Basic Information
ID: ALA3887026
Type: Binding
Description: qHTS Assay: Assay details and protocol: The primary assay monitored ATP depletion using Promega's KinaseGlo technology, where ATP levels are measured through luminescence generated from firefly luciferase, a bioluminescent ATP-dependent enzymes. ATP was held at 35 μM, near its reported KM value, and the KM for galactose was determined under the 1536-well assay conditions to be 50-100M (FIG. 1A). As well, the IC50 for a commercially available CD45 inhibitor (N-(9,10-dioxo-9,10-dihydrophenanthren-2-yl)pivalamide) was confirmed (previously found to inhibit GALK (FIG. 1B)). This was used as the positive control for the assay. The assay used 5 nM GALK and a 1 hr incubation time, which gave sufficient signal:background and stability for the HTS.
Activity Charts
Bioactivity
Activity Types for Assay ALA3887026
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 495.40 | 6.60 | 6.60 |
| 352.39 | 2.76 | 2.76 |
| 336.39 | 3.52 | 3.52 |
| 378.48 | 4.55 | 4.55 |
| 352.39 | 2.76 | 2.76 |
| 364.45 | 4.15 | 4.15 |
| 310.36 | 2.98 | 2.98 |
| 322.37 | 3.13 | 3.13 |
| 368.46 | 3.47 | 3.47 |
| 415.29 | 4.28 | 4.28 |
| 354.44 | 3.08 | 3.08 |
| 350.42 | 3.83 | 3.83 |
| 350.42 | 3.76 | 3.76 |
| 412.49 | 4.91 | 4.91 |
| 364.45 | 4.15 | 4.15 |
| 322.37 | 3.13 | 3.13 |
| 392.85 | 4.60 | 4.60 |
| 350.42 | 3.83 | 3.83 |
| 378.82 | 4.21 | 4.21 |
| 412.49 | 4.91 | 4.91 |
| 370.84 | 4.17 | 4.17 |
| 412.49 | 5.19 | 5.19 |
| 426.40 | 4.97 | 4.97 |
| 376.39 | 4.09 | 4.09 |
| 393.83 | 4.00 | 4.00 |
| 392.85 | 4.60 | 4.60 |
| 376.39 | 4.09 | 4.09 |
| 388.43 | 3.96 | 3.96 |
| 392.85 | 4.60 | 4.60 |
| 378.46 | 4.32 | 4.32 |
| 372.43 | 4.26 | 4.26 |
| 388.43 | 3.96 | 3.96 |
| 359.39 | 3.34 | 3.34 |
| 359.39 | 3.34 | 3.34 |
| 358.40 | 3.95 | 3.95 |
| 401.47 | 4.01 | 4.01 |
| 426.40 | 4.97 | 4.97 |
| 386.45 | 4.67 | 4.67 |
| 382.81 | 3.32 | 3.32 |
| 530.43 | 5.95 | 5.95 |
| 427.39 | 4.36 | 4.36 |
| 438.29 | 4.10 | 4.10 |
| 427.26 | 3.43 | 3.43 |
| 438.29 | 4.10 | 4.10 |
| 349.44 | 3.26 | 3.26 |
| 532.40 | 5.62 | 5.62 |
| 469.92 | 3.09 | 3.09 |
| 532.40 | 5.62 | 5.62 |
| 484.30 | 4.55 | 4.55 |
| 508.42 | 5.43 | 5.43 |
| 439.91 | 3.65 | 3.65 |
| 504.96 | 4.84 | 4.84 |
| 348.37 | 2.67 | 2.67 |
| 385.82 | 2.34 | 2.34 |
| 378.46 | 4.32 | 4.32 |
| 516.40 | 5.92 | 5.92 |
| 454.33 | 4.06 | 4.06 |
| 427.39 | 4.36 | 4.36 |
| 411.85 | 2.87 | 2.87 |
| 518.99 | 4.85 | 4.85 |
| 427.29 | 5.25 | 5.25 |
| 493.32 | 4.60 | 4.60 |
| 536.82 | 6.27 | 6.27 |
| 372.43 | 4.26 | 4.26 |
| 441.29 | 3.44 | 3.44 |
| 437.30 | 4.71 | 4.71 |
| 388.43 | 3.96 | 3.96 |
| 526.39 | 6.27 | 6.27 |
| 546.02 | 4.76 | 4.76 |
| 399.84 | 2.35 | 2.35 |
| 458.55 | 5.03 | 5.03 |
| 452.86 | 3.23 | 3.23 |
| 502.37 | 5.62 | 5.62 |
| 426.52 | 5.30 | 5.30 |
| 516.40 | 5.29 | 5.29 |
| 339.40 | 2.53 | 2.53 |
| 425.88 | 2.88 | 2.88 |
| 392.42 | 3.41 | 3.41 |
| 509.39 | 5.07 | 5.07 |
| 409.48 | 3.28 | 3.28 |
| 393.83 | 4.00 | 4.00 |
| 516.40 | 5.92 | 5.92 |
| 510.38 | 4.47 | 4.47 |
| 536.82 | 6.27 | 6.27 |
| 438.29 | 4.10 | 4.10 |
| 362.39 | 2.98 | 2.98 |
| 531.99 | 4.75 | 4.75 |
| 396.84 | 3.33 | 3.33 |