# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA1810789 | B | Inhibition of KHK-mediated conversion of D-fructose to fructose-1-phosphate after 60 mins by high throughput mass spectrometry analysis | 42 | single protein format | Scientific Literature | |||
2. | ALA2019654 | B | Inhibition of human ketohexokinase isoform C expressed in Escherichia coli BL21 (DE3) cells using D-fructose as substrate after 12 to 15 mins by fluorescence polarization assay | Homo sapiens | 49 | cell-based format | Scientific Literature | ||
3. | ALA2019655 | B | Inhibition of ketokinase isoform C in human HepG2 cells assessed as levels of fructose-1-phosphate preincubated for 30 mins followed by substrate addition measured after 3 hrs by LC-MS analysis | Homo sapiens | 8 | cell-based format | Scientific Literature | ||
4. | ALA2065101 | B | Inhibition of recombinant human hepatic KHKC | Homo sapiens | 19 | single protein format | Scientific Literature | ||
5. | ALA2065102 | B | Inhibition of KHKC in human HepG2 cells assessed as level of fructose-1-phosphate | Homo sapiens | 2 | cell-based format | Scientific Literature | ||
6. | ALA1273541 | B | Inhibition of ketohexokinase assessed as conversion of D-fructose to fructose-1-phosphate after 60 mins | 1 | single protein format | Scientific Literature | |||
7. | ALA3705469 | B | Enzyme Assay: An enzymatic assay was developed to measure KHK-mediated conversion of D-fructose to Fructose-1-P (F-1-P) using High Throughput Mass Spectroscopy (HTMS) as a means of product detection. This assay served as a primary screen to evaluate the ability to inhibit KHK enzyme activity and it has been adapted to high throughput mass spectrometry (HTMS, BioTrove RapidFire) format for higher throughput.The compounds to be tested were dosed in 12-points concentration from 511 uM to 0.5 uM. Inhibition of the fragment, IC50, was determined in a dose-response curve under the established steady-state conditions of 200 uM fructose, 100 uM ATP and 2 nM KHK for 60 min at 25 C. The assay was carried out in 384-well plate format. | 154 | organism-based format | BindingDB Database | |||
8. | ALA4019530 | B | Inhibition of recombinant human N-terminal His-tagged KHK-C expressed in Escherichia coli BL21(DE3) using fructose as substrate incubated for 30 mins followed by ATP addition measured for 30 mins by pyruvate kinase-lactate dehydrogenase coupled enzyme assay | Homo sapiens | 1 | assay format | Scientific Literature | ||
9. | ALA4019531 | B | Binding affinity to full length recombinant human biotin-labeled KHK by SPR assay | Homo sapiens | 4 | single protein format | Scientific Literature | ||
10. | ALA4019532 | B | Inhibition of recombinant human N-terminal His-tagged KHK expressed in Escherichia coli BL21(DE3) using fructose as substrate incubated for 30 mins followed by ATP addition measured for 30 mins by pyruvate kinase-lactate dehydrogenase coupled enzyme assay | Homo sapiens | 9 | assay format | Scientific Literature | ||
11. | ALA4019558 | B | Inhibition of recombinant human N-terminal His-tagged KHK-A expressed in Escherichia coli BL21(DE3) using fructose as substrate incubated for 30 mins followed by ATP addition measured for 30 mins by pyruvate kinase-lactate dehydrogenase coupled enzyme assay | Homo sapiens | 1 | assay format | Scientific Literature | ||
12. | ALA4019560 | B | Inhibition of KHK (unknown origin) using D-fructose as substrate after 60 mins in presence of ATP by LC-MS analysis | Homo sapiens | 2 | single protein format | Scientific Literature | ||
13. | ALA4019561 | B | Inhibition of recombinant full length human His-tagged KHK expressed in Escherichia coli BL21(DE3) using at 240 uM by 1D NMR-STD spectroscopic method | Homo sapiens | 4 | assay format | Scientific Literature | ||
14. | ALA4344288 | B | Inhibition of recombinant His-tagged human KHK expressed in Escherichia coli in presence of NADPH | Homo sapiens | 4 | assay format | Scientific Literature | ||
15. | ALA4344289 | B | Binding affinity to recombinant His-tagged human KHK expressed in Escherichia coli in presence of NADPH | Homo sapiens | 2 | assay format | Scientific Literature | ||
16. | ALA4676054 | B | Inhibition of 10 nM recombinant human N-terminal His-tagged KHKC expressed in Escherichia coli BL21 (DE3) using fructose as substrate preincubated for 30 mins followed by ATP addition and measured for 30 mins by pyruvate kinase-lactate dehydrogenase coupled assay | Homo sapiens | 6 | assay format | Scientific Literature | ||
17. | ALA4676055 | B | Inhibition of 1 nM recombinant human N-terminal His-tagged KHKC expressed in Escherichia coli BL21 (DE3) using fructose as substrate preincubated for 30 mins followed by ATP addition and measured for 3 hrs by pyruvate kinase-lactate dehydrogenase coupled assay | Homo sapiens | 3 | assay format | Scientific Literature | ||
18. | ALA4676064 | B | Inhibition of recombinant human N-terminal His-tagged KHKC expressed in Escherichia coli BL21 (DE3) using 8 mM fructose as substrate preincubated for 30 mins followed by 2 mM ATP addition and measured for 30 min by pyruvate kinase-lactate dehydrogenase coupled assay | Homo sapiens | 1 | assay format | Scientific Literature | ||
19. | ALA4676065 | B | Inhibition of recombinant human N-terminal His-tagged KHKA expressed in Escherichia coli BL21 (DE3) using 8 mM fructose as substrate preincubated for 30 mins followed by 2 mM ATP addition and measured for 30 min by pyruvate kinase-lactate dehydrogenase coupled assay | Homo sapiens | 1 | assay format | Scientific Literature | ||
20. | ALA4676073 | B | Mixed noncompetitive inhibition of 10 nM recombinant human N-terminal His-tagged KHKC expressed in Escherichia coli BL21 (DE3) at 0.0016 to 5 uM using fructose as substrate preincubated for 30 mins with ATP and fructose followed by enzyme addition and measured for 30 mins by Lineweaver-burk plot analysis | Homo sapiens | 1 | assay format | Scientific Literature |