Basic Information
ID: ALA3707927
Type: Binding
Description: Kinase Assay: Inhibition of kinase activity by test compound disclosed herein was estimated by quantifying the amount of [33P] incorporation of substrate in the presence of test compound. Standard assay conditions were 2 ng of recombinant C-Raf or 5 ng of recombinant B-Raf or 5 ng of recombinant B-Raf (V600E) kinase (Upstate Biotechnology) with 500 ng MEK1(K97R) in assay buffer {8 μM ATP, 0.5 μCi [33P]ATP (specific activity 3000 Ci/mmol, PerkinElmer), 50 mM Tris/HCl (pH7.5), and 1 mM EGTA, 1 mM Na3VO4, 1% 2-mercaptoethanol, 0.1% Brij 35, and 0.2 mg/ml BSA} at a final volume of 25 μL. Reactions were incubated at 30° C. for 30 min and stopped by adding 3% phosphoric acid, harvested onto a 96-well GF/B UniFilter (PerkinElmer) using a unifilter harvester (PerkinElmer), and counted with a TopCount microplate scintillation counter (PerkinElmer). The IC50 values of inhibitors were determined after carrying out assays at 3-fold serially diluted concentrations of each compound in duplication.
Format: BAO_0000357
Organism: Homo sapiens
Target: Serine/threonine-protein kinase RAF(ALA1906)
Document: ALA3638563
BindingDB Source: 6407
Activity Charts
Bioactivity
Activity Types for Assay ALA3707927
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 327.39 | 5.05 | 5.05 |
| 343.39 | 4.75 | 4.75 |
| 313.36 | 4.75 | 4.75 |
| 359.39 | 4.46 | 4.46 |
| 395.82 | 5.55 | 5.55 |
| 361.38 | 4.89 | 4.89 |
| 395.82 | 5.55 | 5.55 |
| 375.40 | 5.20 | 5.20 |
| 379.37 | 5.03 | 5.03 |
| 393.83 | 5.11 | 5.11 |
| 373.41 | 4.76 | 4.76 |
| 359.39 | 4.46 | 4.46 |
| 422.47 | 3.40 | 3.40 |
| 373.41 | 4.77 | 4.77 |
| 386.41 | 3.85 | 3.85 |
| 403.39 | 4.16 | 4.16 |
| 386.41 | 3.85 | 3.85 |
| 388.38 | 4.66 | 4.66 |
| 387.40 | 4.48 | 4.48 |
| 383.41 | 4.63 | 4.63 |
| 403.44 | 4.78 | 4.78 |
| 423.86 | 5.12 | 5.12 |
| 400.44 | 4.71 | 4.71 |
| 454.41 | 5.26 | 5.26 |
| 422.47 | 3.40 | 3.40 |
| 359.39 | 4.46 | 4.46 |
| 383.41 | 4.63 | 4.63 |
| 361.38 | 4.89 | 4.89 |
| 383.41 | 4.63 | 4.63 |
| 393.83 | 5.11 | 5.11 |
| 428.28 | 5.77 | 5.77 |
| 329.36 | 4.45 | 4.45 |
| 329.36 | 4.45 | 4.45 |
| 343.39 | 4.75 | 4.75 |
| 384.40 | 4.03 | 4.03 |
| 394.44 | 4.88 | 4.88 |
| 406.47 | 4.12 | 4.12 |
| 385.40 | 5.06 | 5.06 |
| 385.40 | 5.06 | 5.06 |
| 401.86 | 5.58 | 5.58 |
| 381.44 | 5.23 | 5.23 |
| 381.44 | 5.23 | 5.23 |
| 389.82 | 5.71 | 5.71 |
| 371.83 | 5.57 | 5.57 |
| 355.38 | 5.06 | 5.06 |
| 384.40 | 4.03 | 4.03 |
| 385.40 | 5.06 | 5.06 |
| 373.37 | 5.19 | 5.19 |
| 337.39 | 4.92 | 4.92 |
| 362.40 | 5.47 | 5.47 |
| 397.44 | 4.93 | 4.93 |
| 380.45 | 4.98 | 4.98 |
| 355.38 | 5.06 | 5.06 |
| 382.38 | 4.82 | 4.82 |
| 381.44 | 5.32 | 5.32 |
| 367.41 | 4.41 | 4.41 |
| 430.49 | 4.29 | 4.29 |
| 381.40 | 4.65 | 4.65 |
| 380.41 | 4.02 | 4.02 |
| 395.42 | 4.74 | 4.74 |
| 397.44 | 4.64 | 4.64 |
| 358.40 | 5.07 | 5.07 |
| 376.39 | 5.20 | 5.20 |
| 362.40 | 4.79 | 4.79 |
| 382.42 | 5.24 | 5.24 |
| 369.40 | 5.36 | 5.36 |
| 397.44 | 4.93 | 4.93 |
| 356.43 | 4.81 | 4.81 |
| 444.52 | 4.68 | 4.68 |
| 458.55 | 5.07 | 5.07 |
| 384.41 | 5.67 | 5.67 |
| 396.45 | 5.54 | 5.54 |
| 400.87 | 6.18 | 6.18 |
| 394.43 | 5.34 | 5.34 |
| 379.42 | 4.62 | 4.62 |
| 409.39 | 5.36 | 5.36 |
| 361.38 | 4.89 | 4.89 |
| 414.49 | 4.93 | 4.93 |
| 351.41 | 5.10 | 5.10 |
| 457.56 | 5.67 | 5.67 |
| 366.42 | 5.53 | 5.53 |
| 417.86 | 5.28 | 5.28 |
| 399.41 | 3.92 | 3.92 |
| 453.50 | 4.87 | 4.87 |
| 454.48 | 4.27 | 4.27 |
| 353.39 | 4.62 | 4.62 |
| 379.37 | 5.03 | 5.03 |
| 353.39 | 4.62 | 4.62 |
| 377.41 | 4.79 | 4.79 |
| 373.41 | 4.77 | 4.77 |
| 391.40 | 4.91 | 4.91 |
| 393.83 | 5.11 | 5.11 |
| 395.37 | 4.74 | 4.74 |
| 411.82 | 5.25 | 5.25 |
| 383.79 | 5.68 | 5.68 |
| 377.38 | 4.60 | 4.60 |
| 395.37 | 4.74 | 4.74 |
| 389.37 | 4.90 | 4.90 |
| 383.79 | 5.68 | 5.68 |
| 416.47 | 3.86 | 3.86 |