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Found 753 with Last Name = 'yamashita' and Initial = 'ds'
TargetCathepsin K(Homo sapiens (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
TargetCathepsin K(Homo sapiens (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 DepthDetails ArticlePubMed
TargetProcathepsin L(Homo sapiens (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 DepthDetails ArticlePubMed
TargetRAC-alpha serine/threonine-protein kinase(Homo sapiens (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 DepthDetails ArticlePubMed
TargetCathepsin K(Homo sapiens (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 DepthDetails ArticlePubMed
TargetRAC-alpha serine/threonine-protein kinase(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50278098(CHEMBL520788 | N-((S)-1-amino-3-(2-(trifluoromethy...)
Affinity DataKi:  0.0500nMAssay Description:Inhibition of AKT1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetRAC-alpha serine/threonine-protein kinase(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50278837(CHEMBL496690 | N-((S)-1-amino-3-(4-fluorophenyl)pr...)
Affinity DataKi:  0.0600nMAssay Description:Inhibition of AKT1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin L2(Homo sapiens (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 DepthDetails ArticlePubMed
TargetProcathepsin L(Homo sapiens (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 DepthDetails ArticlePubMed
TargetRAC-alpha serine/threonine-protein kinase(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50278099(CHEMBL482536 | N-((S)-1-amino-3-(3-(trifluoromethy...)
Affinity DataKi:  0.100nMAssay Description:Inhibition of AKT1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetRAC-alpha serine/threonine-protein kinase(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50278099(CHEMBL482536 | N-((S)-1-amino-3-(3-(trifluoromethy...)
Affinity DataKi:  0.100nMAssay Description:Inhibition of AKT1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin K(Homo sapiens (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 DepthDetails ArticlePubMed
TargetCathepsin K(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM19769((2S)-2-(1-benzofuran-2-ylformamido)-4-methyl-N-[(4...)
Affinity DataKi:  0.160nMAssay Description:Inhibition of Human cathepsin KMore data for this Ligand-Target Pair
TargetCathepsin K(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM19769((2S)-2-(1-benzofuran-2-ylformamido)-4-methyl-N-[(4...)
Affinity DataKi:  0.160nMAssay Description:Apparent inhibitory constant against human cathepsin KMore data for this Ligand-Target Pair
TargetCathepsin K(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM19769((2S)-2-(1-benzofuran-2-ylformamido)-4-methyl-N-[(4...)
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
TargetCathepsin S(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50084650(CHEMBL177914 | {(S)-1-[(S)-1-Formyl-2-(4-hydroxy-p...)
Affinity DataKi:  0.260nMAssay Description:Apparent inhibitory constant against human cathepsin SMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProcathepsin L(Homo sapiens (Human))
Gsk

LigandPNGBDBM50002402(CHEMBL194643)
Affinity DataKi:  0.430nMAssay Description:Apparent inhibitory constant against human cathepsin LMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProcathepsin L(Homo sapiens (Human))
Gsk

LigandPNGBDBM50084650(CHEMBL177914 | {(S)-1-[(S)-1-Formyl-2-(4-hydroxy-p...)
Affinity DataKi:  0.470nMAssay Description:Apparent inhibitory constant against human cathepsin LMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProcathepsin L(Homo sapiens (Human))
Gsk

LigandPNGBDBM50098576(5-(2-MORPHOLIN-4-YLETHOXY)BENZOFURAN-2-CARBOXYLIC ...)
Affinity DataKi:  0.490nMAssay Description:Inhibitory activity of the compound against Human cathepsin LMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin K(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50066647(CHEMBL113724 | {(S)-3-Methyl-1-[3-oxo-1-(4-phenoxy...)
Affinity DataKi:  0.5nMAssay Description:Inhibition of cathepsin KMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (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 DepthDetails ArticlePubMed
TargetProcathepsin L(Homo sapiens (Human))
Gsk

LigandPNGBDBM50002374(CHEMBL194861)
Affinity DataKi:  0.570nMAssay Description:Apparent inhibitory constant against human cathepsin LMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Homo sapiens (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 DepthDetails ArticlePubMed
TargetProcathepsin L(Homo sapiens (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 DepthDetails ArticlePubMed
TargetRAC-beta serine/threonine-protein kinase(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50278836(CHEMBL523586 | N-((S)-1-amino-3-(3-fluorophenyl)pr...)
Affinity DataKi:  0.630nMAssay Description:Inhibition of AKT2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin K(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50084650(CHEMBL177914 | {(S)-1-[(S)-1-Formyl-2-(4-hydroxy-p...)
Affinity DataKi:  0.740nMAssay Description:Apparent inhibitory constant against human cathepsin KMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProcathepsin L(Homo sapiens (Human))
Gsk

LigandPNGBDBM50002399(CHEMBL197958)
Affinity DataKi:  0.870nMAssay Description:Apparent inhibitory constant against human cathepsin LMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin K(Homo sapiens (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 DepthDetails ArticlePubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Homo sapiens (Human))
Smithkline Beecham Pharmaceuticals

LigandPNGBDBM36612(Rapamycin C-7, analog 6a)
Affinity DataKi:  1nM EC50:  4nMAssay Description:FKBP12 assay using rapamycin analogs.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Homo sapiens (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
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Homo sapiens (Human))
Smithkline Beecham Pharmaceuticals

LigandPNGBDBM36623(Rapamycin C-7, analog 12)
Affinity DataKi:  1nM EC50:  2nMAssay Description:FKBP12 assay using rapamycin analogs.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Homo sapiens (Human))
Smithkline Beecham Pharmaceuticals

LigandPNGBDBM36613(Rapamycin C-7, analog 6b)
Affinity DataKi:  1nM EC50:  4nMAssay Description:FKBP12 assay using rapamycin analogs.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Homo sapiens (Human))
Smithkline Beecham Pharmaceuticals

LigandPNGBDBM36627(Rapamycin C-7, analog 16a)
Affinity DataKi:  1nM EC50:  45nMAssay Description:FKBP12 assay using rapamycin analogs.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin K(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM93183(Cathepsin Inhibitor, Column 6 Row 1)
Affinity DataKi:  1.30nMpH: 5.5Assay Description:Inhibitors were assayed against human liver Cathepsin L and B. Inhibitors were also evaluated for inhibition against purified recombinant Cathepsin ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin K(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM19780((2S)-2-(1-benzofuran-2-ylformamido)-4-methyl-N-[(4...)
Affinity DataKi:  1.40nM ΔG°:  -50.0kJ/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 DepthDetails ArticlePubMed
TargetProcathepsin L(Homo sapiens (Human))
Gsk

LigandPNGBDBM50002400(CHEMBL382286)
Affinity DataKi:  1.40nMAssay Description:Apparent inhibitory constant against human cathepsin LMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin K(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM19771((2S)-2-(1-benzofuran-2-ylformamido)-4-methyl-N-[(4...)
Affinity DataKi:  1.5nM ΔG°:  -49.9kJ/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 DepthDetails ArticlePubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Homo sapiens (Human))
Smithkline Beecham Pharmaceuticals

LigandPNGBDBM36622(Rapamycin C-7, analog 11b)
Affinity DataKi:  1.5nM EC50:  70nMAssay Description:FKBP12 assay using rapamycin analogs.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin K(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50098580(Benzofuran-2-carboxylic acid {3-methyl-1-[2-oxo-3-...)
Affinity DataKi:  1.60nMAssay Description:Inhibition of Human cathepsin KMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM19778((2S)-2-(1-benzofuran-2-ylformamido)-4-methyl-N-[(4...)
Affinity DataKi:  1.60nMAssay 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 DepthDetails ArticlePubMed
TargetCathepsin K(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM93180(Cathepsin Inhibitor, Column 5 Row 1)
Affinity DataKi:  1.70nMpH: 5.5Assay Description:Inhibitors were assayed against human liver Cathepsin L and B. Inhibitors were also evaluated for inhibition against purified recombinant Cathepsin ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProcathepsin L(Homo sapiens (Human))
Gsk

LigandPNGBDBM50002367(CHEMBL407633)
Affinity DataKi:  1.70nMAssay Description:Apparent inhibitory constant against human cathepsin LMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin L2(Homo sapiens (Human))
Gsk

LigandPNGBDBM19769((2S)-2-(1-benzofuran-2-ylformamido)-4-methyl-N-[(4...)
Affinity DataKi:  1.80nMAssay 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 DepthDetails ArticlePubMed
TargetRAC-alpha serine/threonine-protein kinase(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50278100(CHEMBL482537 | N-((S)-1-amino-3-(4-(trifluoromethy...)
Affinity DataKi:  2nMAssay Description:Inhibition of AKT1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin K(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50002399(CHEMBL197958)
Affinity DataKi:  2nMAssay Description:Apparent inhibitory constant against human cathepsin KMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetRAC-beta serine/threonine-protein kinase(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50278837(CHEMBL496690 | N-((S)-1-amino-3-(4-fluorophenyl)pr...)
Affinity DataKi:  2nMAssay Description:Inhibition of AKT2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetRAC-alpha serine/threonine-protein kinase(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50278833(CHEMBL498051 | N-((S)-1-amino-3-(pyridin-4-yl)prop...)
Affinity DataKi:  2nMAssay Description:Inhibition of AKT1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin K(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50098584(CHEMBL31947 | {1-[4-(2-Benzyloxycarbonylamino-4-me...)
Affinity DataKi:  2nMAssay Description:Inhibition of Human cathepsin KMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProcathepsin L(Homo sapiens (Human))
Gsk

LigandPNGBDBM19769((2S)-2-(1-benzofuran-2-ylformamido)-4-methyl-N-[(4...)
Affinity DataKi:  2.20nM ΔG°:  -48.9kJ/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 DepthDetails ArticlePubMed
TargetProcathepsin L(Homo sapiens (Human))
Gsk

LigandPNGBDBM19769((2S)-2-(1-benzofuran-2-ylformamido)-4-methyl-N-[(4...)
Affinity DataKi:  2.20nMAssay Description:Apparent inhibitory constant against human cathepsin LMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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