| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA3858373 | B | Antagonist activity at recombinant rat P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of Bz-ATP-induced Ca2+ flux preincubated for 30 mins followed by agonist addition measured after 180 sec by calcium-4 dye based FLIPR assay | Rattus norvegicus | 20 | cell-based format | Scientific Literature | ||
| 2. | ALA3858374 | A | Extraction ratio in human liver microsomes at 1 uM upto 60 mins in presence of NDPH by LC/MS/MS analysis | Homo sapiens | 17 | tissue-based format | Scientific Literature | ||
| 3. | ALA3858375 | A | Extraction ratio in rat liver microsomes at 1 uM upto 60 mins in presence of NDPH by LC/MS/MS analysis | Rattus norvegicus | 17 | tissue-based format | Scientific Literature | ||
| 4. | ALA3858376 | B | Antagonist activity at recombinant human P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of Bz-ATP-induced Ca2+ flux preincubated for 30 mins followed by agonist addition measured after 180 sec by calcium-4 dye based FLIPR assay | Homo sapiens | 20 | cell-based format | Scientific Literature | ||
| 5. | ALA3858377 | B | Antagonist activity at recombinant mouse P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of Bz-ATP-induced Ca2+ flux preincubated for 30 mins followed by agonist addition measured after 180 sec by calcium-4 dye based FLIPR assay | Mus musculus | 4 | cell-based format | Scientific Literature | ||
| 6. | ALA3858378 | B | Displacement of [3H]-(S)-7-(2-chloro-3-(trifluoromethyl)benzyl)-6-methyl-3-(pyrazin-2-yl)-6,7-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8(5H)-one from recombinant human P2X7 receptor expressed in human 1321N1 cell membranes after 1 hr | Homo sapiens | 4 | cell-based format | Scientific Literature | ||
| 7. | ALA3858379 | A | Protein binding in human plasma at 1 uM after 6 hrs by LC/MS/MS based equilibrium dialysis method | Homo sapiens | 4 | cell-free format | Scientific Literature | ||
| 8. | ALA3858380 | A | Protein binding in rat plasma at 1 uM after 6 hrs by LC/MS/MS based equilibrium dialysis method | Rattus norvegicus | 4 | cell-free format | Scientific Literature | ||
| 9. | ALA3858382 | A | Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate after 15 mins by LC/MS/MS analysis | Homo sapiens | 3 | tissue-based format | Scientific Literature | ||
| 10. | ALA3858383 | A | Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate after 15 mins by LC/MS/MS analysis | Homo sapiens | 4 | tissue-based format | Scientific Literature | ||
| 11. | ALA3858384 | A | Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate after 15 mins by LC/MS/MS analysis | Homo sapiens | 3 | tissue-based format | Scientific Literature | ||
| 12. | ALA3858385 | A | Inhibition of CYP2C8 in human liver microsomes using paclitaxel as substrate after 15 mins by LC/MS/MS analysis | Homo sapiens | 3 | tissue-based format | Scientific Literature | ||
| 13. | ALA3858386 | A | Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate after 15 mins by LC/MS/MS analysis | Homo sapiens | 3 | tissue-based format | Scientific Literature | ||
| 14. | ALA3858444 | B | Displacement of [3H]astemizole from human ERG expressed in HEK293 cells by competitive binding assay | Homo sapiens | 4 | cell-based format | Scientific Literature | ||
| 15. | ALA3858445 | P | Solubility of compound in phosphate buffer at at pH 2 at 30 degC after 3 days | 4 | small-molecule physicochemical format | Scientific Literature | |||
| 16. | ALA3858446 | P | Solubility of the compound in phosphate buffer at pH 7 at 30 degC after 3 days | 4 | small-molecule physicochemical format | Scientific Literature | |||
| 17. | ALA3889238 | B | Radioligand Binding Assay: human or rat P2X7-1321 N1 cells were collected and frozen @−80° C. On the day of the experiment, cell membrane preparations were made according to standard published methods. The total assay volume was 100 μl: 10 μl compound (10×)+(b) 40 μl tracer (2.5×)+50 μl membrane (2×). The tracer used for the assay was tritiated A-804598. The compound can be prepared as described in the literature. (Donnelly-Roberts, D. Neuropharmacology 2009, 56 (1), 223-229.) Compounds, tracer and membranes were incubated for 1 hour @ 4° C. The assay was terminated by filtration (GF/B filters pre-soaked with 0.3% PEI) and washed with washing buffer (Tris-HCl 50 mM). | 228 | assay format | BindingDB Database | |||
| 18. | ALA3889240 | B | FLIPR Assay: 1321 N1 cells expressing the recombinant human, rat or mouse P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium) high glucose supplemented with 10% Fetal Bovine Serum (FBS) and appropriate selection marker. Cells were seeded at a density of 25000 cells/well (96-well clear bottom black walled plates) in 100 ul volume/well. On the day of the experiment, cell plates were washed with assay buffer, containing (in mM): 130 NaCl, 2 KCl, 1 CaCl2, 1 MgCl2, 10 HEPES, 5 glucose; pH 7.40 and 300 mOs. After the wash, cells were loaded with the Calcium-4 dye (Molecular Device) and incubated in the dark for 60 minutes. Test compounds were prepared at 250ÿ the test concentration in neat DMSO. Intermediate 96-well compound plates were prepared by transferring 1.2 uL of the compound into 300 uL of assay buffer. A further 3x dilution occurred when transferring 50 uL/well of the compound plate to 100 uL/well in the cell plate. Cells were incubate with test compounds and dye for 30 minutes. Calcium dye fluorescence was monitored in FLIPR as the cells were challenged by adding 50 uL/well of BzATP (final concentration is 250 uM BzATP (human and rat) or 600 (mouse)). The fluorescence change was measured 180 seconds after adding the agonist. | 293 | cell-based format | BindingDB Database | |||
| 19. | ALA3889241 | B | FLIPR Assay: 1321 N1 cells expressing the recombinant human, rat or mouse P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium) high glucose supplemented with 10% Fetal Bovine Serum (FBS) and appropriate selection marker. Cells were seeded at a density of 25000 cells/well (96-well clear bottom black walled plates) in 100 ul volume/well. On the day of the experiment, cell plates were washed with assay buffer, containing (in mM): 130 NaCl, 2 KCl, 1 CaCl2, 1 MgCl2, 10 HEPES, 5 glucose; pH 7.40 and 300 mOs. After the wash, cells were loaded with the Calcium-4 dye (Molecular Device) and incubated in the dark for 60 minutes. Test compounds were prepared at 250ÿ the test concentration in neat DMSO. Intermediate 96-well compound plates were prepared by transferring 1.2 uL of the compound into 300 uL of assay buffer. A further 3x dilution occurred when transferring 50 uL/well of the compound plate to 100 uL/well in the cell plate. Cells were incubate with test compounds and dye for 30 minutes. Calcium dye fluorescence was monitored in FLIPR as the cells were challenged by adding 50 uL/well of BzATP (final concentration is 250 uM BzATP (human and rat) or 600 (mouse)). The fluorescence change was measured 180 seconds after adding the agonist. | 293 | cell-based format | BindingDB Database |
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