Compile Data Set for Download or QSAR
Report error Found 34 Enz. Inhib. hit(s) with all data for entry = 50009909
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533417(RO 4929097 | RO-4929097 | Rg 4733 | Rg-4733 | Ro49...)
Affinity DataEC50:  5nMAssay Description:Inhibition of gamma secretase mediated Notch1 signaling in HEK293 cells expressing truncated human Notch1 by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533417(RO 4929097 | RO-4929097 | Rg 4733 | Rg-4733 | Ro49...)
Affinity DataEC50:  14nMAssay Description:Inhibition of gamma secretase in HEK293 cells expressing APP695 assessed as reduction in amyloid beta (1 to 40 residues) by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50241259(LY-411575 | (2S)-2-((S)-2-(3,5-difluorophenyl)-2-h...)
Affinity DataIC50: 0.0800nMAssay Description:Inhibition of gamma secretase in HEK293 cells expressing APP 695 assessed as reduction in amyloid beta levels after 5 hrs by Western blot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533414(CHEMBL4436451)
Affinity DataIC50: 0.270nMAssay Description:Inhibition of gamma secretase (unknown origin) mediated Notch activationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50241259(LY-411575 | (2S)-2-((S)-2-(3,5-difluorophenyl)-2-h...)
Affinity DataIC50: 0.390nMAssay Description:Inhibition of gamma secretase mediated Notch signaling in HEK293 cells after 5 hrs by Western blot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533419(CHEMBL4476008)
Affinity DataIC50: 0.410nMAssay Description:Inhibition of gamma secretase (unknown origin) mediated Notch signalingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533416(CHEMBL4303400)
Affinity DataIC50: 2.60nMAssay Description:Inhibition of gamma secretase in human SupT1 cells assessed as reduction in amyloid beta 40 after 16 hrs by chemiluminescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533416(CHEMBL4303400)
Affinity DataIC50: 2.90nMAssay Description:Inhibition of gamma secretase mediated Notch signaling in human SupT1 cells after 16 hrs by chemiluminescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533417(RO 4929097 | RO-4929097 | Rg 4733 | Rg-4733 | Ro49...)
Affinity DataIC50: 4nMAssay Description:Inhibition of recombinant human gamma secretase expressing APP751 by electrochemiluminescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50458158(Mk-0752)
Affinity DataIC50: 5nMAssay Description:Inhibition of gamma secretase in human MCF7 cells assessed as reduction in amyloid beta 40 after 3 days by Western blot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDisintegrin and metalloproteinase domain-containing protein 10(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533418(CHEMBL4435465)
Affinity DataIC50: 5.30nMAssay Description:Inhibition of ADAM10 (unknown origin) assessed as blockage of TNF-alpha sheddingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50458159(Nirogacestat | PF 03084014 | PF 3084014 | PF-03084...)
Affinity DataIC50: 6.20nMAssay Description:Inhibition of gamma secretase isolated from human HeLa cell derived P2 membrane assessed as reduction in amyloid beta (1 to 40 residues) using recomb...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM28944((2S)-2-hydroxy-3-methyl-N-[(1S)-1-{[(1S)-3-methyl-...)
Affinity DataIC50: 11nMAssay Description:Inhibition of gamma secretase (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50477339(BMS-299897 | CHEMBL247471)
Affinity DataIC50: 12nMAssay Description:Inhibition of gamma secretase (unknown origin) assessed as reduction in amyloid beta levels by sandwich ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM28944((2S)-2-hydroxy-3-methyl-N-[(1S)-1-{[(1S)-3-methyl-...)
Affinity DataIC50: 14nMAssay Description:Inhibition of gamma secretase (unknown origin) mediated Notch signalingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM28922((2S)-N-(5-chlorothiophen-2-yl)-4,4,4-trifluoro-1-h...)
Affinity DataIC50: 15nMAssay Description:Inhibition of gamma secretase (unknown origin) mediated APP cleavage in CHO cells expressing APP Swedish KM/NL mutant assessed as reduction in amyloi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50100434(tert-butyl (2S,3R,5R)-5-(((S)-1-((S)-1-amino-1-oxo...)
Affinity DataIC50: 17nMAssay Description:Inhibition of gamma secretase (unknown origin) assessed as reduction in amyloid beta levels by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM28986(N-{4-[(4-chlorobenzene)sulfonyl]-4-(2,5-difluoroph...)
Affinity DataIC50: 65nMAssay Description:Inhibition of gamma secretase in HEK293 cells expressing APP assessed as reduction in amyloid beta levelsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50100434(tert-butyl (2S,3R,5R)-5-(((S)-1-((S)-1-amino-1-oxo...)
Affinity DataIC50: 115nMAssay Description:Inhibition of full-length human gamma secretase expressed in SH-SY5Y spbetaA4CTF cells assessed as reduction in amyloid beta levels after 90 mins by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50478375(CHEBI:86193 | CHEMBL255682)
Affinity DataIC50: 115nMAssay Description:Inhibition of gamma secretase in human primary neuronal cells assessed as reduction in amyloid beta 40More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533420(CHEMBL4560794)
Affinity DataIC50: 150nMAssay Description:Modulation of gamma secretase in HEK cells expressing APP Swedish mutant assessed as reduction in amyloid beta levels after 5 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM28922((2S)-N-(5-chlorothiophen-2-yl)-4,4,4-trifluoro-1-h...)
Affinity DataIC50: 209nMAssay Description:Inhibition of gamma secretase (unknown origin) mediated Notch M1726V mutant activation in CHO K1 cells after 48 hrs by chemiluminescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50478375(CHEBI:86193 | CHEMBL255682)
Affinity DataIC50: 500nMAssay Description:Inhibition of gamma secretase (unknown origin) mediated Notch signaling by cell based luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetDisintegrin and metalloproteinase domain-containing protein 17(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533418(CHEMBL4435465)
Affinity DataIC50: 541nMAssay Description:Inhibition of ADAM17 (unknown origin) assessed as blockage of TNF-alpha sheddingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50110176(CHEMBL3604460)
Affinity DataIC50: 2.30E+3nMAssay Description:Inhibition of gamma secretase mediated Notch delta E activation in human HeLa cells expressing EGFP after 16 hrs by immunofluorescence analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetDisintegrin and metalloproteinase domain-containing protein 17(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533421(CHEMBL4544135)
Affinity DataIC50: 8.10E+3nMAssay Description:Inhibition of ADAM17 (unknown origin) assessed as blockage of TNF-alpha sheddingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533415(CHEMBL149518)
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of gamma secretase mediated amyloid beta level reduction in HEK293 cells expressing APP after 72 hrs by chemiluminescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50172473((2R)-2-(2-fluoro-[1,1'-biphenyl-4-yl])propanoic ac...)
Affinity DataIC50: 1.00E+5nMAssay Description:Modulation of gamma secretase (unknown origin) assessed as reduction in amyloid beta levelsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetProprotein convertase subtilisin/kexin type 7(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533413(CHEMBL3126388)
Affinity DataKi:  0.120nMAssay Description:Inhibition of recombinant C-terminal truncated human SPC7 expressed in drosophila Schneider 2 cells after 1 hr by spectrofluorometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetProprotein convertase subtilisin/kexin type 5(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533413(CHEMBL3126388)
Affinity DataKi:  0.120nMAssay Description:Inhibition of recombinant C-terminal truncated human SPC6 expressed in drosophila Schneider 2 cells after 1 hr by spectrofluorometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetNeuroendocrine convertase 2(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533413(CHEMBL3126388)
Affinity DataKi:  0.360nMAssay Description:Inhibition of recombinant C-terminal truncated human SPC2 expressed in drosophila Schneider 2 cells after 1 hr by spectrofluorometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetFurin(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533413(CHEMBL3126388)
Affinity DataKi:  1nMAssay Description:Inhibition of recombinant C-terminal truncated human SPC1 expressed in drosophila Schneider 2 cells after 1 hr by spectrofluorometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetNeuroendocrine convertase 1(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533413(CHEMBL3126388)
Affinity DataKi:  2nMAssay Description:Inhibition of recombinant C-terminal truncated human SPC3 expressed in drosophila Schneider 2 cells after 1 hr by spectrofluorometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetProprotein convertase subtilisin/kexin type 6(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50533413(CHEMBL3126388)
Affinity DataKi:  3.60nMAssay Description:Inhibition of recombinant C-terminal truncated human SPC4 expressed in drosophila Schneider 2 cells after 1 hr by spectrofluorometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed