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

Found 24 hits in this display   

TargetKelch-like ECH-associated protein 1(Homo sapiens (Human))
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50180850(CHEMBL3819587)
Affinity DataKi:  1nMAssay Description:Inhibition of Cys5-LDEETGEFL-NH2 binding to recombinant human KEAP1 Kelch domain (321 to 609 residues) expressed in Escherichia coli BL21 (DE3) measu...More data for this Ligand-Target Pair
TargetKelch-like ECH-associated protein 1(Homo sapiens (Human))
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50180850(CHEMBL3819587)
Affinity DataIC50:  8nMAssay Description:Inhibition of Cys5-LDEETGEFL-NH2 binding to recombinant human KEAP1 Kelch domain (321 to 609 residues) expressed in Escherichia coli BL21 (DE3) measu...More data for this Ligand-Target Pair
TargetKelch-like ECH-associated protein 1(Homo sapiens (Human))
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM304727(3-(7-methoxy-1-methyl-1H-benzo[d][1,2,3]triazol-5-...)
Affinity DataIC50:  10nMAssay 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
LigandPNGBDBM304727(3-(7-methoxy-1-methyl-1H-benzo[d][1,2,3]triazol-5-...)
Affinity DataIC50: <10nMAssay 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
TargetKelch-like ECH-associated protein 1(Homo sapiens (Human))
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM304748(BDBM304749 | US10144731, Example 34a)
Affinity DataIC50:  24nMAssay 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
In DepthDetails ArticlePubMed
TargetKelch-like ECH-associated protein 1 [321-609](Homo sapiens (Human))
Glaxosmithkline

US Patent
LigandPNGBDBM304748(BDBM304749 | US10144731, Example 34a)
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
In DepthDetails US Patent
TargetKelch-like ECH-associated protein 1 [321-609](Homo sapiens (Human))
Glaxosmithkline

US Patent
LigandPNGBDBM304748(BDBM304749 | US10144731, Example 34a)
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
In DepthDetails US Patent
TargetSolute carrier organic anion transporter family member 1B1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50180850(CHEMBL3819587)
Affinity DataIC50:  2.50E+3nMAssay Description:Inhibition of OATP1B1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBile salt export pump(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50180850(CHEMBL3819587)
Affinity DataIC50:  4.00E+3nMAssay Description:Inhibition of BSEP (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3A(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50180850(CHEMBL3819587)
Affinity DataIC50:  1.00E+4nMAssay Description:Inhibition of PDE3A (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKelch-like ECH-associated protein 1(Homo sapiens (Human))
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50180850(CHEMBL3819587)
Affinity DataKd:  1.30nMAssay Description:Binding affinity to human recombinant N-terminal His6 and Avi-tagged KEAP1 (321 to 609 residues) expressed in baculovirus infected sf9 cells by isoth...More data for this Ligand-Target Pair
TargetNuclear factor erythroid 2-related factor 2(Homo sapiens (Human))
Glaxosmithkline

US Patent
LigandPNGBDBM304748(BDBM304749 | US10144731, Example 34a)
Affinity DataEC50:  550nMAssay 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
In DepthDetails US Patent
TargetNuclear factor erythroid 2-related factor 2(Homo sapiens (Human))
Glaxosmithkline

US Patent
LigandPNGBDBM50180850(CHEMBL3819587)
Affinity DataEC50:  12nMAssay Description:Inhibition of KEAP1/NRF2 interaction in human BEAS2B cells assessed as induction of NQO1 specific activity incubated for 48 hrs measured on day 4 pos...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNuclear factor erythroid 2-related factor 2(Homo sapiens (Human))
Glaxosmithkline

US Patent
LigandPNGBDBM50180850(CHEMBL3819587)
Affinity DataEC50:  22nMAssay Description:Inhibition of KEAP1/NRF2 interaction in human bronchial epithelial cells from COPD patient assessed as induction of NQO1 mRNA expression incubated fo...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNuclear factor erythroid 2-related factor 2(Homo sapiens (Human))
Glaxosmithkline

US Patent
LigandPNGBDBM50180850(CHEMBL3819587)
Affinity DataEC50:  36nMAssay Description:Inhibition of KEAP1/NRF2 interaction in human bronchial epithelial cells from COPD patient assessed as induction of GCLM mRNA expression incubated fo...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNuclear factor erythroid 2-related factor 2(Homo sapiens (Human))
Glaxosmithkline

US Patent
LigandPNGBDBM50180850(CHEMBL3819587)
Affinity DataEC50:  16nMAssay Description:Inhibition of KEAP1/NRF2 interaction in human bronchial epithelial cells from COPD patient assessed as induction of HO-1 mRNA expression incubated fo...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNuclear factor erythroid 2-related factor 2(Homo sapiens (Human))
Glaxosmithkline

US Patent
LigandPNGBDBM50180850(CHEMBL3819587)
Affinity DataEC50:  27nMAssay Description:Inhibition of KEAP1/NRF2 interaction in human bronchial epithelial cells from COPD patient assessed as induction of TXNRD1 mRNA expression incubated ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNuclear factor erythroid 2-related factor 2(Homo sapiens (Human))
Glaxosmithkline

US Patent
LigandPNGBDBM304727(3-(7-methoxy-1-methyl-1H-benzo[d][1,2,3]triazol-5-...)
Affinity DataEC50:  11nMAssay 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))
Glaxosmithkline

US Patent
LigandPNGBDBM304748(BDBM304749 | US10144731, Example 34a)
Affinity DataEC50:  83nMAssay 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
In DepthDetails ArticlePubMed
TargetKelch-like ECH-associated protein 1(Homo sapiens (Human))
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50180850(CHEMBL3819587)
Affinity DataEC50:  1.90E+3nMAssay Description:Binding affinity to recombinant human KEAP1 Kelch domain (321 to 609 residues) expressed in Escherichia coli BL21 (DE3) assessed as thermal stabiliza...More data for this Ligand-Target Pair
TargetKelch-like ECH-associated protein 1(Homo sapiens (Human))
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50180850(CHEMBL3819587)
Affinity DataKd:  1.40nMAssay Description:Binding affinity to recombinant human KEAP1 Kelch domain (321 to 609 residues) expressed in Escherichia coli BL21 (DE3) by surface plasmon resonance ...More data for this Ligand-Target Pair
TargetKelch-like ECH-associated protein 1(Homo sapiens (Human))
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50180850(CHEMBL3819587)
Affinity DataKd:  1.60nMAssay Description:Binding affinity to recombinant human KEAP1 Kelch domain (321 to 609 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation rate...More data for this Ligand-Target Pair
TargetNuclear factor erythroid 2-related factor 2(Homo sapiens (Human))
Glaxosmithkline

US Patent
LigandPNGBDBM304727(3-(7-methoxy-1-methyl-1H-benzo[d][1,2,3]triazol-5-...)
Affinity DataEC50:  55nMAssay 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
TargetNuclear factor erythroid 2-related factor 2(Homo sapiens (Human))
Glaxosmithkline

US Patent
LigandPNGBDBM304748(BDBM304749 | US10144731, Example 34a)
Affinity DataEC50:  550nMAssay 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
In DepthDetails US Patent