Supplementary Table S3

Compound Target(s) for which the Additional target candidates reported References

compound was developed (Kd or Ki/IC50 ≤ 100 nM) (assessment of (references) target potencies) Staurosporine NA 176 out of 291 kinases showed a Kd ≤ 100 nM Karaman et al., 2008 Ro 31-7549 Pan-PKC PKC , PKC , PKC , GSK3A, GSK3B Brehmer et al.,2004 (Brehmer et al.,2004) PD173955 SRC, ABL EPHA2, EPHB1, EPHB2, EPHB4, FGFR1, Wissing et al., (Wisniewski et al.,2002) FYN, GAK, LYN, MAPK14/p38  2004; Caligiuri et al., 2006 Sunitinib PDGFR, VEGFR, KIT, AAK1, AMPK, ARK5, AXL, BIKE, BLK, Karaman et al., FLT3 CAMK2A, CLK1, CLK2, CLK4, C-FMS, 2008 (Vakkalanka, 2008) CSNK1D, CSNK1E, CSNK2A1, DAPK3, DLK, DRAK1, FLT1, FLT4, GAK, ITK, JAK1, LKB1, LOK, MAP4K1, MAP4K5, MER, MLCK, MST1, MST2, MST3, MYLK2, PAK3, PHKG1, PHKG2, PIP5K2B, PTK2B, RET, RIOK1, RPS6KA2, RPS6KA4, RPS6KA5, SgK085, SLK, STK33, TNIK, TRKA, TTK, TYRO3 Vandetanib EGFR, VEGFR, RET ABL2, BLK, DDR1, EPHA6, EPHA8, GAK, Karaman et al., (ZD6474) (Herbst et al., 2007). LCK, LOK, PDGFR, RIPK2, SLK, SRC, 2008 TYRO3 Dasatinib ABL, FYN, SRC, LCK ABL2*, BLK, BMX, BTK*, C-FMS, CSK*, *Bantscheff et al, (Doggrell, 2005) DDR1*, DDR2*, EPHA1, EPHA2, EPHA3, 2007; Karaman et EPHA4, EPHA5, EPHA8, EPHB1, EPHB2*, al., 2008, EPHB3, EPHB4*, EPHB6, ERBB4, FAK*, FGR, FRK, GAK, HCK, KIT*, LIMK2, LYN, MAP4K5, MAPK14/p38 QIK*, PDGFR, PTK6, RIPK2*, SNF1LK, SNF1LK2, SRC, SRMS, TEC*, TESK1, TNK2, TNNI3K, TXK, YES, ZAK

1 Supplementary Table S3, cont’d

Compound Target(s) for which the Additional target candidates reported References

compound was developed (Kd or Ki/IC50 ≤ 100 nM) (assessment of (references) target potencies) Bosutinib ABL, FYN, SRC, LCK ABL2*, ALK4*, BCR, BMX, BTK, *Bantscheff et al, (SKI-606) (Puttini et al.,2006) CAMK1D, CSK, DDR1*, EPHB4*, FAK*, 2007; Remsing Rix FGR, FRK, FYN, GAK*, GCK*, HCK, LOK, et al., 2008 LYN*, MAP4K2, MAP4K3*, MAP4K5, MER*, MINK1, MST3, SYK*, TNK2, YES TKI258 FGF, VEGFR, FLT4, ANKK1, BIKE, C-FMS, FLT1, FLT3, KIT, Karaman et al., (CHIR-258) PDGFR, KIT MAP4K1, MLCK, MYLK2, RET, SgK085, 2008 TNIK, TRKA Pazopanib KIT, PDGFR, VEGFR, C-FMS, DDR1, DDR2, FLT1, LOK Karaman et al., (GW786034) FLT4 2008 (Sonpavde et al., 2008) Axitinib PDGFR, VEGFR, FLT4 Rugo et al., 2005 (AG013736) (Sonpavde et al., 2008) Sorafenib VEGFR, BRAF C-FMS, DDR1, DDR2, ERK8, FLT1, FLT3, Karaman et al., (Vakkalanka, 2008) FLT4, KIT, PDGFR, RET, TIE1, VEGFR2, 2008 ZAK R406 SYK, FLT3 LCK, LYN Braselmann et al., (Wong et al., 2004) 2006 BMS-387032 CDK2 CDC2L1, CDC2L2, CDK2, CDK3, CDK7, Karaman et al.,

(SNS-032) (Misra et al., 2004) CDK9, GSK3A, GSK3B, PCTK1, PCTK2, 2008 PCTK3 Flavopiridol CDK2 CDK9, CAMKK1, CDK11, CDK7, DYRK1B, Karaman et al.,

(Alvocidib) TNNI3K 2008

R-roscovitine CDK2 Karaman et al.,

(Seliciclib) (Hahntow et al., 2004) 2008