Basic Information
ID: ALA3706061
Type: Binding
Description: Inhibition of Histone Deacetylase Enzymatic Assay: For deacetylase assays, 20,000 cpm of the [3H]-metabolically labeled acetylated histone substrate (M. Yoshida et al., J. Biol. Chem. 265(28): 17174-17179 (1990)) is incubated with 30 ug of H446 nuclear extract or an equivalent amount of the cloned recombinant hHDAC-1 for 10 minutes at 37 C. The reaction is stopped by adding acetic acid (0.04 M, final concentration) and HCl (250 mM, final concentration). The mixture is extracted with ethyl acetate and the released [3H]-acetic acid was quantified by scintillation counting. For inhibition studies, the enzyme is preincubated with compounds at 4 C. for 30 minutes prior to initiation of the enzymatic assay. IC50 values for HDAC enzyme inhibitors are determined by performing dose response curves with individual compounds and determining the concentration of inhibitor producing fifty percent of the maximal inhibition. Alternatively, the following protocol is used to assay the compounds of the invention.
Organism: Homo sapiens
Activity Charts
Bioactivity
Activity Types for Assay ALA3706061
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 334.40 | 2.32 | 2.32 |
| 318.35 | 2.01 | 2.01 |
| 362.45 | 2.81 | 2.81 |
| 378.41 | 2.02 | 2.02 |
| 386.35 | 3.02 | 3.02 |
| 397.43 | 0.65 | 0.65 |
| 387.24 | 3.31 | 3.31 |
| 387.24 | 3.31 | 3.31 |
| 402.35 | 2.90 | 2.90 |
| 363.35 | 1.91 | 1.91 |
| 374.46 | 3.30 | 3.30 |
| 332.38 | 2.31 | 2.31 |
| 332.38 | 2.31 | 2.31 |
| 320.37 | 1.93 | 1.93 |
| 332.38 | 2.40 | 2.40 |
| 334.40 | 2.17 | 2.17 |
| 352.80 | 2.66 | 2.66 |
| 332.38 | 2.03 | 2.03 |
| 348.38 | 2.01 | 2.01 |
| 407.50 | 4.03 | 4.03 |
| 394.45 | 3.67 | 3.67 |
| 378.41 | 2.02 | 2.02 |
| 357.37 | 2.87 | 2.87 |
| 394.45 | 3.67 | 3.67 |
| 469.57 | 5.39 | 5.39 |
| 453.52 | 3.74 | 3.74 |
| 407.50 | 4.03 | 4.03 |
| 469.57 | 5.39 | 5.39 |
| 453.52 | 3.74 | 3.74 |
| 332.38 | 2.31 | 2.31 |
| 368.41 | 3.16 | 3.16 |
| 411.48 | 3.23 | 3.23 |
| 369.40 | 2.55 | 2.55 |
| 470.55 | 4.78 | 4.78 |
| 467.55 | 4.73 | 4.73 |
| 423.49 | 3.73 | 3.73 |
| 449.58 | 5.02 | 5.02 |
| 443.53 | 4.87 | 4.87 |
| 241.29 | 2.59 | 2.59 |
| 273.29 | 2.14 | 2.14 |
| 331.76 | 3.50 | 3.50 |
| 319.38 | 2.21 | 2.21 |
| 348.42 | 2.71 | 2.71 |
| 273.36 | 3.14 | 3.14 |
| 283.37 | 3.30 | 3.30 |
| 324.38 | 2.07 | 2.07 |
| 368.41 | 3.16 | 3.16 |
| 374.44 | 3.22 | 3.22 |
| 332.38 | 2.15 | 2.15 |
| 408.44 | 3.91 | 3.91 |
| 406.51 | 3.80 | 3.80 |
| 444.60 | 5.38 | 5.38 |
| 403.24 | 3.02 | 3.02 |
| 455.54 | 3.66 | 3.66 |
| 392.44 | 3.01 | 3.01 |
| 273.29 | 2.07 | 2.07 |
| 348.40 | 3.86 | 3.86 |
| 347.37 | 4.00 | 4.00 |
| 335.40 | 4.02 | 4.02 |
| 239.27 | 2.98 | 2.98 |
| 283.37 | 3.76 | 3.76 |
| 297.40 | 3.69 | 3.69 |
| 311.42 | 4.08 | 4.08 |
| 269.34 | 2.91 | 2.91 |
| 478.58 | 3.30 | 3.30 |
| 494.62 | 4.95 | 4.95 |
| 417.49 | 3.62 | 3.62 |
| 320.35 | 3.54 | 3.54 |
| 337.34 | 3.72 | 3.72 |
| 322.41 | 3.78 | 3.78 |
| 351.37 | 4.32 | 4.32 |
| 351.37 | 4.32 | 4.32 |
| 327.38 | 3.03 | 3.03 |
| 351.37 | 4.32 | 4.32 |