Table 2. Chemical characterization of GS-9973.

Panel A shows the chemical structure for GS-9973. Panel B shows the relative selectivity of GS-9973 compared to the Syk inhitor R406 using the DiscoveRx panel for Kd determinations

Kinome Scan Symbol GS-9973 R406 Kd (nM) Selectivity (Fold) Kd (nM) Selectivity (Fold) ABL1-nonphos. 8400 800 8400 560 ABL1-phos. 560 53 560 37 ALK 2900 276 240 16 AXL 1900 181 82 5 BIKE 1100 105 1900 127 BLK 420 40 25 1.7 BRK 330 31 360 24 CHEK2 40000 3810 1000 67 CSF1R 180 17 31 2.1 CSNK2A1 540 51 1400 93 CSNK2A2 110 10 1200 80 DAPK1 40000 3810 55 4 DAPK3 40000 3810 13 0.9 EGFR 1400 133 300 20 EPHA1 470 45 67 4 EPHB6 550 52 310 21 FGR 230 22 33 2.2 FLT3 320 30 0.71 0.05 FLT3-autoinhib. 40000 3810 13 0.9 GAK 1300 124 250 17 GRK4 40000 3810 450 30 HCK 410 39 150 10 HIPK1 40000 3810 820 55 HIPK3 40000 3810 3200 213 INSR 1800 171 1100 73 IRAK1 140 13 9.7 0.6 IRAK3 120 11 11 0.7 JAK1(JH1-cat.) 730 70 21 1.4 JAK2(JH1-cat.) 110 10 3.5 0.2 JAK3(JH1-cat.) 3200 305 36 2.4 JNK1 2000 190 38 3 KIT 210 20 6.8 0.5 LCK 820 78 30 2.0 LOK 40000 3810 70 5 LTK 1200 114 800 53 MA P4K2 40000 3810 670 45 MEK5 200 19 27 1.8 MERTK 3300 314 170 11 MLK1 570 54 4.3 0.3 PDGFRB 670 64 3.3 0.2 PIP5K1A 40000 3810 1900 127 PIP5K1C 40000 3810 PIP5K2B 40000 3810 1200 80 PRKR 3000 286 180 12 RET 1000 95 4.1 0.3 RIOK1 40000 3810 340 23 RIOK2 160 15 3400 227 RIOK3 40000 3810 210 14 SBK1 40000 3810 93 6 SLK 820 78 33 2.2 SRC 110 10 8.4 0.6 SRMS 910 87 610 41 SRPK1 40000 3810 590 39 SRPK3 3200 305 400 27 STK16 330 31 1.7 0.1 STK33 40000 3810 970 65 SYK 10.5 1 15 1 TAK1 490 47 49 3 TGFBR2 390 37 330 22 TNK1 86 8 25 1.7 TNK2 670 64 70 5 TYK2(JH1-cat.) 180 17 190 13 ULK3 510 49 7.1 0.5 VEGF R2 40000 3810 40 3 YES 450 43 35 2.3 YSK4 440 42 67 4 ZAP70 410 39 21 1.4