Basic Information
ID: ALA3705754
Type: Binding
Description: AlphaScreen Assay: Pim 1, Pim 2 & Pim 3 AlphaScreen assays using high ATP (11-125.times. ATP Km) were used to determine the biochemical activity of the inhibitors. The activity of Pim 1, Pim 2, & Pim 3 is measured using a homogeneous bead based system quantifying the amount of phosphorylated peptide substrate resulting from kinase-catalyzed phosphoryl transfer to a peptide substrate. Compounds to be tested are dissolved in 100% DMSO and directly distributed to a white 384-well plate at 0.25 .mu.l per well. To start the reaction, 5 .mu.l of 100 nM Bad peptide (Biotin-AGAGRSRHSSYPAGT-OH (SEQ ID NO:1)) and ATP (concentrations described below) in assay buffer (50 mM Hepes, pH=7.5, 5 mM MgCl.sub.2, 0.05% BSA, 0.01% Tween-20, 1 mM DTT) is added to each well. This is followed by the addition of 5 .mu.l/well of Pim 1, Pim 2 or Pim 3 kinase in assay buffer (concentrations described below). Final assay concentrations (described below) are in 2.5% DMSO. The reactions are performed for .about.2 hours.
Activity Charts
Bioactivity
Activity Types for Assay ALA3705754
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 507.52 | 4.49 | 4.49 |
| 527.55 | 3.79 | 3.79 |
| 525.58 | 4.79 | 4.79 |
| 590.64 | 5.16 | 5.16 |
| 508.51 | 3.43 | 3.43 |
| 469.47 | 4.48 | 4.48 |
| 522.54 | 3.74 | 3.74 |
| 527.55 | 4.77 | 4.77 |
| 541.57 | 5.16 | 5.16 |
| 513.52 | 4.38 | 4.38 |
| 454.45 | 4.22 | 4.22 |
| 483.49 | 4.66 | 4.66 |
| 483.49 | 4.66 | 4.66 |
| 552.56 | 3.58 | 3.58 |
| 548.59 | 3.43 | 3.43 |
| 533.58 | 3.57 | 3.57 |
| 533.58 | 3.57 | 3.57 |
| 456.47 | 2.92 | 2.92 |
| 534.56 | 2.51 | 2.51 |
| 562.61 | 4.08 | 4.08 |
| 498.51 | 3.10 | 3.10 |
| 513.52 | 4.38 | 4.38 |
| 497.52 | 4.16 | 4.16 |
| 497.52 | 4.16 | 4.16 |
| 533.58 | 3.57 | 3.57 |
| 533.58 | 3.57 | 3.57 |
| 481.48 | 5.33 | 5.33 |
| 481.48 | 5.33 | 5.33 |
| 497.52 | 4.16 | 4.16 |
| 502.56 | 4.40 | 4.40 |
| 486.56 | 5.39 | 5.39 |
| 518.56 | 4.07 | 4.07 |
| 486.56 | 5.39 | 5.39 |
| 502.56 | 4.40 | 4.40 |
| 518.56 | 4.07 | 4.07 |
| 532.50 | 5.58 | 5.58 |
| 532.50 | 5.58 | 5.58 |
| 534.56 | 4.00 | 4.00 |
| 498.51 | 4.40 | 4.40 |
| 498.51 | 4.40 | 4.40 |
| 528.53 | 4.51 | 4.51 |
| 528.53 | 4.51 | 4.51 |
| 530.60 | 4.23 | 4.23 |
| 530.60 | 4.23 | 4.23 |
| 507.52 | 4.49 | 4.49 |
| 507.52 | 4.49 | 4.49 |
| 458.53 | 4.59 | 4.59 |
| 453.49 | 3.92 | 3.92 |
| 541.57 | 5.03 | 5.03 |
| 541.57 | 5.03 | 5.03 |
| 469.52 | 3.24 | 3.24 |
| 480.49 | 4.04 | 4.04 |
| 508.51 | 3.43 | 3.43 |
| 466.47 | 3.74 | 3.74 |
| 542.56 | 3.97 | 3.97 |
| 527.55 | 4.72 | 4.72 |
| 527.55 | 4.72 | 4.72 |
| 528.54 | 3.66 | 3.66 |
| 484.52 | 4.98 | 4.98 |
| 512.59 | 4.46 | 4.46 |
| 512.59 | 4.46 | 4.46 |
| 512.54 | 3.44 | 3.44 |
| 538.53 | 2.92 | 2.92 |
| 465.48 | 4.79 | 4.79 |
| 465.48 | 4.79 | 4.79 |
| 473.55 | 4.17 | 4.17 |
| 468.51 | 3.51 | 3.51 |
| 487.58 | 4.56 | 4.56 |
| 517.56 | 2.83 | 2.83 |
| 576.64 | 4.39 | 4.39 |
| 576.64 | 4.39 | 4.39 |
| 470.50 | 4.67 | 4.67 |
| 470.50 | 4.67 | 4.67 |
| 562.61 | 4.08 | 4.08 |
| 562.61 | 4.08 | 4.08 |
| 468.51 | 3.51 | 3.51 |
| 528.54 | 3.63 | 3.63 |
| 514.51 | 3.32 | 3.32 |
| 473.55 | 4.17 | 4.17 |
| 523.56 | 5.26 | 5.26 |
| 523.56 | 5.26 | 5.26 |
| 509.53 | 4.95 | 4.95 |
| 509.53 | 4.95 | 4.95 |
| 482.47 | 4.28 | 4.28 |
| 484.52 | 5.06 | 5.06 |
| 498.55 | 5.37 | 5.37 |
| 484.52 | 5.06 | 5.06 |
| 498.55 | 5.37 | 5.37 |
| 470.50 | 4.67 | 4.67 |
| 544.57 | 4.69 | 4.69 |
| 602.68 | 4.96 | 4.96 |
| 512.58 | 5.79 | 5.79 |
| 572.60 | 5.64 | 5.64 |
| 528.58 | 4.90 | 4.90 |
| 540.59 | 5.04 | 5.04 |
| 554.61 | 5.56 | 5.56 |
| 528.58 | 5.21 | 5.21 |
| 528.58 | 5.46 | 5.46 |
| 484.52 | 4.98 | 4.98 |
| 484.52 | 4.98 | 4.98 |
| 501.56 | 3.32 | 3.32 |
| 588.59 | 3.35 | 3.35 |
| 587.60 | 4.40 | 4.40 |
| 618.68 | 4.63 | 4.63 |
| 588.65 | 4.44 | 4.44 |
| 582.70 | 3.51 | 3.51 |
| 620.67 | 5.04 | 5.04 |
| 573.67 | 4.40 | 4.40 |
| 548.59 | 4.08 | 4.08 |
| 533.55 | 5.50 | 5.50 |
| 521.62 | 3.57 | 3.57 |
| 576.64 | 4.60 | 4.60 |
| 570.61 | 4.67 | 4.67 |
| 662.73 | 4.08 | 4.08 |
| 592.64 | 4.09 | 4.09 |
| 506.60 | 3.99 | 3.99 |
| 618.68 | 4.07 | 4.07 |
| 532.59 | 4.38 | 4.38 |
| 533.55 | 5.50 | 5.50 |
| 544.57 | 4.69 | 4.69 |
| 620.69 | 4.62 | 4.62 |
| 534.64 | 4.11 | 4.11 |
| 572.60 | 5.64 | 5.64 |
| 626.76 | 3.53 | 3.53 |
| 664.72 | 5.06 | 5.06 |
| 636.69 | 4.11 | 4.11 |
| 496.55 | 3.35 | 3.35 |
| 581.60 | 4.51 | 4.51 |
| 550.65 | 4.01 | 4.01 |
| 458.53 | 4.59 | 4.59 |
| 565.67 | 3.59 | 3.59 |
| 528.58 | 5.21 | 5.21 |
| 570.61 | 5.23 | 5.23 |
| 540.59 | 5.04 | 5.04 |
| 632.71 | 4.46 | 4.46 |
| 662.73 | 4.64 | 4.64 |
| 620.69 | 4.87 | 4.87 |
| 528.58 | 5.46 | 5.46 |
| 500.52 | 4.68 | 4.68 |
| 592.64 | 4.09 | 4.09 |
| 485.51 | 4.25 | 4.25 |
| 577.63 | 3.67 | 3.67 |
| 566.59 | 4.22 | 4.22 |
| 572.59 | 4.11 | 4.11 |
| 571.60 | 5.17 | 5.17 |
| 533.55 | 5.06 | 5.06 |
| 610.62 | 4.40 | 4.40 |
| 533.55 | 5.06 | 5.06 |
| 611.64 | 5.93 | 5.93 |
| 510.57 | 3.99 | 3.99 |
| 565.60 | 5.02 | 5.02 |
| 511.56 | 2.93 | 2.93 |
| 566.59 | 3.97 | 3.97 |
| 584.60 | 3.69 | 3.69 |
| 614.62 | 3.88 | 3.88 |
| 608.62 | 3.43 | 3.43 |
| 522.54 | 3.74 | 3.74 |
| 539.56 | 4.96 | 4.96 |
| 524.55 | 4.54 | 4.54 |
| 583.61 | 4.75 | 4.75 |
| 581.60 | 4.51 | 4.51 |
| 495.56 | 4.41 | 4.41 |
| 613.64 | 4.94 | 4.94 |
| 607.64 | 5.04 | 5.04 |
| 577.61 | 4.86 | 4.86 |
| 544.53 | 3.33 | 3.33 |
| 529.52 | 2.90 | 2.90 |
| 528.54 | 3.96 | 3.96 |
| 522.54 | 4.07 | 4.07 |
| 614.62 | 3.32 | 3.32 |
| 613.64 | 4.38 | 4.38 |
| 607.64 | 4.48 | 4.48 |
| 527.55 | 4.69 | 4.69 |
| 521.55 | 4.80 | 4.80 |
| 569.58 | 4.49 | 4.49 |
| 609.65 | 5.51 | 5.51 |
| 579.62 | 5.32 | 5.32 |
| 547.59 | 5.36 | 5.36 |
| 547.59 | 5.52 | 5.52 |
| 514.50 | 4.12 | 4.12 |
| 514.50 | 4.12 | 4.12 |
| 543.55 | 4.39 | 4.39 |
| 537.55 | 4.50 | 4.50 |
| 538.53 | 3.44 | 3.44 |
| 523.52 | 3.01 | 3.01 |
| 609.63 | 5.46 | 5.46 |
| 571.66 | 3.93 | 3.93 |
| 572.65 | 2.87 | 2.87 |
| 578.65 | 2.76 | 2.76 |
| 616.62 | 4.30 | 4.30 |
| 577.66 | 3.82 | 3.82 |
| 615.63 | 5.35 | 5.35 |
| 571.60 | 4.92 | 4.92 |
| 572.59 | 3.86 | 3.86 |
| 502.56 | 4.40 | 4.40 |