL1807646)
Affinity DataIC50: 0.760nMAssay Description:Inhibition of human recombinant cathepsin S using Ac-KQLR-AMC as substrate by fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2012
Entry Details Article
PubMed
TargetRAC-alpha serine/threonine-protein kinase(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50306095((S)-1-(6-fluoro-1H-indol-3-yl)-3-(6-(furan-3-yl)-5...)
Affinity DataIC50: 0.800nMAssay Description:Inhibition of full length AKT1More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2010
Entry Details Article
PubMed
TargetRAC-alpha serine/threonine-protein kinase(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50306097((2S)-1-(1H-indol-3-yl)-3-(5-(3-methyl-1H-indazol-5...)
Affinity DataIC50: 0.800nMAssay Description:Inhibition of full length AKT1More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2010
Entry Details Article
PubMed
TargetProcathepsin L(Human)
Gsk

LigandPNGBDBM50002399(CHEMBL197958)
Affinity DataKi:  0.870nMAssay Description:Apparent inhibitory constant against human cathepsin LMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetCathepsin K(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50002366(CHEMBL433985)
Affinity DataKi:  0.890nMAssay Description:Apparent inhibitory constant against human cathepsin KMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetRAC-gamma serine/threonine-protein kinase(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50306165(3-((2S)-2-amino-3-(2-amino-5-(3-methyl-1H-pyrazolo...)
Affinity DataIC50: 1nMAssay Description:Inhibition of human AKT3More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2010
Entry Details Article
PubMed
TargetRAC-alpha serine/threonine-protein kinase(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50278693((+/-)-N-(1-amino-3-phenylpropan-2-yl)-4-bromo-5-(1...)
Affinity DataIC50: 1nMAssay Description:Inhibition of AKT1More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetRAC-alpha serine/threonine-protein kinase(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50306165(3-((2S)-2-amino-3-(2-amino-5-(3-methyl-1H-pyrazolo...)
Affinity DataIC50: 1nMAssay Description:Inhibition of human AKT1More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2010
Entry Details Article
PubMed
TargetRibosomal protein S6 kinase alpha-5(Human)
Glaxosmithkline

LigandPNGBDBM24994(4-[1-ethyl-7-(piperidin-4-ylmethoxy)-1H-imidazo[4,...)
Affinity DataIC50: 1nMAssay Description:IC50 is the inhibitor concentration, which inhibits 50% of kinase activity that catalyzes the transfer of the terminal phosphate from radiolabeled AT...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/25/2008
Entry Details Article
PubMed
TargetRAC-gamma serine/threonine-protein kinase(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50305878((S)-1-(6-(furan-3-yl)-5-(3-methyl-1H-indazol-5-yl)...)
Affinity DataIC50: 1nMAssay Description:Inhibition of AKT3More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2010
Entry Details Article
PubMed
TargetCathepsin K(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50349198(CHEMBL1807649)
Affinity DataIC50: 1nMAssay Description:Inhibition of human recombinant cathepsin K using z-LR-AFC as substrate by fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2012
Entry Details Article
PubMed
TargetRAC-alpha serine/threonine-protein kinase(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50278771(N-((S)-1-amino-3-cyclohexylpropan-2-yl)-4-bromo-5-...)
Affinity DataIC50: 1nMAssay Description:Inhibition of AKT1More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetRAC-alpha serine/threonine-protein kinase(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50278770(N-((S)-1-amino-3-phenylpropan-2-yl)-4-bromo-5-(1H-...)
Affinity DataIC50: 1nMAssay Description:Inhibition of AKT1More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetRAC-gamma serine/threonine-protein kinase(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50305883((S)-1-(6-(furan-3-yl)-5-(3-methyl-1H-pyrazolo[3,4-...)
Affinity DataIC50: 1nMAssay Description:Inhibition of AKT3More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2010
Entry Details Article
PubMed
TargetRAC-alpha serine/threonine-protein kinase(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50306154((2S)-1-(1H-indol-3-yl)-3-(5-(3-methyl-1H-pyrazolo[...)
Affinity DataIC50: 1nMAssay Description:Inhibition of human AKT1More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2010
Entry Details Article
PubMed
TargetRAC-alpha serine/threonine-protein kinase(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50278836(N-((S)-1-amino-3-(3-fluorophenyl)propan-2-yl)-4-br...)
Affinity DataIC50: 1nMAssay Description:Inhibition of AKT1More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetRAC-alpha serine/threonine-protein kinase(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50278835(N-((S)-1-amino-3-(2-fluorophenyl)propan-2-yl)-4-br...)
Affinity DataIC50: 1nMAssay Description:Inhibition of AKT1More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetRAC-alpha serine/threonine-protein kinase(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50278770(N-((S)-1-amino-3-phenylpropan-2-yl)-4-bromo-5-(1H-...)
Affinity DataIC50: 1nMAssay Description:Inhibition of AKT1More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetRAC-gamma serine/threonine-protein kinase(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50306155(3-((S)-2-amino-3-(1H-indol-3-yl)propoxy)-5-(3-meth...)
Affinity DataIC50: 1nMAssay Description:Inhibition of human AKT3More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2010
Entry Details Article
PubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Human)
Smithkline Beecham Pharmaceuticals

LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataKi:  1nM EC50:  30nMAssay Description:FKBP12 assay using rapamycin analogs.More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/15/2011
Entry Details Article
PubMed
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