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Found 238 with Last Name = 'coppola' and Initial = 'gm'
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
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
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
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
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
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
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
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
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
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
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
Target[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrial(Rattus norvegicus)
Novartis Institute For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50472804(CHEMBL83273)
Affinity DataIC50:  3.30nMAssay Description:Inhibitory activity tested against Pyruvate Dehydrogenase Kinase (PDHK) receptor from rats.More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
Target3-hydroxy-3-methylglutaryl-coenzyme A reductase(Rattus norvegicus (rat))
TBA

Curated by ChEMBL
LigandPNGBDBM50291237(CHEMBL153492 | Sodium; (E)-(3R,5S)-7-[4-(4-fluoro-...)
Affinity DataIC50:  4.40nMAssay Description:Tested in vitro for the HMG-CoA reductase inhibitory activity in a microsomal preparationMore data for this Ligand-Target Pair
In DepthDetails Article
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
Target[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrial(Rattus norvegicus)
Novartis Institute For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50472836(CHEMBL311125)
Affinity DataIC50:  4.5nMAssay Description:Inhibitory activity tested against Pyruvate Dehydrogenase Kinase (PDHK) receptor from rats.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
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM50034842((2R,4S)-5-Biphenyl-4-yl-4-(3-carboxy-propionylamin...)
Affinity DataIC50:  6nMAssay 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
Target3-hydroxy-3-methylglutaryl-coenzyme A reductase(Rattus norvegicus (rat))
TBA

Curated by ChEMBL
LigandPNGBDBM50291241(CHEMBL153021 | Sodium; (E)-(3R,5S)-7-[4-(4-fluoro-...)
Affinity DataIC50:  6.30nMAssay Description:Tested in vitro for the HMG-CoA reductase inhibitory activity in a microsomal preparationMore data for this Ligand-Target Pair
In DepthDetails Article
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM130354(US8822534, Example 5-4 | US8993631, 5-2)
Affinity DataIC50:  6.70nMAssay 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
LigandPNGBDBM50509655(CHEMBL4466321)
Affinity DataIC50:  6.90nMAssay 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
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM153109(US8993631, 16-8 | US9006249, Example 3-60)
Affinity DataIC50:  7.30nMpH: 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
LigandPNGBDBM309463(US9603819, Example 3-60)
Affinity DataIC50:  7.30nMAssay 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
LigandPNGBDBM50509649(CHEMBL4474653)
Affinity DataIC50:  8nMAssay 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
Target[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrial(Rattus norvegicus)
Novartis Institute For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50472839(CHEMBL3349325)
Affinity DataIC50:  9.10nMAssay Description:Inhibitory activity tested against Pyruvate Dehydrogenase Kinase (PDHK) receptor from rats.More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
Target3-hydroxy-3-methylglutaryl-coenzyme A reductase(Rattus norvegicus (rat))
TBA

Curated by ChEMBL
LigandPNGBDBM50291258(CHEMBL152366 | Sodium; (E)-(3R,5S)-7-[4-(4-fluoro-...)
Affinity DataIC50:  9.70nMAssay Description:Tested in vitro for the HMG-CoA reductase inhibitory activity in a microsomal preparationMore data for this Ligand-Target Pair
In DepthDetails Article
TargetDiacylglycerol O-acyltransferase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50239481(CHEMBL4061308)
Affinity DataIC50:  10nMAssay Description:Inhibition of recombinant human His6-tagged DGAT1 expressed in Sf9 insect cell membranes assessed as inhibition of triglyceride formation using diole...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrial(Rattus norvegicus)
Novartis Institute For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50472841(CHEMBL443012)
Affinity DataIC50:  13nMAssay Description:Inhibitory activity tested against Pyruvate Dehydrogenase Kinase (PDHK) receptor from rats.More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetDiacylglycerol O-acyltransferase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50239482(CHEMBL1683001)
Affinity DataIC50:  14nMAssay Description:Inhibition of recombinant human His6-tagged DGAT1 expressed in Sf9 insect cell membranes assessed as inhibition of triglyceride formation using diole...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM155342(US9006249, Example 13-1)
Affinity DataIC50:  14nMpH: 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
LigandPNGBDBM309468((2R,4S)-5-biphenyl-4-yl-2-methyl-4-[(1H-tetrazole-...)
Affinity DataIC50:  14nMAssay 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
Target[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrial(Rattus norvegicus)
Novartis Institute For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50472793(CHEMBL313878)
Affinity DataIC50:  14nMAssay Description:Inhibitory activity tested against Pyruvate Dehydrogenase Kinase (PDHK) receptor from rats.More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
Target3-hydroxy-3-methylglutaryl-coenzyme A reductase(Rattus norvegicus (rat))
TBA

Curated by ChEMBL
LigandPNGBDBM50291255(CHEMBL358623 | Sodium; (E)-(3R,5S)-7-[4-(4-fluoro-...)
Affinity DataIC50:  15nMAssay Description:Tested in vitro for the HMG-CoA reductase inhibitory activity in a microsomal preparationMore data for this Ligand-Target Pair
In DepthDetails Article
Target[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrial(Rattus norvegicus)
Novartis Institute For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50236533(CHEMBL316388)
Affinity DataIC50:  16nMAssay Description:Inhibitory activity tested against Pyruvate Dehydrogenase Kinase (PDHK) receptor from rats.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDiacylglycerol O-acyltransferase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50239480(CHEMBL4074410)
Affinity DataIC50:  17nMAssay Description:Inhibition of recombinant human His6-tagged DGAT1 expressed in Sf9 insect cell membranes assessed as inhibition of triglyceride formation using diole...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1,/2,/3,/4, mitochondrial(Homo sapiens (Human))
Novartis Institute For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50236533(CHEMBL316388)
Affinity DataIC50:  17nMAssay Description:In vitro inhibitory activity against Pyruvate dehydrogenase kinase by primary enzymatic assayMore data for this Ligand-Target Pair
Target[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrial(Rattus norvegicus)
Novartis Institute For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50472825(CHEMBL81574)
Affinity DataIC50:  19nMAssay Description:Inhibitory activity tested against Pyruvate Dehydrogenase Kinase (PDHK) receptor from rats.More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM50509648(CHEMBL4439270)
Affinity DataIC50:  20nMAssay 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
Target[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrial(Rattus norvegicus)
Novartis Institute For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50472811(CHEMBL310879)
Affinity DataIC50:  20nMAssay Description:Inhibitory activity tested against Pyruvate Dehydrogenase Kinase (PDHK) receptor from rats.More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
Target3-hydroxy-3-methylglutaryl-coenzyme A reductase(Rattus norvegicus (rat))
TBA

Curated by ChEMBL
LigandPNGBDBM50291256(CHEMBL152129 | Sodium; (E)-(3R,5S)-7-[5-(4-chloro-...)
Affinity DataIC50:  21nMAssay Description:Tested in vitro for the HMG-CoA reductase inhibitory activity in a microsomal preparationMore data for this Ligand-Target Pair
In DepthDetails Article
Target[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1,/2,/3,/4, mitochondrial(Homo sapiens (Human))
Novartis Institute For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50472310(CHEMBL84231)
Affinity DataIC50:  21nMAssay Description:In vitro inhibitory activity against Pyruvate dehydrogenase kinase by primary enzymatic assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
Target[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrial(Rattus norvegicus)
Novartis Institute For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50472310(CHEMBL84231)
Affinity DataIC50:  21nMAssay Description:Inhibitory activity tested against Pyruvate Dehydrogenase Kinase (PDHK) receptor from rats.More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM50509650(CHEMBL4592467)
Affinity DataIC50:  21nMAssay 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
TargetDiacylglycerol O-acyltransferase 1(Homo sapiens (Human))
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50239484(CHEMBL4103025)
Affinity DataIC50:  23nMAssay Description:Inhibition of recombinant human His6-tagged DGAT1 expressed in Sf9 insect cell membranes assessed as inhibition of triglyceride formation using diole...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM50509660(CHEMBL4434901)
Affinity DataIC50:  24nMAssay 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
Target[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrial(Rattus norvegicus)
Novartis Institute For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50472831(CHEMBL84271)
Affinity DataIC50:  25nMAssay Description:Inhibitory activity tested against Pyruvate Dehydrogenase Kinase (PDHK) receptor from rats.More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNeprilysin(Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM7494(US8822534, 5-36 | US8822534, Example 5-1 | US89936...)
Affinity DataIC50:  25nMAssay 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
LigandPNGBDBM50509656(CHEMBL4568947)
Affinity DataIC50:  26nMAssay 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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