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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)

Found 8 hits in this display   

TargetBeta-secretase 1(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM41542(US8865911, 122)
Affinity DataKi:  26nMAssay Description:Inhibition of recombinant human BACE1 (1 to 460 residues) using CEVNLDAEFK as substrate preincubated for 10 mins followed by substrate addition measu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 2(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM41542(US8865911, 122)
Affinity DataKi:  372nMAssay Description:Inhibition of human BACE2 (1 to 473 residues) using CEVNLDAEFK as substrate preincubated for 10 mins followed by substrate addition measured after 6....More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAmyloid-beta precursor protein(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM41537(US10231967, Example 114 | US8865911, 114 | US99189...)
Affinity DataIC50:  0.140nMAssay Description:SH-SY5Y cells were cultured in DMEM/F-12 with Glutamax, 10% FCS and 1% non-essential amino acids and cryopreserved and stored at −140° C. at a ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBeta-secretase 1(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM41542(US8865911, 122)
Affinity DataIC50:  0.600nMAssay Description:Inhibition of BACE-1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetBeta-secretase 1 [1-460](Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM41537(US10231967, Example 114 | US8865911, 114 | US99189...)
Affinity DataIC50:  1.20nMAssay Description:The enzyme (truncated form) was diluted to 6 μg/mL (stock 1.3 mg/mL) and the substrate (Europium)CEVNLDAEFK(Qsy7) to 200 nM (stock 120 μM) ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBeta-secretase 1(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM41537(US10231967, Example 114 | US8865911, 114 | US99189...)
Affinity DataIC50:  1.20nMpH: 9.2Assay Description:The beta-secretase enzyme used in the TR-FRET is prepared as follows: The cDNA for the soluble part of the human beta-Secretase (AA 1-AA 460) was clo...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetAmyloid-beta precursor protein(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM41537(US10231967, Example 114 | US8865911, 114 | US99189...)
Affinity DataIC50:  1.20nMAssay Description:The β-secretase enzyme used in the TR-FRET is prepared as follows: The cDNA for the soluble part of the human β-Secretase (AA 1-AA 460) was...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBeta-secretase 1(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM41542(US8865911, 122)
Affinity DataIC50:  25nMpH: 9.2Assay Description:The beta-secretase enzyme used in the TR-FRET is prepared as follows: The cDNA for the soluble part of the human beta-Secretase (AA 1-AA 460) was clo...More data for this Ligand-Target Pair
In DepthDetails US Patent