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Found 275 with Last Name = 'iwaki' and Initial = 'y'
TargetSerine/threonine-protein kinase WNK1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50258546(CHEMBL4087727)
Affinity DataKi:  32nMAssay Description:Allosteric inhibition of WNK1 (unknown origin) expressed in HEK293 cells co-expressing flag-OSR1 assessed as reduction in sorbitol-stimulated OSR1 ph...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM155343(US9006249, Example 49-2 | US9603819, Example 49-2)
Affinity DataIC50:  0.0300nMAssay Description:The activity of a compound according to the present invention can be assessed by the following in vitro & in vivo methods and/or by the following in ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM155343(US9006249, Example 49-2 | US9603819, Example 49-2)
Affinity DataIC50:  0.0300nMpH: 7.4 T: 2°CAssay Description:See A fluorescence lifetime-based assay for protease inhibitor profiling on human kallikrein 7 Doering K, Meder G, Hinnenberger M, Woelcke J, Mayr L ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM153121(US8993631, 29-2 | US9006249, Example 49-1)
Affinity DataIC50:  0.0400nMpH: 7.4 T: 2°CAssay Description:See A fluorescence lifetime-based assay for protease inhibitor profiling on human kallikrein 7 Doering K, Meder G, Hinnenberger M, Woelcke J, Mayr L ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM309469((2R,4S)-5-(3′-Chloro-biphenyl-4-yl)-4-[(3-hy...)
Affinity DataIC50:  0.0400nMAssay Description:The activity of a compound according to the present invention can be assessed by the following in vitro & in vivo methods and/or by the following in ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMembrane metallo-endopeptidase-like 1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM130367(US8822534, Example 11-14)
Affinity DataIC50:  0.0700nMpH: 7.4 T: 2°CAssay Description:Recombinant human neutral endopeptidase (expressed in insect cells and purified using standard methods, final concentration 7 μM) is pre-incubat...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM138390(US8877786, Example 3-1)
Affinity DataIC50:  0.0900nMpH: 7.4 T: 2°CAssay Description:The in vitro inhibition of recombinant human neutral endopeptidase (NEP, EC 3.424.11) can be determined as follows:Recombinant human neutral endopept...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMembrane metallo-endopeptidase-like 1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM130365(US8822534, Example 11-1 | US8822534, Example 12-1 ...)
Affinity DataIC50:  0.200nMpH: 7.4 T: 2°CAssay Description:Recombinant human neutral endopeptidase (expressed in insect cells and purified using standard methods, final concentration 7 μM) is pre-incubat...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM138396(US8877786, Example 3-13)
Affinity DataIC50:  0.200nMpH: 7.4 T: 2°CAssay Description:The in vitro inhibition of recombinant human neutral endopeptidase (NEP, EC 3.424.11) can be determined as follows:Recombinant human neutral endopept...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM138395(US8877786, Example 3-12)
Affinity DataIC50:  0.200nMpH: 7.4 T: 2°CAssay Description:The in vitro inhibition of recombinant human neutral endopeptidase (NEP, EC 3.424.11) can be determined as follows:Recombinant human neutral endopept...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM153128(US8993631, 36)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of recombinant human NEP expressed in insect cells preincubated for 1 hr using Cys(PT14)-Arg-Arg-Leu-Trp-OH as substrate and measured afte...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM155344(US9006249, Example 49-3 | US9603819, Example 49-3)
Affinity DataIC50:  0.300nMAssay Description:The activity of a compound according to the present invention can be assessed by the following in vitro & in vivo methods and/or by the following in ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM155344(US9006249, Example 49-3 | US9603819, Example 49-3)
Affinity DataIC50:  0.300nMpH: 7.4 T: 2°CAssay Description:See A fluorescence lifetime-based assay for protease inhibitor profiling on human kallikrein 7 Doering K, Meder G, Hinnenberger M, Woelcke J, Mayr L ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM138391(US8877786, Example 3-2)
Affinity DataIC50:  0.300nMpH: 7.4 T: 2°CAssay Description:The in vitro inhibition of recombinant human neutral endopeptidase (NEP, EC 3.424.11) can be determined as follows:Recombinant human neutral endopept...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM130359(US8822534, Example 5-39 | US8993631, 5-8)
Affinity DataIC50:  0.380nMAssay Description:Inhibition of recombinant human NEP expressed in insect cells preincubated for 1 hr using Cys(PT14)-Arg-Arg-Leu-Trp-OH as substrate and measured afte...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMembrane metallo-endopeptidase-like 1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM130360(US8822534, Example 5-46 | US8993631, 5-9)
Affinity DataIC50:  0.5nMpH: 7.4 T: 2°CAssay Description:Recombinant human neutral endopeptidase (expressed in insect cells and purified using standard methods, final concentration 7 μM) is pre-incubat...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMembrane metallo-endopeptidase-like 1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM130366(US8822534, Example 11-11 | US8993631, 9-6)
Affinity DataIC50:  0.5nMpH: 7.4 T: 2°CAssay Description:Recombinant human neutral endopeptidase (expressed in insect cells and purified using standard methods, final concentration 7 μM) is pre-incubat...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMembrane metallo-endopeptidase-like 1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM130362(US8822534, Example 5-55 | US8993631, 5-11)
Affinity DataIC50:  0.700nMpH: 7.4 T: 2°CAssay Description:Recombinant human neutral endopeptidase (expressed in insect cells and purified using standard methods, final concentration 7 μM) is pre-incubat...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMembrane metallo-endopeptidase-like 1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM130359(US8822534, Example 5-39 | US8993631, 5-8)
Affinity DataIC50:  0.700nMpH: 7.4 T: 2°CAssay Description:Recombinant human neutral endopeptidase (expressed in insect cells and purified using standard methods, final concentration 7 μM) is pre-incubat...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM50509659(CHEMBL4443138)
Affinity DataIC50:  0.800nMAssay Description:Inhibition of recombinant human NEP expressed in insect cells preincubated for 1 hr using Cys(PT14)-Arg-Arg-Leu-Trp-OH as substrate and measured afte...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMembrane metallo-endopeptidase-like 1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM130369(US8822534, Example 14-1 | US8993631, 11-1)
Affinity DataIC50:  0.800nMpH: 7.4 T: 2°CAssay Description:Recombinant human neutral endopeptidase (expressed in insect cells and purified using standard methods, final concentration 7 μM) is pre-incubat...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSerine/threonine-protein kinase WNK1 [166-489](Homo sapiens (Human))
Novartis Institutes

LigandPNGBDBM203827(N-(tert-butyl)-1-(1-(5-(5-(trifluoromethyl)-1,3,4-...)
Affinity DataIC50:  1nMpH: 7.3 T: 2°CAssay Description:Each well of the MBP-coated ScintiPlates held 100 ul of a solution containing 20 mM HEPES pH 7.3, 5 mM MnCl2 (WNK1 and WNK4) or 3 mM MnCl2 (WNK2 and ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM153108(US8993631, 16-5 | US9006249, Example 3-32 | US9603...)
Affinity DataIC50:  1nMpH: 7.4 T: 2°CAssay Description:See A fluorescence lifetime-based assay for protease inhibitor profiling on human kallikrein 7 Doering K, Meder G, Hinnenberger M, Woelcke J, Mayr L ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCathepsin S(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50273289(2-Cyano-4-(1-methyl-piperidin-4-yloxy)-6-[(spiro[2...)
Affinity DataIC50:  1nMAssay Description:Inhibition of human recombinant cathepsin S by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM153108(US8993631, 16-5 | US9006249, Example 3-32 | US9603...)
Affinity DataIC50:  1nMAssay Description:The activity of a compound according to the present invention can be assessed by the following in vitro & in vivo methods and/or by the following in ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMembrane metallo-endopeptidase-like 1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM130365(US8822534, Example 11-1 | US8822534, Example 12-1 ...)
Affinity DataIC50:  1.10nMpH: 7.4 T: 2°CAssay Description:Recombinant human neutral endopeptidase (expressed in insect cells and purified using standard methods, final concentration 7 μM) is pre-incubat...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMembrane metallo-endopeptidase-like 1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM130370(US8822534, Example 15-1 | US8993631, 12-1)
Affinity DataIC50:  1.20nMpH: 7.4 T: 2°CAssay Description:Recombinant human neutral endopeptidase (expressed in insect cells and purified using standard methods, final concentration 7 μM) is pre-incubat...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM130365(US8822534, Example 11-1 | US8822534, Example 12-1 ...)
Affinity DataIC50:  1.5nMAssay Description:Inhibition of recombinant human NEP expressed in insect cells preincubated for 1 hr using Cys(PT14)-Arg-Arg-Leu-Trp-OH as substrate and measured afte...More data for this Ligand-Target Pair
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM50509652(CHEMBL4557208)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of recombinant human NEP expressed in insect cells preincubated for 1 hr using Cys(PT14)-Arg-Arg-Leu-Trp-OH as substrate and measured afte...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50263668(2-Cyano-4-[2-(1-methyl-piperidin-4-yl)-ethoxy]-6-[...)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant cathepsin S by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50273288(2-Cyano-4-[(spiro[2.5]oct-6-ylmethyl)-amino]-pyrim...)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant cathepsin S by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50272786(5-Bromo-4-[2-(1-methyl-piperidin-4-yl)-ethoxy]-6-[...)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant cathepsin S by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM50509666(CHEMBL4442804)
Affinity DataIC50:  2nMAssay Description:Inhibition of recombinant human NEP expressed in insect cells preincubated for 1 hr using Cys(PT14)-Arg-Arg-Leu-Trp-OH as substrate and measured afte...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMembrane metallo-endopeptidase-like 1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM130358(US8822534, Example 5-37 | US8993631, 5-7)
Affinity DataIC50:  2.30nMpH: 7.4 T: 2°CAssay Description:Recombinant human neutral endopeptidase (expressed in insect cells and purified using standard methods, final concentration 7 μM) is pre-incubat...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM138393(US8877786, Example 3-7 | US8993631, 32-4)
Affinity DataIC50:  2.40nMpH: 7.4 T: 2°CAssay Description:The in vitro inhibition of recombinant human neutral endopeptidase (NEP, EC 3.424.11) can be determined as follows:Recombinant human neutral endopept...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMembrane metallo-endopeptidase-like 1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM130361(US8822534, Example 5-47 | US8993631, 5-10)
Affinity DataIC50:  2.70nMpH: 7.4 T: 2°CAssay Description:Recombinant human neutral endopeptidase (expressed in insect cells and purified using standard methods, final concentration 7 μM) is pre-incubat...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCathepsin S(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50263557(2-cyano-4-((1-isopropylpiperidin-4-yl)methoxy)-N-m...)
Affinity DataIC50:  3nMAssay Description:Inhibition of human recombinant cathepsin S by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50263609(2-cyano-4-((1-(2-hydroxyethyl)piperidin-4-yl)metho...)
Affinity DataIC50:  3nMAssay Description:Inhibition of human recombinant cathepsin S by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50263555(2-cyano-N-methyl-4-((1-methylpiperidin-4-yl)methox...)
Affinity DataIC50:  3nMAssay Description:Inhibition of human recombinant cathepsin S by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50273220(2-Cyano-4-[(spiro[2.5]oct-6-ylmethyl)-amino]-pyrim...)
Affinity DataIC50:  3nMAssay Description:Inhibition of human recombinant cathepsin S by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMembrane metallo-endopeptidase-like 1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM130356(US8822534, Example 5-11 | US8993631, 5-4)
Affinity DataIC50:  3nMpH: 7.4 T: 2°CAssay Description:Recombinant human neutral endopeptidase (expressed in insect cells and purified using standard methods, final concentration 7 μM) is pre-incubat...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCathepsin S(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50263554(2-cyano-N-methyl-4-(2-(1-methylpiperidin-4-yl)etho...)
Affinity DataIC50:  4nMAssay Description:Inhibition of human recombinant cathepsin S by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMembrane metallo-endopeptidase-like 1(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM130355(US8822534, Example 5-7 | US8993631, 5-3)
Affinity DataIC50:  4nMpH: 7.4 T: 2°CAssay Description:Recombinant human neutral endopeptidase (expressed in insect cells and purified using standard methods, final concentration 7 μM) is pre-incubat...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetSerine/threonine-protein kinase WNK1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50258566(CHEMBL4088706)
Affinity DataIC50:  4nMAssay Description:Allosteric inhibition of recombinant human N-terminal GST-tagged WNK1 catalytic domain (1 to 491 residues) expressed in baculovirus expression system...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50273256(2-Cyano-4-[(spiro[2.5]oct-6-ylmethyl)-amino]-pyrim...)
Affinity DataIC50:  4nMAssay Description:Inhibition of human recombinant cathepsin S by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM130355(US8822534, Example 5-7 | US8993631, 5-3)
Affinity DataIC50:  4.5nMAssay Description:Inhibition of recombinant human NEP expressed in insect cells preincubated for 1 hr using Cys(PT14)-Arg-Arg-Leu-Trp-OH as substrate and measured afte...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50263610(2-cyano-N-methyl-4-(piperidin-4-ylmethoxy)-6-(spir...)
Affinity DataIC50:  5nMAssay Description:Inhibition of human recombinant cathepsin S by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin S(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50263611(2-cyano-N-methyl-4-(spiro[3.5]nonan-7-ylmethylamin...)
Affinity DataIC50:  5nMAssay Description:Inhibition of human recombinant cathepsin S by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase WNK1 [1-491](Homo sapiens (Human))
Novartis Institutes

LigandPNGBDBM203827(N-(tert-butyl)-1-(1-(5-(5-(trifluoromethyl)-1,3,4-...)
Affinity DataIC50:  5nMpH: 7.3 T: 2°CAssay Description:Each well of the MBP-coated ScintiPlates held 100 ul of a solution containing 20 mM HEPES pH 7.3, 5 mM MnCl2 (WNK1 and WNK4) or 3 mM MnCl2 (WNK2 and ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM50509647(CHEMBL4518426)
Affinity DataIC50:  5.40nMAssay Description:Inhibition of recombinant human NEP expressed in insect cells preincubated for 1 hr using Cys(PT14)-Arg-Arg-Leu-Trp-OH as substrate and measured afte...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
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