Assay Report Card

Basic Information

ID: ALA3705470

Type: Binding

Description: Inhibition Assay: The PDE9-inhibiting activity was measured by the following method. That is, to a buffer solution containing tris(hydroxymethyl)aminomethane-hydrochloric acid (40 mM, pH 8.0), magnesium chloride (5 mM), and 2-mercaptoethanol (4 mM) were added cGMP (1 μM) and 3H-cGMP (0.33 μCi/ml) to give a substrate buffer solution. A test substance solution and an enzyme solution which had been adjusted to an optimal concentration were added thereto to perform a reaction at 30° C. The enzyme reaction was stopped by the addition of Scintillation Proximity Assay (SPA) Beads (Perkin Elmer, USA) containing 5 mM 3-isobutyl-1-methylxanthine (IBMX). For the enzyme activity, the amount of 5′-GMP, which is a reaction degradation product bound to SPA beads, was measured with a TopCount microplate reader (Hewlett Packard, USA).

Activity Charts

Compound Summary

Parent Molecular WeightALogPPolar Surface Area
339.444.264.26
335.484.434.43
335.484.434.43
432.914.854.85
486.582.892.89
394.483.163.16
448.914.094.09
471.563.363.36
476.513.583.58
553.715.065.06
472.552.902.90
487.563.623.62
507.643.303.30
438.533.043.04
438.533.183.18
464.573.573.57
486.583.063.06
473.542.292.29
452.563.573.57
463.583.103.10
452.563.433.43
481.602.722.72
452.563.433.43
451.573.103.10
511.633.743.74
451.573.103.10
481.602.722.72
424.502.652.65
450.543.323.32
438.533.043.04
474.513.423.42
470.553.523.52
451.572.782.78
495.623.113.11
509.653.503.50
467.572.842.84
481.603.193.19
495.623.113.11
491.513.253.25
509.653.363.36
503.552.582.58
505.543.643.64
493.612.862.86
465.603.483.48
438.533.043.04
491.513.253.25
506.534.144.14
495.622.802.80
461.493.623.62
475.523.883.88
489.522.192.19
466.583.823.82
464.573.713.71
521.543.223.22
488.543.813.81
470.553.523.52
456.523.133.13
451.573.093.09
517.613.263.26
517.613.263.26
509.653.503.50
519.574.024.02
477.492.862.86
479.633.873.87
479.633.563.56
489.544.084.08
493.653.953.95
503.574.474.47
474.513.423.42
462.473.953.95
529.634.514.51
465.603.173.17
450.543.183.18
438.533.183.18
491.513.253.25
452.563.433.43
450.543.323.32
478.473.333.33
515.613.803.80
505.543.643.64
539.555.045.04
475.523.693.69
489.544.094.09
489.544.404.40
514.633.843.84
512.663.973.97
464.573.573.57
436.512.932.93
507.512.832.83
456.523.133.13
478.473.073.07
498.584.104.10
477.492.862.86
515.614.124.12
451.572.782.78
465.603.173.17
465.603.483.48
481.602.722.72
438.533.043.04
388.454.674.67