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TargetNeprilysin(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
In Depth
Date in BDB:
10/26/2015
Entry Details
US Patent

TargetNeprilysin(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
In Depth
Date in BDB:
4/23/2019
Entry Details
US Patent

TargetNeprilysin(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 Depth
Date in BDB:
10/26/2015
Entry Details
US Patent

TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM309469(US9603819, Example 49-1 | (2R,4S)-5-(3′-Chlo...)
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
In Depth
Date in BDB:
4/23/2019
Entry Details
US Patent

TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50175518((3R,7S)-7-((R)-2-Mercapto-3-phenyl-propionylamino)...)
Affinity DataIC50: 0.0800nMAssay Description:Inhibitory concentration against neutral endopeptidaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2012
Entry Details Article
PubMed
TargetNeprilysin(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 Depth
Date in BDB:
4/13/2015
Entry Details
US Patent

TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM186570(US9163040, 2)
Affinity DataIC50: 0.110nMpH: 7.4 T: 2°CAssay Description:Recombinant human neutral endopeptidase (expressed in insect cells and purified using standard methods, final concentration 7 pM) is pre-incubated wi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/18/2016
Entry Details
US Patent

TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50073120((4S,6S,9aS)-6-((S)-2-Mercapto-3-phenyl-propionylam...)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of NEP (unknown origin) preincubated for 10 mins followed by fluorogenic substrate addition and measured after 20 mins by fluorescence ass...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetNeprilysin(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 Depth
Date in BDB:
4/13/2015
Entry Details
US Patent

TargetNeprilysin(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 Depth
Date in BDB:
4/13/2015
Entry Details
US Patent

TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM298285(US11547687, Example 2A | US11547687, Compound Exam...)
Affinity DataKi:  0.200nMAssay Description:Recombinant human NEP and recombinant human ACE were obtained commercially (R&D Systems, Minneapolis, Minn., catalog numbers 1182-ZN and 929-ZN, resp...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/23/2023
Entry Details
US Patent

TargetNeprilysin/Angiotensin-converting enzyme(Human)
Theravance Biopharma R&D Ip

US Patent
LigandPNGBDBM298285(US11547687, Example 2A | US11547687, Compound Exam...)
Affinity DataKi:  0.200nMAssay Description:The assays were performed in 384-well white opaque plates at 37° C. using the fluorogenic peptide substrates at a concentration of 10 μM in Assa...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2023
Entry Details
US Patent

TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50411736(CHEMBL271225)
Affinity DataKi:  0.280nMAssay Description:Inhibition of human recombinant NEP by fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/21/2013
Entry Details Article
PubMed
TargetNeprilysin(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
In Depth
Date in BDB:
10/26/2015
Entry Details
US Patent

TargetNeprilysin(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 Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMed
TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50344193((S)-2-(1-((S)-1-carboxy-2-(5-phenyloxazol-2-yl)eth...)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of neutral endopeptidaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2011
Entry Details Article
PubMed
TargetNeprilysin(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 Depth
Date in BDB:
4/13/2015
Entry Details
US Patent

TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50344195((S)-2-(1-((S)-1-carboxy-2-(5-(4-chlorophenyl)oxazo...)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of neutral endopeptidaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2011
Entry Details Article
PubMed
TargetNeprilysin(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
In Depth
Date in BDB:
4/23/2019
Entry Details
US Patent

TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM582847(US11547687, Comparative Compound I | US20230285340...)
Affinity DataKi:  0.316nMAssay Description:Recombinant human NEP and recombinant human ACE were obtained commercially (R&D Systems, Minneapolis, Minn., catalog numbers 1182-ZN and 929-ZN, resp...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/23/2023
Entry Details
US Patent

TargetNeprilysin/Angiotensin-converting enzyme(Human)
Theravance Biopharma R&D Ip

US Patent
LigandPNGBDBM582848(US11547687, Comparative Compound J | US20230285340...)
Affinity DataKi:  0.316nMAssay Description:The assays were performed in 384-well white opaque plates at 37° C. using the fluorogenic peptide substrates at a concentration of 10 μM in Assa...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2023
Entry Details
US Patent

TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50354041(CHEMBL1829584)
Affinity DataIC50: 0.360nMAssay Description:Inhibition of neutral endopeptidase in human fibroblasts homogenates using glutaryl-Ala-Ala-Phe-4-methoxy-2-naphtylamide as substrate after 1 hrs by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/24/2012
Entry Details Article
PubMed
TargetNeprilysin(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 Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMed
TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50614468(CHEMBL5272269)
Affinity DataKi:  0.400nMAssay Description:Binding affinity to neutral endopeptidase (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM582848(US11547687, Comparative Compound J | US20230285340...)
Affinity DataKi:  0.501nMAssay Description:Recombinant human NEP and recombinant human ACE were obtained commercially (R&D Systems, Minneapolis, Minn., catalog numbers 1182-ZN and 929-ZN, resp...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/23/2023
Entry Details
US Patent

TargetNeprilysin/Angiotensin-converting enzyme(Human)
Theravance Biopharma R&D Ip

US Patent
LigandPNGBDBM582849(US11547687, Comparative Compound K)
Affinity DataKi:  0.501nMAssay Description:The assays were performed in 384-well white opaque plates at 37° C. using the fluorogenic peptide substrates at a concentration of 10 μM in Assa...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2023
Entry Details
US Patent

TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50354042(CHEMBL1829585)
Affinity DataIC50: 0.510nMAssay Description:Inhibition of neutral endopeptidase in human fibroblasts homogenates using glutaryl-Ala-Ala-Phe-4-methoxy-2-naphtylamide as substrate after 1 hrs by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/24/2012
Entry Details Article
PubMed
TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50085452(Sampatrilat | (S)-2-[((S)-6-Amino-2-methanesulfony...)
Affinity DataIC50: 0.600nMAssay Description:Inhibition of neutral endopeptidaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2011
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50291559({2-Benzo[1,3]dioxol-5-yl-1-[(S)-2-biphenyl-4-yl-1-...)
Affinity DataIC50: 0.600nMAssay Description:Inhibition of neutral endopeptidase 24.11(NEP)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/28/2012
Entry Details Article

TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50403254(CHEMBL51389)
Affinity DataIC50: 0.600nMAssay Description:Tested in vitro for inhibition of neutral endopeptidase (NEP)More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/19/2013
Entry Details Article

TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50344191((S)-2-(1-((S)-1-carboxy-2-(5-phenyloxazol-2-yl)eth...)
Affinity DataIC50: 0.600nMAssay Description:Inhibition of neutral endopeptidaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2011
Entry Details Article
PubMed
TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50503875(CHEMBL4435800)
Affinity DataIC50: 0.631nMAssay Description:Inhibition of NEP (unknown origin) preincubated for 10 mins followed by fluorogenic substrate addition and measured after 20 mins by fluorescence ass...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMed
TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50503883(CHEMBL4443691)
Affinity DataIC50: 0.631nMAssay Description:Inhibition of NEP (unknown origin) preincubated for 10 mins followed by fluorogenic substrate addition and measured after 20 mins by fluorescence ass...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMed
TargetNeprilysin/Angiotensin-converting enzyme(Human)
Theravance Biopharma R&D Ip

US Patent
LigandPNGBDBM298305(US11547687, Compound Example 5A | US10123984, Exam...)
Affinity DataKi:  0.631nMAssay Description:The assays were performed in 384-well white opaque plates at 37° C. using the fluorogenic peptide substrates at a concentration of 10 μM in Assa...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2023
Entry Details
US Patent

TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM617465(US20230285340, Example 5A)
Affinity DataKi:  0.631nMAssay Description:Recombinant human NEP and recombinant human ACE were obtained commercially (R&D Systems, Minneapolis, Minn., catalog numbers 1182-ZN and 929-ZN, resp...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/23/2023
Entry Details
US Patent

TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50287299((2S,4S)-5-Biphenyl-4-yl-4-(4-carboxymethyl-thiazol...)
Affinity DataIC50: 0.690nMAssay Description:In vitro inhibition of Neutral EndopeptidaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/26/2012
Entry Details Article

TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50407297(CHEMBL2052008)
Affinity DataKi:  0.700nMAssay Description:In vivo inhibitory potency against neutral endopeptidase by displacement of [3H]HACBOGly binding in mouse kidneyMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50024101((S)-2-((S)-2-Mercaptomethyl-3-phenyl-propionylamin...)
Affinity DataKi:  0.700nMAssay Description:Inhibition of human recombinant NEP using Suc-Ala-Ala-Phe-AMC as substrate after 30 mins by fluorimetryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/12/2015
Entry Details Article
PubMed
TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50291555({2-Benzo[1,3]dioxol-4-yl-1-[(S)-2-biphenyl-4-yl-1-...)
Affinity DataIC50: 0.700nMAssay Description:Inhibition of neutral endopeptidase 24.11(NEP)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/28/2012
Entry Details Article

TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50407297(CHEMBL2052008)
Affinity DataKi:  0.700nMAssay Description:In vivo inhibitory potency against neutral endopeptidase by displacement of [3H]HACBOGly binding in mouse kidneyMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50291558({1-[(S)-2-Biphenyl-4-yl-1-(1H-tetrazol-5-yl)-ethyl...)
Affinity DataIC50: 0.740nMAssay Description:Inhibition of neutral endopeptidase 24.11(NEP)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/28/2012
Entry Details Article

TargetNeprilysin(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
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMed
TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50411731(CHEMBL257726)
Affinity DataKi:  0.800nMAssay Description:Inhibition of human recombinant NEP by fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/21/2013
Entry Details Article
PubMed
TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50400808(CHEMBL2204326)
Affinity DataIC50: 0.800nMAssay Description:Inhibition of neutral endopeptidaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50064106({[(S)-2-Biphenyl-4-yl-1-(2H-tetrazol-5-yl)-ethylam...)
Affinity DataIC50: 0.900nMAssay Description:Inhibition of neutral endopeptidase 24.11(NEP)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/28/2012
Entry Details Article

TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50056252((6S,9S)-6-Mercaptomethyl-7-oxo-6,7,8,9,10,11,12,13...)
Affinity DataIC50: 0.900nMAssay Description:Inhibition of neutral endopeptidaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM50056252((6S,9S)-6-Mercaptomethyl-7-oxo-6,7,8,9,10,11,12,13...)
Affinity DataIC50: 0.900nMAssay Description:Inhibitory concentration required to inhibit neutral endopeptidase (NEP)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM299642(US9593110, Example 87b | US9593110, Example 88b | ...)
Affinity DataKi: <1nMAssay Description:Recombinant human NEP and recombinant human ACE were obtained commercially (R&D Systems, Minneapolis, Minn., catalog numbers 1182-ZN and 929-ZN, resp...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/14/2019
Entry Details
US Patent

TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM299643(US9593110, Example 13 | (2R,4R)-2-Amino-5-(5′...)
Affinity DataKi: <1nMAssay Description:Recombinant human NEP and recombinant human ACE were obtained commercially (R&D Systems, Minneapolis, Minn., catalog numbers 1182-ZN and 929-ZN, resp...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/14/2019
Entry Details
US Patent

TargetNeprilysin(Human)
Novartis

US Patent
LigandPNGBDBM299642(US9593110, Example 87b | US9593110, Example 88b | ...)
Affinity DataKi: <1nMAssay Description:Recombinant human NEP and recombinant human ACE were obtained commercially (R&D Systems, Minneapolis, Minn., catalog numbers 1182-ZN and 929-ZN, resp...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/14/2019
Entry Details
US Patent

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