Inhibition of N-terminal GFP tagged human DOCK5 (1212-1642 residues) expressed in HEK293T cells assessed as reduction in exchange activity incubated for 1 hr by Western blot analysis based Rac-GTP pull-down assay
Inhibition of C-terminal 6-histidine tagged human DOCK5 (1212 to 1642 residues) expressed in Escherichia coli assessed as reduction in nucleotide exchange efficiency at 20 to 60 uM by N-methylanthraniloyl-GDP fluorescence based nucleotide exchange assay
Inhibition of C-terminal 6-histidine tagged human TRIOGEF1 (R1232 to T1550 residues) expressed in Escherichia coli assessed as reduction in nucleotide exchange efficiency at 20 to 60 uM by N-methylanthraniloyl-GDP fluorescence based nucleotide exchange assay
Toxicity in mouse peripheral blood cell-derived osteoclasts assessed as reduction in osteoclasts number up to 20 uM incubated for 48 hrs by TRAP-staining based assay
Antiosteoporotic activity in C57BL6/J mouse model of OVX-induced bone loss assessed as trabecular bone volume per tissue volume level in femoral metaphysis at 20 mg/kg, ip QD for 4 weeks by histomorphometry (11.67 +/- 2.37%)
Antiosteoporotic activity in C57BL6/J mouse model of OVX-induced bone loss assessed as trabecular thickness level in femoral metaphysis at 20 mg/kg, ip QD for 4 weeks by histomorphometry (39.96 +/- 5.42 um)
Antiosteoporotic activity in C57BL6/J mouse model of OVX-induced bone loss assessed as trabecular number level in femoral metaphysis at 20 mg/kg, ip QD for 4 weeks by histomorphometry (2.99 +/- 0.80 /mm)
Antiosteoporotic activity in C57BL6/J mouse model of OVX-induced bone loss assessed as trabecular separation level in femoral metaphysis at 20 mg/kg, ip QD for 4 weeks by histomorphometry (319.80 +/- 106.52 um)
Antiosteoporotic activity in C57BL6/J mouse model of OVX-induced bone loss assessed as trabecular bone volume per tissue volume level in tibial metaphysis at 20 mg/kg, ip QD for 4 weeks by microCT analysis (17.49 +/- 2.91 %)
Antiosteoporotic activity in C57BL6/J mouse model of OVX-induced bone loss assessed as trabecular pattern factor level in tibial metaphysis at 20 mg/kg, ip QD for 4 weeks by microCT analysis (17.17 +/- 3.41 um/day)
Antiosteoporotic activity in C57BL6/J mouse model of OVX-induced bone loss assessed as degree of anisotropy (range 0-1) level in tibial metaphysis at 20 mg/kg, ip QD for 4 weeks by microCT analysis (0.53 +/- 0.07 No_unit)
Antiosteoporotic activity in C57BL6/J mouse model of OVX-induced bone loss assessed as structure model index level in tibial metaphysis at 20 mg/kg, ip QD for 4 weeks by microCT analysis (1.92 +/- 0.19 No_unit)
Antiosteoporotic activity in C57BL6/J mouse model of OVX-induced bone loss assessed as cortical thickness level in tibial diaphysis at 20 mg/kg, ip QD for 4 weeks by microCT analysis (179.27 +/- 7.57 um)