Assay Report Card

Basic Information

ID: ALA3707725

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.

Organism: Homo sapiens

Activity Charts

Compound Summary

Parent Molecular WeightALogPPolar Surface Area
507.524.494.49
527.553.793.79
525.584.794.79
590.645.165.16
508.513.433.43
469.474.484.48
522.543.743.74
527.554.774.77
541.575.165.16
513.524.384.38
454.454.224.22
483.494.664.66
483.494.664.66
552.563.583.58
548.593.433.43
533.583.573.57
533.583.573.57
456.472.922.92
534.562.512.51
562.614.084.08
498.513.103.10
513.524.384.38
497.524.164.16
497.524.164.16
533.583.573.57
533.583.573.57
481.485.335.33
481.485.335.33
497.524.164.16
502.564.404.40
486.565.395.39
518.564.074.07
486.565.395.39
502.564.404.40
518.564.074.07
532.505.585.58
532.505.585.58
534.564.004.00
498.514.404.40
498.514.404.40
528.534.514.51
528.534.514.51
530.604.234.23
530.604.234.23
507.524.494.49
507.524.494.49
458.534.594.59
453.493.923.92
541.575.035.03
541.575.035.03
469.523.243.24
480.494.044.04
508.513.433.43
466.473.743.74
542.563.973.97
527.554.724.72
527.554.724.72
528.543.663.66
484.524.984.98
512.594.464.46
512.594.464.46
512.543.443.44
538.532.922.92
465.484.794.79
465.484.794.79
473.554.174.17
468.513.513.51
487.584.564.56
517.562.832.83
576.644.394.39
576.644.394.39
470.504.674.67
470.504.674.67
562.614.084.08
562.614.084.08
468.513.513.51
528.543.633.63
514.513.323.32
473.554.174.17
523.565.265.26
523.565.265.26
509.534.954.95
509.534.954.95
482.474.284.28
484.525.065.06
498.555.375.37
484.525.065.06
498.555.375.37
470.504.674.67
544.574.694.69
602.684.964.96
512.585.795.79
572.605.645.64
528.584.904.90
540.595.045.04
554.615.565.56
528.585.215.21
528.585.465.46
484.524.984.98
484.524.984.98
501.563.323.32
588.593.353.35
587.604.404.40
618.684.634.63
588.654.444.44
582.703.513.51
620.675.045.04
573.674.404.40
548.594.084.08
533.555.505.50
533.583.653.65
521.623.573.57
576.644.604.60
570.614.674.67
662.734.084.08
592.644.094.09
506.603.993.99
618.684.074.07
532.594.384.38
533.555.505.50
544.574.694.69
620.694.624.62
534.644.114.11
572.605.645.64
626.763.533.53
664.725.065.06
636.694.114.11
496.553.353.35
581.604.514.51
550.654.014.01
458.534.594.59
565.673.593.59
528.585.215.21
570.615.235.23
540.595.045.04
632.714.464.46
662.734.644.64
620.694.874.87
528.585.465.46
500.524.684.68
592.644.094.09
485.514.254.25
577.633.673.67
566.594.224.22
572.594.114.11
571.605.175.17
533.555.065.06
610.624.404.40
533.555.065.06
611.645.935.93
510.573.993.99
565.605.025.02
511.562.932.93
566.593.973.97
584.603.693.69
614.623.883.88
608.623.433.43
522.543.743.74
539.564.964.96
524.554.544.54
583.614.754.75
581.604.514.51
495.564.414.41
613.644.944.94
607.645.045.04
577.614.864.86
544.533.333.33
529.522.902.90
528.543.963.96
522.544.074.07
614.623.323.32
613.644.384.38
607.644.484.48
527.554.694.69
521.554.804.80
569.584.494.49
609.655.515.51
579.625.325.32
547.595.365.36
547.595.525.52
514.504.124.12
514.504.124.12
543.554.394.39
537.554.504.50
538.533.443.44
523.523.013.01
609.635.465.46
571.663.933.93
572.652.872.87
578.652.762.76
616.624.304.30
577.663.823.82
615.635.355.35
571.604.924.92
572.593.863.86
502.564.404.40