Compile Data Set for Download or QSAR
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TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM209917(US9273042, 6 | US9556135, 23)
Affinity DataIC50: 0.000200nMT: 2°CAssay Description:The Abeta 40 AlphaLISA Assay can be used. The HEK293 APP cells were seeded in 96 well Microtiter plates in cell culture medium (Iscove's, plus 10% (v...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/25/2017
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM50012660(US9273042, 5 | CHEMBL3261078 | US9556135, 19)
Affinity DataIC50: 0.000900nMT: 2°CAssay Description:The Abeta 40 AlphaLISA Assay can be used. The HEK293 APP cells were seeded in 96 well Microtiter plates in cell culture medium (Iscove's, plus 10% (v...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/25/2017
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM209918(US9273042, 7 | US9556135, 17)
Affinity DataIC50: 0.000900nMT: 2°CAssay Description:The Abeta 40 AlphaLISA Assay can be used. The HEK293 APP cells were seeded in 96 well Microtiter plates in cell culture medium (Iscove's, plus 10% (v...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/25/2017
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM209920(US9273042, 9)
Affinity DataIC50: 0.00100nMT: 2°CAssay Description:The Abeta 40 AlphaLISA Assay can be used. The HEK293 APP cells were seeded in 96 well Microtiter plates in cell culture medium (Iscove's, plus 10% (v...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/25/2017
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM209919(US9273042, 8)
Affinity DataIC50: 0.00180nMT: 2°CAssay Description:The Abeta 40 AlphaLISA Assay can be used. The HEK293 APP cells were seeded in 96 well Microtiter plates in cell culture medium (Iscove's, plus 10% (v...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/25/2017
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM209916(US9273042, 4)
Affinity DataIC50: 0.00570nMT: 2°CAssay Description:The Abeta 40 AlphaLISA Assay can be used. The HEK293 APP cells were seeded in 96 well Microtiter plates in cell culture medium (Iscove's, plus 10% (v...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/25/2017
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM160666(US9045498, 8)
Affinity DataIC50: 0.00600nMAssay Description:Inhibition of BACE1 in human H4 cells expressing wild type APP695 assessed as reduction in soluble APPbeta level after 18 hrs by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/8/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM209915(US9273042, 3 | US9556135, 29)
Affinity DataIC50: 0.00610nMT: 2°CAssay Description:The Abeta 40 AlphaLISA Assay can be used. The HEK293 APP cells were seeded in 96 well Microtiter plates in cell culture medium (Iscove's, plus 10% (v...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/25/2017
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM209914(US9273042, 2)
Affinity DataIC50: 0.00820nMT: 2°CAssay Description:The Abeta 40 AlphaLISA Assay can be used. The HEK293 APP cells were seeded in 96 well Microtiter plates in cell culture medium (Iscove's, plus 10% (v...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/25/2017
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM209913(US9273042, 1)
Affinity DataIC50: 0.0110nMT: 2°CAssay Description:The Abeta 40 AlphaLISA Assay can be used. The HEK293 APP cells were seeded in 96 well Microtiter plates in cell culture medium (Iscove's, plus 10% (v...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/25/2017
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM223332(US9315520, 19 | US9605007, Example 19 | US9744173,...)
Affinity DataIC50: 0.0140nMAssay Description:Inhibition of BACE1 in human H4 cells transfected with wild type APP assessed as reduction in soluble portion of APPbeta level in cells incubated for...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM50398475(CHEMBL2179131)
Affinity DataKi:  0.0170nMAssay Description:Inhibition of recombinant BACE1 expressed in Escherichia coli using Arg- Glu(EDANS)-Glu-Val-Asn-Leu-Asp-Ala-Glu-Phe-Lys(Dabcyl)-Arg as substrate by f...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM50259962(CHEMBL4088234)
Affinity DataIC50: 0.0240nMAssay Description:Inhibition of BACE1 in human H4 cells expressing wild type APP695 assessed as reduction in soluble APPbeta level after 18 hrs by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/8/2020
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM50005021(CHEMBL2408786 | US9650336, Example 3)
Affinity DataIC50: 0.0300nMAssay Description:Inhibition of BACE1 in human SH-SY5Y cells assessed as release of sAPPbeta after 17 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/26/2014
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM50452875(CHEMBL4212046)
Affinity DataIC50: 0.0330nMAssay Description:Inhibition of BACE1 in human H4 cells transfected with wild type APP assessed as reduction in soluble portion of APPbeta level in cells incubated for...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM50452884(CHEMBL4217023)
Affinity DataIC50: 0.0340nMAssay Description:Inhibition of BACE1 in human H4 cells transfected with wild type APP assessed as reduction in soluble portion of APPbeta level in cells incubated for...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM50398472(CHEMBL2179138)
Affinity DataKi:  0.0360nMAssay Description:Inhibition of recombinant BACE1 expressed in Escherichia coli using Arg- Glu(EDANS)-Glu-Val-Asn-Leu-Asp-Ala-Glu-Phe-Lys(Dabcyl)-Arg as substrate by f...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM705875(US20160046618, Example 1001)
Affinity DataIC50: 0.0590nMAssay Description:The cDNAs for both human recombinant BACE1 and BACE2 with C-terminal 6-His Tags were cloned into transient protein expression vectors, which were sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
4/9/2025
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM705874((1S,5S,6S)-3-amino-5-(2-fluoro-5-(5-(2,2,2-trifluo...)
Affinity DataIC50: 0.0700nMAssay Description:The cDNAs for both human recombinant BACE1 and BACE2 with C-terminal 6-His Tags were cloned into transient protein expression vectors, which were sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
4/9/2025
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM50510795(CHEMBL4561849)
Affinity DataIC50: 0.0900nMAssay Description:Inhibition of BACE1 in HEK293 cells harboring APP assessed as reduction in amyloidbeta 40 level incubated for 18 to 20 hrs by AlphaLISA AssayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM705873((1S,5S,6S)-3-amino-N-(2,2-difluoroethyl)-5-(2-fluo...)
Affinity DataIC50: 0.0900nMAssay Description:The cDNAs for both human recombinant BACE1 and BACE2 with C-terminal 6-His Tags were cloned into transient protein expression vectors, which were sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
4/9/2025
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM705833(US20160046618, Example 959)
Affinity DataIC50: 0.0900nMAssay Description:The cDNAs for both human recombinant BACE1 and BACE2 with C-terminal 6-His Tags were cloned into transient protein expression vectors, which were sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
4/9/2025
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM124179(US8754075, 50)
Affinity DataIC50: 0.100nMT: 2°CAssay Description:The assay uses the principle of inhibition of human TMEM27 cleavage by endogenous cellular BACE2 in the Ins1e rat cell line and shedding from the cel...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/11/2014
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM705878(N-(3-((1S,5S,6S)-3-amino-5-methyl-1-(morpholine-4-...)
Affinity DataIC50: 0.100nMAssay Description:The cDNAs for both human recombinant BACE1 and BACE2 with C-terminal 6-His Tags were cloned into transient protein expression vectors, which were sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
4/9/2025
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM705841(US20160046618, Example 967)
Affinity DataIC50: 0.110nMAssay Description:The cDNAs for both human recombinant BACE1 and BACE2 with C-terminal 6-His Tags were cloned into transient protein expression vectors, which were sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
4/9/2025
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM50452883(CHEMBL4203860)
Affinity DataIC50: 0.110nMAssay Description:Inhibition of BACE1 in human H4 cells transfected with wild type APP assessed as reduction in soluble portion of APPbeta level in cells incubated for...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM16254(N2-[(2R,4S,5S)-5-{[N-{[(2,5-dimethyl-1,3-oxazol-4-...)
Affinity DataKi:  0.120nM ΔG°:  -58.9kJ/molepH: 4.5 T: 2°CAssay Description:Enzyme activities were assayed by monitoring the hydrolysis of substrate in the presence or absence of inhibitor compounds. The hydrolysis was record...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/10/2007
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM16254(N2-[(2R,4S,5S)-5-{[N-{[(2,5-dimethyl-1,3-oxazol-4-...)
Affinity DataKi:  0.120nMAssay Description:Inhibition of recombinant memapsin 2More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM16254(N2-[(2R,4S,5S)-5-{[N-{[(2,5-dimethyl-1,3-oxazol-4-...)
Affinity DataKi:  0.120nMAssay Description:Inhibition of BACE1More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM50231938((2,5-dimethyloxazol-4-yl)methyl (R)-1-((4S,5S,7R)-...)
Affinity DataKi:  0.120nMAssay Description:Binding affinity to recombinant memapsin 2More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/11/2009
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM210070(US9270353, 17)
Affinity DataKi:  0.130nMAssay Description:Displacement of [3H] JNJ-962 from BACE1 (unknown origin) expressed in HEK293 cell membranes assessed as inhibition constant at pH 6.2 by scintillatio...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/4/2023
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM705861(US20160046618, Example 987)
Affinity DataIC50: 0.140nMAssay Description:The cDNAs for both human recombinant BACE1 and BACE2 with C-terminal 6-His Tags were cloned into transient protein expression vectors, which were sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
4/9/2025
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM705872(N-(3-((1S,5S,6S)-3-amino-5-methyl-1-(morpholine-4-...)
Affinity DataIC50: 0.146nMAssay Description:The cDNAs for both human recombinant BACE1 and BACE2 with C-terminal 6-His Tags were cloned into transient protein expression vectors, which were sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
4/9/2025
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM589176(US11548903, Example 109)
Affinity DataIC50: 0.149nMAssay Description:The cDNAs for both human recombinant BACE1 and 2 with C-terminal 6-His Tags were cloned into transient protein expression vectors, which were subsequ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/6/2023
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM50387062(CHEMBL2047041)
Affinity DataIC50: 0.150nMAssay Description:Inhibition of BACE1 expressed in human HEK293 cells expressing Swedish mutant APP assessed as reduction on amyloid beta (1 to 40) production after 24...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/8/2013
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM50398266(CHEMBL2177305)
Affinity DataIC50: 0.150nMAssay Description:Inhibition of BACE1 in human SH-SY5Y cells assessed as inhibition of sAPPbeta release after 16 hrs by immunoassayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM50510787(CHEMBL4564324)
Affinity DataIC50: 0.157nMAssay Description:Inhibition of BACE1 in human SH-SY5Y cells transfected with APP695 assessed as reduction in amyloidbeta (1 to 40 residues) incubated for 24 hrs by sa...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM50393088(CHEMBL2152903)
Affinity DataIC50: 0.160nMAssay Description:Inhibition of BACE1 in human SH-SY5Y cells assessed as inhibition of sAPPbeta release after 16 hrs by immunoassayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM149939(US8975415, 221 | US9242973, 221)
Affinity DataIC50: 0.160nMT: 2°CAssay Description:Test Example 3: The potency of compounds against BACE1 activity was determined in a cellular assay of Aβ production. Human SK-N-BE(2) neuroblast...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/5/2016
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM705631((E)-3-((1R,5S,6S)-3-amino-5-(5-(5-chloropicolinami...)
Affinity DataIC50: 0.176nMAssay Description:The cDNAs for both human recombinant BACE1 and BACE2 with C-terminal 6-His Tags were cloned into transient protein expression vectors, which were sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
4/9/2025
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM705942(US20160046618, Example 1068)
Affinity DataIC50: 0.178nMAssay Description:The cDNAs for both human recombinant BACE1 and BACE2 with C-terminal 6-His Tags were cloned into transient protein expression vectors, which were sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
4/9/2025
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM589190(US11548903, Example 120)
Affinity DataIC50: 0.186nMAssay Description:The cDNAs for both human recombinant BACE1 and 2 with C-terminal 6-His Tags were cloned into transient protein expression vectors, which were subsequ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/6/2023
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM705837(US20160046618, Example 963)
Affinity DataIC50: 0.194nMAssay Description:The cDNAs for both human recombinant BACE1 and BACE2 with C-terminal 6-His Tags were cloned into transient protein expression vectors, which were sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
4/9/2025
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM705843(US20160046618, Example 969)
Affinity DataIC50: 0.197nMAssay Description:The cDNAs for both human recombinant BACE1 and BACE2 with C-terminal 6-His Tags were cloned into transient protein expression vectors, which were sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
4/9/2025
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM705793(US20160046618, Example 919)
Affinity DataIC50: 0.199nMAssay Description:The cDNAs for both human recombinant BACE1 and BACE2 with C-terminal 6-His Tags were cloned into transient protein expression vectors, which were sub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
4/9/2025
Entry Details
US Patent

TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM50012629(CHEMBL3261045)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of Fc domain of IgG1-fused human BACE (1 to 460) expressed in HEK293 cells preincubated for 10 mins followed by substrate addition measure...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2015
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM50012615(CHEMBL3260839)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of BACE1 (unknown origin) incubated for 1 hr prior to testing measured after 1 hr by FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2015
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM50510993(CHEMBL4437161)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of BACE1 (unknown origin) using FRET peptide substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by FRE...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM50393088(CHEMBL2152903)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of BACE1 by secreted AAPbeta release assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Hoffmann-La Roche

US Patent
LigandPNGBDBM50061831(CHEMBL3394227)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of human recombinant BACE1 pre-incubated with enzyme for 60 mins before fluorescent substrate addition FRET methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/4/2016
Entry Details Article
PubMed
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