| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA1924715 | B | Inhibition of LTC4 synthase | 1 | single protein format | Scientific Literature | |||
| 2. | ALA1743238 | A | Substrates for human microsomal glutathione transferase LTC4S | Homo sapiens | 1 | assay format | Scientific Literature | ||
| 3. | ALA2389915 | B | Inhibition of LTC4S (unknown origin) | Homo sapiens | 1 | single protein format | Scientific Literature | ||
| 4. | ALA3880639 | B | Inhibition of recombinant human LTC4 synthase expressed in Pichia pastoris using LTA4 as substrate preincubated for 10 mins followed by substrate addition measured after 5 mins by HTRF method | Homo sapiens | 41 | assay format | Patent Bioactivity Data | ||
| 5. | ALA3880641 | B | Inhibition of recombinant human LTC4 synthase expressed in Pichia pastoris using LTA4 as substrate preincubated for 10 mins followed by substrate addition measured after 1 min by HTRF method | Homo sapiens | 3 | assay format | Patent Bioactivity Data | ||
| 6. | ALA3888328 | B | In Vitro hLTC4 Synthase Enzyme Assay (Test A): In the assay, LTC4 synthase catalyses the reaction where the substrate LTA4 is converted to LTC4. Recombinant human LTC4 synthase is expressed in Piccia pastoralis and the purified enzyme is dissolved in 25 mM tris-buffer pH 7.8 supplemented with 0.1 mM glutathione (GSH) and stored at −80 °C. In order to obtain IC50-values for the compounds, the following procedure was used: A volume (24 μL) of 0.25 g/mL LTC4 synthase in 75 mM tris (pH ~8.5), 0.5 mM MgCl2 and 3 mM GSH was preincubated for 10 min with 0.5 μL of compound of interest in DMSO at ten different concentrations, typically in the range 10^−9,5-10^−5 M as well as with DMSO only. The buffer is used as background. Runs are performed in duplicates. The enzymatic reaction is initiated by addition of 0.5 μL LTA4 in diglyme (final assay concentration 8 μM). The reaction is stopped after 1 min by addition of double the reaction volume of a stop solution (MeOH:H2O:acetic acid 70:30:1). | Homo sapiens | 60 | assay format | BindingDB Database | ||
| 7. | ALA3888329 | B | In Vitro hLTC4 Synthase Enzyme Assay (Test B): In the assay, LTC4 synthase catalyses the reaction where the substrate LTA4 methyl ester is converted to LTC4 methyl ester. In order to obtain IC50-values for the compounds, the following procedure was used: 10 mL of 0.6 nM of human recombinant purified LTC4 synthase expressed from Pichia Pastoris in buffer 50 mM tris (pH 7.5), 0.05% BSA 0.03% DD M 100 mM NaCl was preincubated for 30 min with 10 mL of substrate mix containing 6 mM LTA4-methyl ester substrate and 1 mM glutathione in 50 mM Tris pH7.5 0.05% BSA 0.03% DDM 100 mM NaCl together with 0.1 μL of compound of interest in DMSO at ten different concentrations, typically in the range 10^−9,5-10^−5 M as well as with DMSO only. The enzymatic reaction is initiated by addition of 10 μL LTC4S enzyme solution to 10 μL substrate solution to the assay plate containing 0.5 mL of compound in DMSO or 0.5 mL DMSO control. The reaction is stopped after 30 min by addition of 40 μL 75% (w/v) acetonitrile in H2O. | Homo sapiens | 4 | single protein format | BindingDB Database | ||
| 8. | ALA4231617 | B | Inhibition of LTC4 synthase in LPS/fMLP-stimulated human monocytes assessed as decrease in cys-LT formation pre-incubated with LPS for 30 mins and later stimulated with fMLP for 10 mins by ELISA | Homo sapiens | 1 | cell-based format | Scientific Literature | ||
| 9. | ALA4231623 | B | Inhibition of human LTC4 synthase expressed in HEK293 cell microsomes preincubated for 10 mins followed by LTA4-methyl ester addition and measured after 10 mins by UPLC-MS/MS analysis | Homo sapiens | 2 | assay format | Scientific Literature | ||
| 10. | ALA4273638 | B | Inhibition of LTC4 synthase (unknown origin) | Homo sapiens | 1 | single protein format | Scientific Literature | ||
| 11. | ALA4378183 | B | Inhibition of human N-terminal His6-tagged LTC4S expressed in Pichia pastoris X33 using LTA4 methyl ester and glutathione as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by LC-MS/MS analysis | Homo sapiens | 34 | assay format | Scientific Literature | ||
| 12. | ALA4378184 | B | Inhibition of LTC4S in zymosan-stimulated human PBMC assessed as inhibition of LTC4 production preincubated for 45 mins followed by zymosan stimulation and measured after 20 mins by LC-MS/MS analysis | Homo sapiens | 32 | single protein format | Scientific Literature | ||
| 13. | ALA4378187 | B | Inhibition of LTC4S in zymosan-stimulated human PBMC assessed as unbound drug concentration required for inhibition of LTC4 production preincubated for 45 mins followed by zymosan stimulation and measured after 20 mins by LC-MS/MS analysis | Homo sapiens | 2 | single protein format | Scientific Literature | ||
| 14. | ALA4378216 | B | Inhibition of LTC4S in healthy human whole blood assessed as inhibition of calcium ionophore A23187 stimulated cysteinyl leukotrienes production preincuabted for 30 mins followed by calcium ionophore stimulation and measured after 10 mins by LC-MS analysis | Homo sapiens | 3 | tissue-based format | Scientific Literature | ||
| 15. | ALA4378217 | B | Inhibition of LTC4S in asthmatic human whole blood assessed as inhibition of calcium ionophore A23187 stimulated cysteinyl leukotrienes production preincuabted for 30 mins followed by calcium ionophore stimulation and measured after 10 mins by LC-MS analysis | Homo sapiens | 3 | tissue-based format | Scientific Literature | ||
| 16. | ALA4378222 | B | Inhibition of recombinant human N-terminal His6-tagged LTC4S expressed in in Pichia pastoris X33 assessed as inhibition of EXC4 formation using EXA4 as substrate preincubated for 10 mins followed by substrate addition and measured after 1 min by EIA | Homo sapiens | 2 | assay format | Scientific Literature | ||
| 17. | ALA4880872 | B | Leukotriene LTC4 Synthase Eurofins-Panlabs enzyme assay | Cavia porcellus | 2 | single protein format | Donated Chemical Probes - SGC Frankfurt | ||
| 18. | ALA5158736 | B | Inhibition of human recombinant LTC4S expressed in HEK293 cell microsomal fraction preincubated for 10 mins followed by LTA4-methyl ester addition and measured after 10 mins by UPLC-MS/MS analysis | Homo sapiens | 3 | microsome format | Scientific Literature | ||
| 19. | ALA5158738 | B | Inhibition of recombinant LTC4S (unknown origin) expressed in COS cells | Homo sapiens | 1 | cell-based format | Scientific Literature |
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