| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA3110426 | A | Plasma concentration in Plasmodium chabaudi ASS infected NIH mouse at 110 mg/kg, po qd measured 30 mins after post last dose on day 3 | Mus musculus | 1 | organism-based format | Scientific Literature | ||
| 2. | ALA3110428 | A | Plasma concentration in Plasmodium chabaudi ASS infected NIH mouse at 110 mg/kg, po qd measured 24 hrs after post last dose on day 3 | Mus musculus | 1 | organism-based format | Scientific Literature | ||
| 3. | ALA3110433 | F | Antimalarial activity against Plasmodium chabaudi ASS infected in NIH mouse assessed as inhibition of parasitemia at 110 mg/kg, po qd for 4 days | Plasmodium chabaudi | 1 | organism-based format | Scientific Literature | ||
| 4. | ALA3110809 | A | Inhibition of human recombinant CYP3A4 after 30 mins | Homo sapiens | 4 | single protein format | Scientific Literature | ||
| 5. | ALA3110810 | A | Inhibition of human recombinant CYP2C19 after 30 mins | Homo sapiens | 4 | single protein format | Scientific Literature | ||
| 6. | ALA3110811 | A | Inhibition of human recombinant CYP2D6 after 30 mins | Homo sapiens | 4 | single protein format | Scientific Literature | ||
| 7. | ALA3110812 | A | Inhibition of human recombinant CYP2C9 after 30 mins | Homo sapiens | 4 | single protein format | Scientific Literature | ||
| 8. | ALA3110813 | A | Inhibition of human recombinant CYP1A2 after 30 mins | Homo sapiens | 4 | single protein format | Scientific Literature | ||
| 9. | ALA3110814 | A | Cytotoxicity against human HepG2 cells after 72 hrs | Homo sapiens | 4 | cell-based format | Scientific Literature | ||
| 10. | ALA3110815 | F | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in RBV after 48 hrs by SYBR Green I-based fluorescence method | Plasmodium falciparum | 4 | organism-based format | Scientific Literature | ||
| 11. | ALA3110816 | F | Antimalarial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum Dd2 infected in RBV after 48 hrs by SYBR Green I-based fluorescence method | Plasmodium falciparum | 4 | assay format | Scientific Literature | ||
| 12. | ALA3110821 | F | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in RBV after 72 hrs by SYBR Green I-based fluorescence method | Plasmodium falciparum | 46 | organism-based format | Scientific Literature | ||
| 13. | ALA3887168 | B | Fluorescence Resonance Energy Transfer (FRET) Assay : The recombinant human BACE1, Cathepsin D, and Cathepsin E enzymes were purchased from R&D Systems (catalog numbers are 931-AS, 1014AS and 1294AS, respectively). The enzymatic inhibition activity assays were determined using the fluorescence resonance energy transfer (FRET) assay. The assays were performed in a 384-well plate format. The recombinant human BACE-1 enzyme (R&D Systems, catalog#931-AS) was diluted to 20 ng/μL in assay buffer (100 mM sodium acetate pH 4.0), 10 point 1:3 serial dilutions of compound in DMSO were preincubated with the enzyme for 15 min at room temperature. The concentration of Cathepsin D was 20 ng/μL, and 1 ng/μL of Cathepsin E was used. CatD and CatE were activated by incubation in assay buffer (0.1 M NaOAc, 0.2 M NaCl, pH 3.5) at room temperature for 30 min. Subsequently, the rhBACE-1 substrate (R&D Systems, catalog# ES004), the Cathepsin D and Cathepsin E substrate (R&D Systems, Catalog # ES001) were added accordingly to final concentration | Homo sapiens | 8 | single protein format | BindingDB Database | ||
| 14. | ALA3888550 | B | Enzyme Inhibition Assay : Plasmepsin-2 (PM-2; Plm II) and Plasmepsin (PM-4; Plm IV) expression and purification was performed following the published protocols (Istvan E S and Goldberg D E, 2005). The final purified protein was activated by diluting the protein to 0.3 mg/mL in activating buffer (0.1 M citrate pH 4.5, 0.1% Tween-20, 50 mM dithiothreitol) and incubated at room temperature for 40 min, then the activated enzyme was diluted in assay buffer (50 mM sodium acetate pH 4.7, 0.01% Tween-20). The enzymatic inhibition reaction was performed in 384 well plates with a total volume of 20 μl. 10 μl of diluted PM-2 or PM-4 enzyme was added to the 384-well plate except blank wells (blank wells add 10 μL of assay buffer) and 20 nL of serials of diluted 1000× compounds were added to the wells with 520 Echo® Liquid Handling System (Labcyte Inc.). 10 μL PM-2 peptide substrate (AnaSpec, Cat#, 62050) with assay buffer was then added to final concentration of 20 μM to start the reaction. | Plasmodium falciparum | 82 | assay format | BindingDB Database | ||
| 15. | ALA3888551 | B | Enzyme Inhibition Assay : Plasmepsin-2 (PM-2; Plm II) and Plasmepsin (PM-4; Plm IV) expression and purification was performed following the published protocols (Istvan E S and Goldberg D E, 2005). The final purified protein was activated by diluting the protein to 0.3 mg/mL in activating buffer (0.1 M citrate pH 4.5, 0.1% Tween-20, 50 mM dithiothreitol) and incubated at room temperature for 40 min, then the activated enzyme was diluted in assay buffer (50 mM sodium acetate pH 4.7, 0.01% Tween-20). The enzymatic inhibition reaction was performed in 384 well plates with a total volume of 20 μl. 10 μl of diluted PM-2 or PM-4 enzyme was added to the 384-well plate except blank wells (blank wells add 10 μL of assay buffer) and 20 nL of serials of diluted 1000× compounds were added to the wells with 520 Echo® Liquid Handling System (Labcyte Inc.). 10 μL PM-2 peptide substrate (AnaSpec, Cat#, 62050) with assay buffer was then added to final concentration of 20 μM to start the reaction. | 11 | assay format | BindingDB Database | |||
| 16. | ALA3888552 | B | Fluorescence Resonance Energy Transfer (FRET) Assay : The recombinant human BACE1, Cathepsin D, and Cathepsin E enzymes were purchased from R&D Systems (catalog numbers are 931-AS, 1014AS and 1294AS, respectively). The enzymatic inhibition activity assays were determined using the fluorescence resonance energy transfer (FRET) assay. The assays were performed in a 384-well plate format. The recombinant human BACE-1 enzyme (R&D Systems, catalog#931-AS) was diluted to 20 ng/μL in assay buffer (100 mM sodium acetate pH 4.0), 10 point 1:3 serial dilutions of compound in DMSO were preincubated with the enzyme for 15 min at room temperature. The concentration of Cathepsin D was 20 ng/μL, and 1 ng/μL of Cathepsin E was used. CatD and CatE were activated by incubation in assay buffer (0.1 M NaOAc, 0.2 M NaCl, pH 3.5) at room temperature for 30 min. Subsequently, the rhBACE-1 substrate (R&D Systems, catalog# ES004), the Cathepsin D and Cathepsin E substrate (R&D Systems, Catalog # ES001) were added accordingly to final concentration | Homo sapiens | 42 | single protein format | BindingDB Database | ||
| 17. | ALA3888553 | B | Fluorescence Resonance Energy Transfer (FRET) Assay : The recombinant human BACE1, Cathepsin D, and Cathepsin E enzymes were purchased from R&D Systems (catalog numbers are 931-AS, 1014AS and 1294AS, respectively). The enzymatic inhibition activity assays were determined using the fluorescence resonance energy transfer (FRET) assay. The assays were performed in a 384-well plate format. The recombinant human BACE-1 enzyme (R&D Systems, catalog#931-AS) was diluted to 20 ng/μL in assay buffer (100 mM sodium acetate pH 4.0), 10 point 1:3 serial dilutions of compound in DMSO were preincubated with the enzyme for 15 min at room temperature. The concentration of Cathepsin D was 20 ng/μL, and 1 ng/μL of Cathepsin E was used. CatD and CatE were activated by incubation in assay buffer (0.1 M NaOAc, 0.2 M NaCl, pH 3.5) at room temperature for 30 min. Subsequently, the rhBACE-1 substrate (R&D Systems, catalog# ES004), the Cathepsin D and Cathepsin E substrate (R&D Systems, Catalog # ES001) were added accordingly to final concentration | 8 | single protein format | BindingDB Database |
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