Assay Report Card

Basic Information

ID: ALA3705500

Type: Binding

Description: Inhibition Assay: An MGAT2 inhibition test for test compounds was conducted in accordance with a partially modified version of the method described in John F. Lockwood et al., Am. J. Physiol. Endocrinol. Metab., 2003, 285, E927.A 10 mg/mL microsomal fraction of human small intestine (duodenum- and jejunum-derived fraction purchased from Becton Dickinson Japan) was used as an enzyme source.The test was conducted using a flat-bottom 96-well plate (Corning).A buffer solution with final concentrations of 5 mM magnesium chloride, 1.25 mg/ml bovine serum albumin and 100 mM Tris-HCl (pH=7.5) was prepared and the microsomal fraction of human small intestine was added thereto to give a final concentration of 5 .mu.g/ml. Test compounds prepared in various concentrations using dimethyl sulfoxide were added thereto to give a final dimethyl sulfoxide concentration of 1% and a reaction was performed at room temperature for 5 min.

Activity Charts

Compound Summary

Parent Molecular WeightALogPPolar Surface Area
552.766.656.65
538.736.486.48
552.766.556.55
550.746.306.30
538.736.306.30
550.746.626.62
570.735.335.33
524.715.915.91
594.635.195.19
605.707.037.03
563.787.397.39
583.847.497.49
577.817.437.43
603.838.138.13
586.787.197.19
600.807.507.50
624.258.478.47
586.787.197.19
614.837.817.81
667.819.129.12
538.736.056.05
600.807.507.50
566.796.696.69
578.797.487.48
664.876.776.77
581.756.076.07
624.826.496.49
610.796.106.10
580.776.336.33
612.786.676.67
622.736.876.87
608.827.257.25
608.827.257.25
612.786.676.67
578.806.836.83
589.707.157.15
604.888.828.82
622.857.507.50
591.848.138.13
577.817.957.95
577.817.957.95
619.737.597.59
589.707.677.67
458.645.915.91
578.807.357.35
590.697.077.07
602.868.578.57
589.827.887.88