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

Found 4 hits in this display   

TargetKelch-like ECH-associated protein 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM304728(3-(7-methoxy-1-methyl-1H-benzo[d][1,2,3]triazol-5-...)
Affinity DataIC50:  42nMAssay Description:Displacement of 5'-TAMRA-labelled NRF2 peptide from human N-terminal His6-tagged KEAP1 Kelch domain (321 to 609 residues) expressed in baculovirus in...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetKelch-like ECH-associated protein 1 [321-609](Homo sapiens (Human))
Glaxosmithkline

US Patent
LigandPNGBDBM304728(3-(7-methoxy-1-methyl-1H-benzo[d][1,2,3]triazol-5-...)
Affinity DataIC50:  55nMAssay Description:100 nL of 100× compound dose response curves (serial 3-fold dilutions) in DMSO are stamped using an Echo liquid handling system (Labcyte) into 384-we...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetNuclear factor erythroid 2-related factor 2(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM304728(3-(7-methoxy-1-methyl-1H-benzo[d][1,2,3]triazol-5-...)
Affinity DataEC50:  760nMAssay Description:Activation of Nrf2 in human BEAS2B cells assessed as increase in NQO1 enzymatic activity measured after 48 hrs by MTT assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNuclear factor erythroid 2-related factor 2(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM304728(3-(7-methoxy-1-methyl-1H-benzo[d][1,2,3]triazol-5-...)
Affinity DataEC50:  5.50E+3nMAssay Description:NAD(P)H:quinone oxidoreductase 1 (NQO1), also called DT diaphorase, is a homodimeric FAD-containing enzyme that catalyzes obligatory NAD(P)H-dependen...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent