BDBM28922 (2S)-N-(5-chlorothiophen-2-yl)-4,4,4-trifluoro-1-hydroxy-3-(trifluoromethyl)butane-2-sulfonamido::Begacestat::GSI-953

SMILES OC[C@@H](NS(=O)(=O)c1ccc(Cl)s1)C(C(F)(F)F)C(F)(F)F

InChI Key InChIKey=PSXOKXJMVRSARX-UHFFFAOYSA-N

Data  7 IC50  3 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 10 hits for monomerid = 28922   

LigandPNGBDBM28922((2S)-N-(5-chlorothiophen-2-yl)-4,4,4-trifluoro-1-h...)
Affinity DataEC50:  15nMAssay Description:A Chinese Hamster Ovary cell line stably expressing human beta-APP were aliquoted into a 96-well plate, and after attachment the medium was replaced ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/8/2009
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Nagoya City University

Curated by ChEMBL
LigandPNGBDBM28922((2S)-N-(5-chlorothiophen-2-yl)-4,4,4-trifluoro-1-h...)
Affinity DataIC50: 414nMAssay Description:Inhibition of gamma-secretase (unknown origin) expressed in N2a NL/N cells coexpressing betaAPPNL and NotchdeltaE assessed as Abeta42 secretion by EL...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/31/2020
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Nagoya City University

Curated by ChEMBL
LigandPNGBDBM28922((2S)-N-(5-chlorothiophen-2-yl)-4,4,4-trifluoro-1-h...)
Affinity DataIC50: 203nMAssay Description:Inhibition of gamma-secretase (unknown origin) expressed in N2a NL/N cells coexpressing betaAPPNL and NotchdeltaE assessed as Abeta40 secretion by EL...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/31/2020
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Nagoya City University

Curated by ChEMBL
LigandPNGBDBM28922((2S)-N-(5-chlorothiophen-2-yl)-4,4,4-trifluoro-1-h...)
Affinity DataIC50: 1.60nMAssay Description:Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2020
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Nagoya City University

Curated by ChEMBL
LigandPNGBDBM28922((2S)-N-(5-chlorothiophen-2-yl)-4,4,4-trifluoro-1-h...)
Affinity DataIC50: 11nMAssay Description:Inhibition of gamma-secretase in human IMR32 cell membrane using Notch as substrate after 2 hrs by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2020
Entry Details Article
PubMed
TargetPresenilin-1(Human)
Nagoya City University

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)
Nagoya City University

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)
Nagoya City University

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) assessed as inhibition of Amyloid beta 40 production by cell-based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/21/2023
Entry Details
PubMed
TargetPresenilin-1(Human)
Nagoya City University

Curated by ChEMBL
LigandPNGBDBM28922((2S)-N-(5-chlorothiophen-2-yl)-4,4,4-trifluoro-1-h...)
Affinity DataEC50:  15nMAssay Description:Inhibition of gamma-secretase (unknown origin) assessed as inhibition of Amyloid beta 40 production by cell-free assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/21/2023
Entry Details
PubMed
TargetPresenilin-1(Human)
Nagoya City University

Curated by ChEMBL
LigandPNGBDBM28922((2S)-N-(5-chlorothiophen-2-yl)-4,4,4-trifluoro-1-h...)
Affinity DataEC50:  12nMAssay Description:Inhibition of gamma-secretase (unknown origin) assessed as inhibition of Amyloid beta 42 production by cell-free assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/21/2023
Entry Details
PubMed