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Found 3760 Enz. Inhib. hit(s) with Target = 'Cathepsin S'
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM19859((2S)-N-(cyanomethyl)-3-cyclohexyl-2-(phenylformami...)
Affinity DataIC50:  5.30nM EC50:  10nMpH: 6.5 T: 2°CAssay Description:Prior to the addition of substrate, different concentrations of the inhibitor ranging from 100 uM to 0.2 nM were preincubated for 15 min with enzyme ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Mus musculus (Mouse))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM19859((2S)-N-(cyanomethyl)-3-cyclohexyl-2-(phenylformami...)
Affinity DataIC50:  13nM EC50:  40nMAssay Description:Prior to the addition of substrate, different concentrations of the inhibitor ranging from 100 uM to 0.2 nM were preincubated for 15 min with enzyme ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50322923(6-(4-(3-(4-methylpiperazin-1-yl)propoxy)-3-(triflu...)
Affinity DataEC50:  138nMAssay Description:Inhibition of cathepsin S in human JY cells assessed as induction of accumulation of lip10More data for this Ligand-Target Pair
TargetCathepsin S(Mus musculus (Mouse))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM19854(CHEMBL426819 | CRA-013783/L-006235 | N-{1-[(cyanom...)
Affinity DataIC50:  5.40E+3nM EC50:  318nMAssay Description:Prior to the addition of substrate, different concentrations of the inhibitor ranging from 100 uM to 0.2 nM were preincubated for 15 min with enzyme ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Mus musculus (Mouse))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM19855(Balicatib | CHEMBL371064 | N-[1-(cyanomethylcarbam...)
Affinity DataIC50:  6.35E+3nM EC50:  480nMAssay Description:Prior to the addition of substrate, different concentrations of the inhibitor ranging from 100 uM to 0.2 nM were preincubated for 15 min with enzyme ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50546794(CHEMBL4777335)
Affinity DataEC50:  580nMAssay Description:Inhibition of Cathepsin S in human Raji cells assessed as increase in Lip10 accumulation after 24 hrs by SDS-PAGE analysisMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetCathepsin S(Mus musculus (Mouse))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM19856((2R)-N-(cyanomethyl)-4-methyl-2-{3-[4-(piperazin-1...)
Affinity DataIC50:  3.41E+4nM EC50:  740nMAssay Description:Prior to the addition of substrate, different concentrations of the inhibitor ranging from 100 uM to 0.2 nM were preincubated for 15 min with enzyme ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM19854(CHEMBL426819 | CRA-013783/L-006235 | N-{1-[(cyanom...)
Affinity DataIC50:  4.70E+4nM EC50:  790nMpH: 6.5 T: 2°CAssay Description:Prior to the addition of substrate, different concentrations of the inhibitor ranging from 100 uM to 0.2 nM were preincubated for 15 min with enzyme ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50546795(CHEMBL4777740)
Affinity DataEC50:  1.10E+3nMAssay Description:Inhibition of Cathepsin S in human Raji cells assessed as increase in Lip10 accumulation after 24 hrs by SDS-PAGE analysisMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM19856((2R)-N-(cyanomethyl)-4-methyl-2-{3-[4-(piperazin-1...)
Affinity DataIC50:  2.00E+4nM EC50:  1.34E+3nMpH: 6.5 T: 2°CAssay Description:Prior to the addition of substrate, different concentrations of the inhibitor ranging from 100 uM to 0.2 nM were preincubated for 15 min with enzyme ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM19855(Balicatib | CHEMBL371064 | N-[1-(cyanomethylcarbam...)
Affinity DataIC50:  6.50E+4nM EC50:  2.90E+3nMpH: 6.5 T: 2°CAssay Description:Prior to the addition of substrate, different concentrations of the inhibitor ranging from 100 uM to 0.2 nM were preincubated for 15 min with enzyme ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM19858(N-{1-[(cyanomethyl)carbamoyl]cyclohexyl}-4-(morpho...)
Affinity DataIC50:  5.20E+4nM EC50:  4.80E+3nMpH: 6.5 T: 2°CAssay Description:Prior to the addition of substrate, different concentrations of the inhibitor ranging from 100 uM to 0.2 nM were preincubated for 15 min with enzyme ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Mus musculus (Mouse))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM19857(N-{1-[(cyanomethyl)carbamoyl]cyclohexyl}-4-[2-(mor...)
Affinity DataIC50:  8.50E+3nM EC50:  6.70E+3nMAssay Description:Prior to the addition of substrate, different concentrations of the inhibitor ranging from 100 uM to 0.2 nM were preincubated for 15 min with enzyme ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Mus musculus (Mouse))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM19858(N-{1-[(cyanomethyl)carbamoyl]cyclohexyl}-4-(morpho...)
Affinity DataIC50:  4.50E+3nM EC50:  8.50E+3nMAssay Description:Prior to the addition of substrate, different concentrations of the inhibitor ranging from 100 uM to 0.2 nM were preincubated for 15 min with enzyme ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Mus musculus (Mouse))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM19860(4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]-N-...)
Affinity DataIC50:  3.30E+4nM EC50: >1.00E+4nMAssay Description:Prior to the addition of substrate, different concentrations of the inhibitor ranging from 100 uM to 0.2 nM were preincubated for 15 min with enzyme ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM19857(N-{1-[(cyanomethyl)carbamoyl]cyclohexyl}-4-[2-(mor...)
Affinity DataIC50:  2.70E+4nM EC50: >1.00E+4nMpH: 6.5 T: 2°CAssay Description:Prior to the addition of substrate, different concentrations of the inhibitor ranging from 100 uM to 0.2 nM were preincubated for 15 min with enzyme ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50546794(CHEMBL4777335)
Affinity DataKi:  0.0900nMAssay Description:Inhibition of recombinant human Cathepsin S expressed in baculovirus infected insect cells using Z-VVR-AMC as substrate preincubated for 15 mins foll...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50546794(CHEMBL4777335)
Affinity DataKi:  0.0900nMAssay Description:Inhibition of recombinant human cathepsin S using Z-VVR-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50243232(CHEMBL486232 | GNF-PF-5434 | N-((S)-4-methyl-1-oxo...)
Affinity DataKi: <0.100nMAssay Description:Inhibition of human recombinant cathepsin S by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50030745(CHEMBL3342185 | acs.jmedchem.1c00409_ST.412)
Affinity DataKi:  0.130nMAssay Description:Inhibition of human cathepsin S using Z-Phe-Arg-AMC fluorogenic substrate fluorogenic substrate incubated for 60 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50335289(CHEMBL1651361 | N-{4-[5-(2-Thienyl)-1,2,4-oxadiazo...)
Affinity DataKi:  0.150nMAssay Description:Inhibition of human cathepsin S after 30 mins by spectrophotometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50335281(CHEMBL1651355 | N-(Phenylcarbamoyl)-leucyl-methyla...)
Affinity DataKi:  0.160nMAssay Description:Inhibition of human cathepsin S after 30 mins by spectrophotometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50335283(CHEMBL1651357 | N-{4-[5-(2-Thienyl)-1,2,4-oxadiazo...)
Affinity DataKi:  0.160nMAssay Description:Inhibition of human cathepsin S after 30 mins by spectrophotometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50335282(CHEMBL1651356 | N-[4-(5-Methyl-1,2,4-oxadiazol-3-y...)
Affinity DataKi:  0.170nMAssay Description:Inhibition of human cathepsin S after 30 mins by spectrophotometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50030746(CHEMBL3342184 | acs.jmedchem.1c00409_ST.413)
Affinity DataKi:  0.176nMAssay Description:Inhibition of human cathepsin S using Z-Phe-Arg-AMC fluorogenic substrate fluorogenic substrate incubated for 60 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50335284(CHEMBL1651349 | N-[4-(5-Methyl-1,2,4-oxadiazol-3-y...)
Affinity DataKi:  0.190nMAssay Description:Inhibition of human cathepsin S after 30 mins by spectrophotometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50335280(CHEMBL1651354 | N-(Benzylcarbamoyl)-leucyl-methyla...)
Affinity DataKi:  0.200nMAssay Description:Inhibition of human cathepsin S after 30 mins by spectrophotometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50335278(CHEMBL1651352 | N-(Benzyloxycarbonyl)-cyclohexylal...)
Affinity DataKi:  0.200nMAssay Description:Inhibition of human cathepsin S after 30 mins by spectrophotometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50546795(CHEMBL4777740)
Affinity DataKi:  0.200nMAssay Description:Inhibition of recombinant human Cathepsin S expressed in baculovirus infected insect cells using Z-VVR-AMC as substrate preincubated for 15 mins foll...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50546796(CHEMBL4761229)
Affinity DataKi:  0.25nMAssay Description:Inhibition of recombinant human Cathepsin S expressed in baculovirus infected insect cells using Z-VVR-AMC as substrate preincubated for 15 mins foll...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50410979(CHEMBL207347)
Affinity DataKi: <0.25nMAssay Description:Inhibition of human cathepsin SMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

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
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM109847(US8609681, 70)
Affinity DataKi:  0.300nMAssay Description:Determination of the enzymatic activity of the catalytic domain of human Cathepsin S. This protein is obtained as an inactive enzyme from R&D Systems...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50335285(CHEMBL1651350 | N-{4-[5-(2-Thienyl)-1,2,4-oxadiazo...)
Affinity DataKi:  0.320nMAssay Description:Inhibition of human cathepsin S after 30 mins by spectrophotometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50304794((S)-benzyl 1-(2-cyano-1,2-dimethylhydrazinyl)-4-me...)
Affinity DataKi:  0.330nMAssay Description:Inhibition of human cathepsin S after 30 mins by spectrophotometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM103367(US8552202, Example 4)
Affinity DataKi:  0.400nMAssay Description:In vitro inhibition assay using cathepsin.More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM109859(US8609681, 102)
Affinity DataKi:  0.5nMAssay Description:Determination of the enzymatic activity of the catalytic domain of human Cathepsin S. This protein is obtained as an inactive enzyme from R&D Systems...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50304793((S)-benzyl 1-(2-cyano-1,2-dimethylhydrazinyl)-1-ox...)
Affinity DataKi:  0.510nMAssay Description:Inhibition of human cathepsin S after 30 mins by spectrophotometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50392215(CHEMBL2153161)
Affinity DataKi:  0.550nMAssay Description:Inhibition of human cathepsin S using Z-Phe-Val-Arg-pNA as substrate after 80 mins by spectrophotometric analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50002399(CHEMBL197958)
Affinity DataKi:  0.560nMAssay Description:Apparent inhibitory constant against human cathepsin SMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50255571(4-(3-Cyano-benzenesulfonylamino)-N-[1-(2S-ethyl-4-...)
Affinity DataKi:  0.600nMAssay Description:Inhibition of human recombinant cathepsin S expressed in baculovirus by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50255790(4-(2,4-Dimethyl-thiazole-5-sulfonylamino)-N-[1-(2S...)
Affinity DataKi:  0.700nMAssay Description:Inhibition of human recombinant cathepsin S expressed in baculovirus by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50030747(CHEMBL3342183)
Affinity DataKi:  0.777nMAssay Description:Inhibition of human cathepsin S using Z-Phe-Arg-AMC fluorogenic substrate fluorogenic substrate incubated for 60 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50255133(4-Benzenesulfonylamino-N-[1-(2S-ethyl-4-oxo-tetrah...)
Affinity DataKi:  0.800nMAssay Description:Inhibition of human recombinant cathepsin S expressed in baculovirus by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50255627(4-(2-Cyano-benzenesulfonylamino)-N-[1-(2S-ethyl-4-...)
Affinity DataKi:  0.800nMAssay Description:Inhibition of human recombinant cathepsin S expressed in baculovirus by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50335277(CHEMBL1651351 | N-(Benzyloxycarbonyl)-isoleucyl-me...)
Affinity DataKi:  0.830nMAssay Description:Inhibition of human cathepsin S after 30 mins by spectrophotometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50335279(CHEMBL1651353 | N-(Benzyloxycarbonyl)-tyrosyl-meth...)
Affinity DataKi:  0.860nMAssay Description:Inhibition of human cathepsin S after 30 mins by spectrophotometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50255681(CHEMBL473448 | N-[1-(2S-Ethyl-4-oxo-tetrahydro-fur...)
Affinity DataKi:  0.900nMAssay Description:Inhibition of human recombinant cathepsin S expressed in baculovirus by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM19622((2S)-2-[(7-chloro-1,3-benzoxazol-2-yl)amino]-3-cyc...)
Affinity DataKi:  1nM ΔG°:  -53.4kJ/molepH: 5.5 T: 2°CAssay Description:The recombinant human cathepsin enzyme was preincubated with inhibitor for 20 minutes prior to addition of substrate. The substrate hydrolysis was mo...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Merck Frosst Centre For Therapeutic Research

LigandPNGBDBM50255569(CHEMBL475669 | N-[1-(2S-Ethyl-4-oxo-tetrahydro-fur...)
Affinity DataKi:  1nMAssay Description:Inhibition of human recombinant cathepsin S expressed in baculovirus by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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