ID: ALA3705440
Type: Binding
Description: Inhibition Assay: For sodium-dependent glucose transport assay, cells expressing hSGLT2 were seeded into a 96-well culture plate at a density of 5x104 cells/well in RPMI medium 1640 containing 10% fetal bovine serum. The cells were used 1 day after plating. They were incubated in pretreatment buffer (10 mM HEPES, 5 mM Tris, 140 mM choline chloride, 2 mM KCl, 1 mM CaCl2, and 1 mM MgCl2, pH 7.4) at 37 C. for 10 min. They were then incubated in uptake buffer (10 mM HEPES, 5 mM Tris, 140 mM NaCl, 2 mM KCl, 1 mM CaCl2, 1 mM MgCl2, and 1 mM 14C-nonlabeled AMG pH 7.4) containing 14C-labeled AMG (8 uM) and the inventive compound or dimethyl sulfoxide (DMSO) vehicle at 37 C. for 2 h. Cells were washed twice with washing buffer (pretreatment buffer containing 10 mM AMG at room temperature) and then the radioactivity was measured using a liquid scintillation counter. IC50 was determined by nonlinear regression analysis using GraphPad PRISM [Katsuno, K. et al. J. Pharmacol. Exp. Ther. 2007, 320, 323-330].
Organism: Homo sapiens
Bioactivity
Activity Types for Assay ALA3705440
IC50
Parent Molecular Weight | ALogP | Polar Surface Area |
---|---|---|
449.93 | 1.45 | 1.45 |
464.90 | 1.15 | 1.15 |
422.86 | 1.09 | 1.09 |
480.94 | 1.14 | 1.14 |
464.94 | 2.17 | 2.17 |
450.87 | 1.03 | 1.03 |
452.89 | 0.88 | 0.88 |
449.93 | 1.45 | 1.45 |
506.98 | 1.94 | 1.94 |
461.94 | 1.59 | 1.59 |
490.86 | 2.28 | 2.28 |
478.93 | 2.52 | 2.52 |
464.90 | 2.21 | 2.21 |
445.90 | 1.45 | 1.45 |
478.93 | 1.16 | 1.16 |
464.94 | 2.17 | 2.17 |
478.99 | 2.64 | 2.64 |
442.92 | 1.45 | 1.45 |
435.95 | 2.29 | 2.29 |
449.93 | 1.28 | 1.28 |
465.93 | 1.65 | 1.65 |
479.96 | 1.67 | 1.67 |
449.93 | 1.81 | 1.81 |
448.94 | 2.50 | 2.50 |
450.92 | 1.95 | 1.95 |
462.97 | 2.68 | 2.68 |
464.94 | 2.12 | 2.12 |
464.94 | 2.17 | 2.17 |
478.97 | 2.56 | 2.56 |
433.93 | 2.05 | 2.05 |
478.97 | 2.51 | 2.51 |
464.94 | 2.34 | 2.34 |
478.97 | 2.51 | 2.51 |
464.90 | 1.42 | 1.42 |
480.94 | 1.92 | 1.92 |
456.54 | 2.00 | 2.00 |
458.55 | 2.08 | 2.08 |
461.94 | 1.74 | 1.74 |
463.91 | 1.18 | 1.18 |
490.98 | 2.70 | 2.70 |
474.98 | 3.04 | 3.04 |
476.95 | 2.31 | 2.31 |
448.51 | 2.78 | 2.78 |
459.97 | 2.14 | 2.14 |
414.50 | 1.68 | 1.68 |
418.46 | 1.43 | 1.43 |
464.94 | 2.17 | 2.17 |
466.91 | 1.62 | 1.62 |
436.89 | 1.39 | 1.39 |
434.92 | 1.94 | 1.94 |
450.92 | 1.78 | 1.78 |
415.87 | 1.99 | 1.99 |
416.86 | 1.39 | 1.39 |
436.89 | 1.61 | 1.61 |
416.47 | 1.26 | 1.26 |
420.91 | 2.66 | 2.66 |
422.93 | 2.09 | 2.09 |
494.98 | 2.84 | 2.84 |
417.89 | 1.94 | 1.94 |
418.88 | 1.33 | 1.33 |
418.88 | 1.33 | 1.33 |
432.90 | 1.82 | 1.82 |
432.90 | 1.82 | 1.82 |
446.93 | 2.38 | 2.38 |
446.93 | 2.38 | 2.38 |
452.89 | 1.23 | 1.23 |
478.93 | 1.54 | 1.54 |
464.90 | 1.15 | 1.15 |
464.97 | 3.06 | 3.06 |
438.93 | 1.93 | 1.93 |
468.96 | 1.94 | 1.94 |
422.86 | 1.22 | 1.22 |
438.86 | 0.92 | 0.92 |
402.44 | 0.87 | 0.87 |
408.83 | 1.17 | 1.17 |
404.89 | 1.93 | 1.93 |
418.92 | 2.32 | 2.32 |
436.96 | 2.48 | 2.48 |
450.92 | 2.00 | 2.00 |
420.89 | 1.77 | 1.77 |
424.90 | 1.89 | 1.89 |
422.86 | 1.31 | 1.31 |
420.85 | 1.69 | 1.69 |
438.93 | 1.93 | 1.93 |
470.93 | 0.61 | 0.61 |
448.56 | 3.33 | 3.33 |
464.56 | 3.17 | 3.17 |
482.55 | 3.31 | 3.31 |
478.54 | 2.54 | 2.54 |
481.34 | 1.63 | 1.63 |
499.00 | 3.82 | 3.82 |
489.57 | 3.04 | 3.04 |
470.59 | 3.23 | 3.23 |
470.59 | 3.23 | 3.23 |
438.93 | 2.55 | 2.55 |
422.86 | 1.83 | 1.83 |
422.86 | 1.83 | 1.83 |
422.86 | 1.83 | 1.83 |
468.96 | 2.55 | 2.55 |
452.89 | 1.84 | 1.84 |
479.37 | 2.66 | 2.66 |
454.93 | 2.25 | 2.25 |
386.44 | 1.38 | 1.38 |
404.48 | 1.54 | 1.54 |
480.90 | 0.99 | 0.99 |
462.93 | 1.71 | 1.71 |
442.51 | 1.36 | 1.36 |
478.49 | 1.99 | 1.99 |
438.90 | 2.46 | 2.46 |
466.98 | 3.35 | 3.35 |
454.97 | 3.18 | 3.18 |
486.97 | 1.86 | 1.86 |
468.95 | 2.55 | 2.55 |
454.97 | 3.18 | 3.18 |
450.92 | 2.63 | 2.63 |
447.96 | 2.00 | 2.00 |
430.93 | 2.58 | 2.58 |
444.96 | 2.81 | 2.81 |
432.90 | 2.02 | 2.02 |
474.86 | 2.40 | 2.40 |
441.31 | 2.03 | 2.03 |
474.86 | 2.40 | 2.40 |
434.92 | 2.81 | 2.81 |
452.91 | 2.76 | 2.76 |
464.94 | 2.17 | 2.17 |
430.50 | 1.43 | 1.43 |
450.92 | 1.78 | 1.78 |
450.92 | 1.78 | 1.78 |
448.94 | 2.33 | 2.33 |
460.95 | 2.65 | 2.65 |
462.97 | 2.72 | 2.72 |
464.94 | 2.17 | 2.17 |
448.94 | 2.33 | 2.33 |
446.93 | 2.41 | 2.41 |
460.95 | 2.65 | 2.65 |
418.92 | 2.24 | 2.24 |
433.93 | 1.98 | 1.98 |
435.90 | 1.42 | 1.42 |
466.98 | 2.49 | 2.49 |
481.01 | 2.88 | 2.88 |
513.01 | 2.18 | 2.18 |
497.01 | 2.51 | 2.51 |
462.97 | 2.89 | 2.89 |
462.97 | 2.89 | 2.89 |
448.94 | 2.50 | 2.50 |
466.98 | 2.49 | 2.49 |
464.94 | 2.17 | 2.17 |
450.92 | 2.30 | 2.30 |
452.89 | 1.57 | 1.57 |
480.94 | 2.01 | 2.01 |
464.94 | 2.17 | 2.17 |
406.86 | 1.38 | 1.38 |
448.90 | 1.58 | 1.58 |
450.92 | 1.43 | 1.43 |
452.91 | 2.41 | 2.41 |
446.93 | 2.26 | 2.26 |
444.91 | 3.07 | 3.07 |
446.93 | 3.14 | 3.14 |
464.94 | 1.61 | 1.61 |
456.87 | 2.32 | 2.32 |
470.90 | 2.49 | 2.49 |
426.51 | 1.91 | 1.91 |
474.94 | 1.22 | 1.22 |
446.93 | 2.41 | 2.41 |
448.94 | 2.50 | 2.50 |
430.88 | 1.36 | 1.36 |
449.93 | 1.10 | 1.10 |
463.96 | 1.44 | 1.44 |
461.94 | 1.20 | 1.20 |
431.87 | 1.25 | 1.25 |
448.94 | 2.33 | 2.33 |
446.93 | 2.26 | 2.26 |
460.95 | 2.65 | 2.65 |
450.48 | 2.23 | 2.23 |
438.86 | 1.18 | 1.18 |
414.50 | 1.60 | 1.60 |
434.92 | 1.94 | 1.94 |
450.92 | 1.78 | 1.78 |
452.96 | 2.10 | 2.10 |
460.95 | 2.65 | 2.65 |
481.01 | 3.50 | 3.50 |
432.94 | 2.50 | 2.50 |
479.37 | 2.05 | 2.05 |
448.94 | 2.33 | 2.33 |
465.01 | 3.04 | 3.04 |
448.90 | 2.05 | 2.05 |
464.94 | 2.17 | 2.17 |
466.98 | 2.49 | 2.49 |
462.93 | 2.09 | 2.09 |
450.92 | 1.78 | 1.78 |
436.89 | 1.39 | 1.39 |
452.89 | 1.23 | 1.23 |
450.92 | 1.78 | 1.78 |
448.94 | 2.33 | 2.33 |
464.94 | 2.34 | 2.34 |
450.92 | 1.78 | 1.78 |
493.39 | 2.44 | 2.44 |
448.94 | 2.33 | 2.33 |
436.89 | 1.74 | 1.74 |
477.39 | 2.61 | 2.61 |
432.90 | 2.02 | 2.02 |
434.92 | 1.94 | 1.94 |