Compile Data Set for Download or QSAR
maximum 50k data

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

Found 20 hits in this display   

TargetBeta-secretase 1(Homo sapiens (Human))
Janssen Research & Development

Curated by ChEMBL
LigandPNGBDBM223395(US9315520, 1 | US9315520, Comparator 1 | US9315520...)
Affinity DataIC50:  5nMAssay Description:Inhibition of BACE1 in human H4 cells transfected with APP695 assessed as reduction in APP level incubated for 18 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Janssen Research & Development

Curated by ChEMBL
LigandPNGBDBM223395(US9315520, 1 | US9315520, Comparator 1 | US9315520...)
Affinity DataIC50:  5.10nMAssay 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 DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Janssen Research & Development

Curated by ChEMBL
LigandPNGBDBM223395(US9315520, 1 | US9315520, Comparator 1 | US9315520...)
Affinity DataIC50:  7.30nMAssay Description:Displacement of [3H]-PF-6475886 from recombinant human full length FL-tagged BACE1 expressed in HEK293 cell membranes after 30 mins by parallel scint...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Janssen Research & Development

Curated by ChEMBL
LigandPNGBDBM223395(US9315520, 1 | US9315520, Comparator 1 | US9315520...)
Affinity DataIC50:  31nMAssay Description:Beta-secretase (BACE) is one of the enzymes involved in the generation of the amyloid beta peptide found in the amyloid plaques of Alzheimer's Di...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBeta-secretase 1(Homo sapiens (Human))
Janssen Research & Development

Curated by ChEMBL
LigandPNGBDBM223395(US9315520, 1 | US9315520, Comparator 1 | US9315520...)
Affinity DataIC50:  37nMAssay Description:Inhibition of human BACE1 using biotin-GLTNIKTEEISEISYEVEFR-C[Oregon green]KK-OH as substrate after 3 hrs by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIsoform D of Beta-secretase 1 (BACE-I-432)(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM223395(US9315520, 1 | US9315520, Comparator 1 | US9315520...)
Affinity DataIC50:  41nMpH: 4.5 T: 2°CAssay Description:The substrate is Biotin-GLTNIKTEEISEISY^EVEFR-C[Oregon Green]KK-OH. The BACE1 enzyme is affinity purified material from conditioned media of CHO-K1 c...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBeta-secretase 1(Homo sapiens (Human))
Janssen Research & Development

Curated by ChEMBL
LigandPNGBDBM223395(US9315520, 1 | US9315520, Comparator 1 | US9315520...)
Affinity DataIC50:  41nMAssay Description:Inhibition of BACE1 (unknown origin) expressed in CHO-K1 cells using Biotin-GLTNIKTEEISEISYAEVEFR-C[Oregon Green]KK-OH as substrate incubated for 3 h...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Janssen Research & Development

Curated by ChEMBL
LigandPNGBDBM223395(US9315520, 1 | US9315520, Comparator 1 | US9315520...)
Affinity DataIC50:  41nMAssay Description:Beta-secretase (BACE) is one of the enzymes involved in the generation of the amyloid beta peptide found in the amyloid plaques of Alzheimer's Di...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetIsoform D of Beta-secretase 1 (BACE-I-432)(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM223395(US9315520, 1 | US9315520, Comparator 1 | US9315520...)
Affinity DataIC50:  73nMpH: 4.5 T: 2°CAssay Description:The substrate is Biotin-GLTNIKTEEISEISY^EVEFR-C[Oregon Green]KK-OH. The BACE1 enzyme is affinity purified material from conditioned media of CHO-K1 c...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBeta-secretase 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM223395(US9315520, 1 | US9315520, Comparator 1 | US9315520...)
Affinity DataIC50:  194nMAssay Description:Displacement of [3H]-PF-6475886 from recombinant human full length Myc-DDK-tagged BACE2 expressed in HEK293 cell membranes after 30 mins by parallel ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM223395(US9315520, 1 | US9315520, Comparator 1 | US9315520...)
Affinity DataIC50:  238nMAssay Description:Inhibition of human BACE2 using biotin-GLTNIKTEEISEISYEVEFR-C[Oregon green]KK-OH as substrate after 3 hrs by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM223395(US9315520, 1 | US9315520, Comparator 1 | US9315520...)
Affinity DataIC50:  9.90E+3nMAssay Description:Inhibition of human ERG expressed in CHOK1 cells for 5 mins at -80 mV holding potential by patch clamp methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM223395(US9315520, 1 | US9315520, Comparator 1 | US9315520...)
Affinity DataIC50:  9.90E+3nMT: 2°CAssay Description:All testing was carried out in CHO cells transfected with the hERG gene purchased from Millipore (PrecisION hERG-CHO Recombinant Cell Line CYL3038). ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM223395(US9315520, 1 | US9315520, Comparator 1 | US9315520...)
Affinity DataIC50:  9.90E+3nMAssay Description:Inhibition of human ERG expressed in CHO cells at holding potential of -80 mV by patch clamp methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM223395(US9315520, 1 | US9315520, Comparator 1 | US9315520...)
Affinity DataIC50:  2.36E+4nMT: 2°CAssay Description:All testing was carried out in CHO cells transfected with the hERG gene purchased from Millipore (PrecisION hERG-CHO Recombinant Cell Line CYL3038). ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCytochrome P450 2D6(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM223395(US9315520, 1 | US9315520, Comparator 1 | US9315520...)
Affinity DataIC50: >3.00E+4nMAssay Description:CYP2D6 inhibition was obtained by measuring inhibition of 5 uM Dextromethorphan in pooled HLM (HL-MIX-102).More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCytochrome P450 2D6(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM223395(US9315520, 1 | US9315520, Comparator 1 | US9315520...)
Affinity DataIC50: >3.00E+4nMAssay Description:CYP2D6 inhibition was obtained by measuring inhibition of 5 uM Dextromethorphan in pooled HLM (HL-MIX-102).More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCathepsin D(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM223395(US9315520, 1 | US9315520, Comparator 1 | US9315520...)
Affinity DataIC50: >9.53E+4nMAssay Description:Inhibition of Cathepsin D (unknown origin) by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Janssen Research & Development

Curated by ChEMBL
LigandPNGBDBM223395(US9315520, 1 | US9315520, Comparator 1 | US9315520...)
Affinity DataIC50: >1.00E+5nMAssay Description:The BACE1 and BACE2 binding assays measured beta-site amyloid precursor protein-cleaving enzyme (BACE) binding as a decrease in the counts of radioli...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetIsoform D of Beta-secretase 1 (BACE-I-432)(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM223395(US9315520, 1 | US9315520, Comparator 1 | US9315520...)
Affinity DataIC50: >1.00E+5nMpH: 4.5 T: 2°CAssay Description:The substrate is Biotin-GLTNIKTEEISEISY^EVEFR-C[Oregon Green]KK-OH. The BACE1 enzyme is affinity purified material from conditioned media of CHO-K1 c...More data for this Ligand-Target Pair
In DepthDetails US Patent