Basic Information
ID: ALA3705388
Type: Binding
Description: Inhibiton Assay: For studying inhibition of Plasmodium or human DHODH enzyme, two assays that are in routine use are described, for example, in Baldwin, et al. (2002) JBiol Chem., 277, 41827-41834, and Baldwin, et al. (2005) J. Biol. Chem., 280. 21847-21853.Briefly, this colorimetric assay monitors the reduction of 2,6-dichloroindophenol (DCIP) at 600 nm (e = 18.8 mM-1cm-1) for measuring DHOD inhibition. The assay was carried out using a solution containing 100 mM HEPES, pH 8.0, 150 mM NaCl, 10% glycerol, 0.1% Triton X-100, 20 micro molar CoQD (coenzyme QD), 200 micro molar L-dihydroorotate, and 120 micro molar DCIP. Reactions are initiated by addition of enzyme to a final concentration in the range of about 5 nM to about 50 nM while maintaining the temperature of a circulating water bath at 25° C. Alternatively, for potent compounds, activity was determined by directly measuring the production of orotic acid at 296 nm (ε = 4.3 mM-1 cm-1).
Organism: Plasmodium falciparum
Activity Charts
Bioactivity
Activity Types for Assay ALA3705388
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 341.72 | 4.16 | 4.16 |
| 327.70 | 3.85 | 3.85 |
| 357.29 | 4.31 | 4.31 |
| 307.28 | 3.28 | 3.28 |
| 325.32 | 3.79 | 3.79 |
| 299.35 | 3.61 | 3.61 |
| 277.69 | 2.97 | 2.97 |
| 361.25 | 4.21 | 4.21 |
| 329.23 | 3.47 | 3.47 |
| 279.35 | 3.06 | 3.06 |
| 281.34 | 3.39 | 3.39 |
| 265.32 | 2.01 | 2.01 |
| 283.31 | 2.15 | 2.15 |
| 344.22 | 2.77 | 2.77 |
| 279.35 | 2.40 | 2.40 |
| 297.34 | 2.54 | 2.54 |
| 313.79 | 3.06 | 3.06 |
| 347.22 | 3.91 | 3.91 |
| 295.39 | 3.86 | 3.86 |
| 337.31 | 3.64 | 3.64 |
| 283.31 | 2.80 | 2.80 |
| 335.33 | 4.32 | 4.32 |
| 333.32 | 4.07 | 4.07 |
| 323.73 | 3.94 | 3.94 |
| 371.31 | 4.70 | 4.70 |
| 361.25 | 4.21 | 4.21 |
| 289.73 | 2.84 | 2.84 |
| 321.31 | 3.81 | 3.81 |
| 292.26 | 3.80 | 3.80 |
| 375.28 | 4.45 | 4.45 |
| 393.27 | 4.59 | 4.59 |
| 397.23 | 4.49 | 4.49 |
| 293.37 | 3.48 | 3.48 |
| 347.34 | 4.07 | 4.07 |
| 334.21 | 3.32 | 3.32 |
| 310.25 | 3.94 | 3.94 |
| 264.33 | 3.27 | 3.27 |
| 301.30 | 2.29 | 2.29 |
| 325.37 | 1.00 | 1.00 |
| 311.24 | 3.33 | 3.33 |
| 344.22 | 3.51 | 3.51 |
| 345.69 | 3.99 | 3.99 |
| 347.34 | 3.42 | 3.42 |