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Found 21 Enz. Inhib. hit(s) with Target = 'Ketohexokinase' and Ligand = 'BDBM319585'
TargetKetohexokinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM319585(US10174007, Example 4 | US10787438, Example 4 | US...)
Affinity DataKi:  4.5nMAssay Description:Mixed noncompetitive inhibition of recombinant human N-terminal His-tagged KHKC expressed in Escherichia coli BL21 (DE3) using fructose as substrate ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKetohexokinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM319585(US10174007, Example 4 | US10787438, Example 4 | US...)
Affinity DataIC50:  8.40nMAssay Description:Assay B, using 10-fold less enzyme and measuring absorbance for 3 hours to obtain IC50 values below the 10 nM lower limit of Assay A. Compounds were ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetKetohexokinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM319585(US10174007, Example 4 | US10787438, Example 4 | US...)
Affinity DataIC50:  8.40nMAssay Description:Assay B, using 10-fold less enzyme and measuring absorbance for 3 hours to obtain IC50 values below the 10 nM lower limit of Assay A. Compounds were ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetKetohexokinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM319585(US10174007, Example 4 | US10787438, Example 4 | US...)
Affinity DataIC50:  8.40nMAssay Description:Compounds having an IC50 value less than 20 nM were examined in a second KHK assay, referred to as Assay B, using 10-fold less enzyme and measuring a...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetKetohexokinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM319585(US10174007, Example 4 | US10787438, Example 4 | US...)
Affinity DataIC50:  8.40nMAssay Description:Using 10-fold less enzyme and measuring absorbance for 3 hours to obtain IC50 values below the 10 nM lower limit of Assay A. Compounds were prepared ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetKetohexokinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM319585(US10174007, Example 4 | US10787438, Example 4 | US...)
Affinity DataIC50:  10nMAssay Description:Inhibition of KHK (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetKetohexokinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM319585(US10174007, Example 4 | US10787438, Example 4 | US...)
Affinity DataIC50:  10nMAssay Description:Inhibition of 1 nM recombinant human N-terminal His-tagged KHKC expressed in Escherichia coli BL21 (DE3) using fructose as substrate preincubated for...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKetohexokinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM319585(US10174007, Example 4 | US10787438, Example 4 | US...)
Affinity DataIC50:  14nMAssay Description:Inhibition of recombinant His-tagged human KHK expressed in Escherichia coli in presence of NADPHMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKetohexokinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM319585(US10174007, Example 4 | US10787438, Example 4 | US...)
Affinity DataIC50:  14.2nMAssay Description:Assay A, a 384-well format on a Corning 3653 assay plate is used, and monitored by UV-vis spectroscopy in continuous mode at rt. Compounds were prepa...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetKetohexokinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM319585(US10174007, Example 4 | US10787438, Example 4 | US...)
Affinity DataIC50:  14.2nMAssay Description:Assay A, a 384-well format on a Corning 3653 assay plate is used, and monitored by UV-vis spectroscopy in continuous mode at rt. Compounds were prepa...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetKetohexokinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM319585(US10174007, Example 4 | US10787438, Example 4 | US...)
Affinity DataIC50:  14.2nMAssay Description:A 384-well format on a Corning 3653 assay plate is used, and monitored by UV-vis spectroscopy in continuous mode at rt. Compounds were prepared in DM...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetKetohexokinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM319585(US10174007, Example 4 | US10787438, Example 4 | US...)
Affinity DataIC50:  14.2nMAssay Description:A 384-well format on a Corning 3653 assay plate is used, and monitored by UV-vis spectroscopy in continuous mode at rt. Compounds were prepared in DM...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetKetohexokinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM319585(US10174007, Example 4 | US10787438, Example 4 | US...)
Affinity DataIC50:  28nMAssay Description:Inhibition of recombinant human N-terminal His-tagged KHKC expressed in Escherichia coli BL21 (DE3) using 8 mM fructose as substrate preincubated for...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKetohexokinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM319585(US10174007, Example 4 | US10787438, Example 4 | US...)
Affinity DataIC50:  37.3nMAssay Description:Assay C, was performed at high fructose and ATP concentrations, conditions that would be more consistent with physiological concentrations of the nat...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetKetohexokinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM319585(US10174007, Example 4 | US10787438, Example 4 | US...)
Affinity DataIC50:  37.3nMAssay Description:A third KHK assay, referred to as Assay C, was performed at high fructose and ATP concentrations, conditions that would be more consistent with physi...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetKetohexokinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM319585(US10174007, Example 4 | US10787438, Example 4 | US...)
Affinity DataIC50:  37.3nMAssay Description:Assay C, was performed at high fructose and ATP concentrations, conditions that would be more consistent with physiological concentrations of the nat...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetKetohexokinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM319585(US10174007, Example 4 | US10787438, Example 4 | US...)
Affinity DataIC50:  37.3nMAssay Description:Assay C was performed at high fructose and ATP concentrations, conditions that would be more consistent with physiological concentrations of the natu...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetKetohexokinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM319585(US10174007, Example 4 | US10787438, Example 4 | US...)
Affinity DataIC50:  66nMAssay Description:A fourth assay, referred to as Assay D, was performed using human KHK-A to assess the potency of compounds in inhibiting activity of this enzyme. Com...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetKetohexokinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM319585(US10174007, Example 4 | US10787438, Example 4 | US...)
Affinity DataIC50:  66nMAssay Description:Assay D was performed using human KHK-A to assess the potency of compounds in inhibiting activity of this enzyme. Compounds were prepared in DMSO as ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetKetohexokinase(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM319585(US10174007, Example 4 | US10787438, Example 4 | US...)
Affinity DataIC50:  170nMAssay Description:Inhibition of recombinant human N-terminal His-tagged KHKA expressed in Escherichia coli BL21 (DE3) using 8 mM fructose as substrate preincubated for...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKetohexokinase(Rattus norvegicus)
Pfizer

Curated by ChEMBL
LigandPNGBDBM319585(US10174007, Example 4 | US10787438, Example 4 | US...)
Affinity DataIC50:  210nMAssay Description:Inhibition of recombinant rat N-terminal His-tagged KHK expressed in Escherichia coli BL21 (DE3) using 8 mM fructose as substrate preincubated for 30...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed