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Found 853 with Last Name = 'janson' and Initial = 'ca'
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
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17355(1,2,4-Triazole Compound, 13 | 5-(benzylsulfanyl)-N...)
Affinity DataKi:  0.0400nM ΔG°:  -58.8kJ/molepH: 7.5 T: 2°CAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...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
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17428(1,2,4-Triazole Compound, 86 | N-[5-(benzylsulfanyl...)
Affinity DataKi:  0.0400nMAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More 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
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17388(1,2,4-Triazole Compound, 46 | 5-(benzylsulfanyl)-N...)
Affinity DataKi:  0.0500nMAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More 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
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17365(1,2,4-Triazole Compound, 23 | 5-(benzylsulfanyl)-N...)
Affinity DataKi:  0.0700nM ΔG°:  -57.4kJ/molepH: 7.5 T: 2°CAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThymidylate synthase(Homo sapiens (Human))
Agouron Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50046660(2-[4-(2-Amino-6-methyl-4-oxo-3,4-dihydro-quinazoli...)
Affinity DataKi:  0.124nMAssay Description:Compound was tested for TS activity against human Thymidylate synthase by tight binding kineticsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17390(1,2,4-Triazole Compound, 48 | 5-{[(2-fluorophenyl)...)
Affinity DataKi:  0.130nMAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More 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
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17362(1,2,4-Triazole Compound, 20 | 5-[(3-methylbut-2-en...)
Affinity DataKi:  0.150nM ΔG°:  -55.5kJ/molepH: 7.5 T: 2°CAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...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:  0.160nM 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
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17395(1,2,4-Triazole Compound, 53 | N-(4-methoxyphenyl)-...)
Affinity DataKi:  0.160nMAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17358(1,2,4-Triazole Compound, 16 | 5-{[(2-fluorophenyl)...)
Affinity DataKi:  0.230nM ΔG°:  -54.5kJ/molepH: 7.5 T: 2°CAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17430(1,2,4-Triazole Compound, 88 | N-(5-{[(2-fluorophen...)
Affinity DataKi:  0.300nMAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17411(1,2,4-Triazole Compound, 69 | methyl 4-[(5-{[(2-fl...)
Affinity DataKi:  0.410nMAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17377(1,2,4-Triazole Compound, 35 | 5-(benzylsulfanyl)-N...)
Affinity DataKi:  0.430nMAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More 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
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17352(1,2,4-Triazole Compound, 6 | 5-(benzylsulfanyl)-N-...)
Affinity DataKi:  0.5nM ΔG°:  -52.6kJ/molepH: 7.5 T: 2°CAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17416(1,2,4-Triazole Compound, 74 | methyl 4-({5-[(3-met...)
Affinity DataKi:  0.5nMAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
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
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17431(1,2,4-Triazole Compound, 89 | N-(5-{[(3,4-difluoro...)
Affinity DataKi:  0.5nMAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17385(1,2,4-Triazole Compound, 43 | N-(4-chlorophenyl)-5...)
Affinity DataKi:  0.520nMAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin K(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM19808(benzyl N-[(1S)-1-({1-[(2S)-2-{[(benzyloxy)carbonyl...)
Affinity DataKi:  0.600nM ΔG°:  -52.1kJ/molepH: 5.5 T: 2°CAssay Description:Assays were carried out in the presence of variable concentrations of test compound. Reactions were initiated by addition of enzyme to buffered solut...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17380(1,2,4-Triazole Compound, 38 | N-(4-chlorophenyl)-5...)
Affinity DataKi:  0.610nMAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...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
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17368(1,2,4-Triazole Compound, 26 | 5-{[(2-fluorophenyl)...)
Affinity DataKi:  0.650nM ΔG°:  -51.9kJ/molepH: 7.5 T: 2°CAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17408(1,2,4-Triazole Compound, 66 | methyl 4-{[5-(benzyl...)
Affinity DataKi:  0.700nMAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin K(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50408519(CHEMBL115357)
Affinity DataKi:  0.700nMAssay Description:Relative binding affinity was measured for Cathepsin KMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17354(1,2,4-Triazole Compound, 12 | N-phenyl-5-[(thiophe...)
Affinity DataKi:  0.75nM ΔG°:  -51.6kJ/molepH: 7.5 T: 2°CAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17418(1,2,4-Triazole Compound, 76 | methyl 4-[(5-{[(5-me...)
Affinity DataKi:  0.800nMAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin K(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50408522(CHEMBL126820)
Affinity DataKi:  0.800nMAssay Description:Relative binding affinity was measured for Cathepsin KMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17414(1,2,4-Triazole Compound, 72 | methyl 4-({5-[(pyrid...)
Affinity DataKi:  0.900nMAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17413(1,2,4-Triazole Compound, 71 | methyl 4-({5-[(pyrid...)
Affinity DataKi:  0.900nMAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17405(1,2,4-Triazole Compound, 63 | N-(3,4-dimethoxyphen...)
Affinity DataKi:  0.900nMAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin K(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50408520(CHEMBL126352)
Affinity DataKi:  1nMAssay Description:Relative binding affinity was measured for Cathepsin KMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17468(1,2,3-triazole analogue, 24 | 5-(3,4-dibromophenyl...)
Affinity DataKi:  1nM ΔG°:  -50.9kJ/molepH: 7.5 T: 2°CAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17461(1,2,3-triazole analogue, 17 | 5-(4-iodophenyl)-1H-...)
Affinity DataKi:  1nM ΔG°:  -50.9kJ/molepH: 7.5 T: 2°CAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17446((3R,4S,5S,6R)-5-methoxy-4-[(2R,3R)-2-methyl-3-(3-m...)
Affinity DataKi:  1nMAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17442(1,2,4-Triazole Compound, 101 | 5-[(3-methylbut-2-e...)
Affinity DataKi:  1nMAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17373(1,2,4-Triazole Compound, 31 | 5-[(3-methylbut-2-en...)
Affinity DataKi:  1.20nMAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17400(1,2,4-Triazole Compound, 58 | N-(3,4-dimethoxyphen...)
Affinity DataKi:  1.30nMAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17412(1,2,4-Triazole Compound, 70 | methyl 4-[(5-{[(3,4-...)
Affinity DataKi:  1.30nMAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThymidylate synthase(Homo sapiens (Human))
Agouron Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50046665(2-[4-(2,6-Dimethyl-4-oxo-3,4-dihydro-quinazolin-5-...)
Affinity DataKi:  1.31nMAssay Description:Compound was tested for TS activity against human Thymidylate synthase by tight binding kineticsMore 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
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM17436(1,2,4-Triazole Compound, 94 | N-(5-{[(5-methyl-1,2...)
Affinity DataKi:  1.5nMAssay Description:MetAP2 activity was monitored by measuring the initial velocity of turnover of the artificial substrate Met-AMC. Assays were performed in 96-well mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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