For 317 Kinases. Blank Fields Indicate Combinations That Were Tested, but for Which Binding Was Weak (Kd > 10 Um), Or Not Detected in a Primary Screen (10 Um)

Supplementary Table 1. Binding results (Kd's in nM) for 317 kinases. Blank fields indicate combinations that were tested, but for which binding was weak (Kd > 10 uM), or not detected in a primary screen (10 uM). Adapted from Karaman et al, 2008.

Accession Number Entrez Gene Symbol Kinase Target Imatinib Sorafenib Sunitinib NP_055726.2 AAK1 AAK1 11 NP_005148.2 ABL1 ABL1 12 680 830 NP_005148.2 ABL1 ABL1(E255K) 77 3900 2800 NP_005148.2 ABL1 ABL1(H396P) 35 1600 1000 NP_005148.2 ABL1 ABL1(M351T) 8.5 250 1200 NP_005148.2 ABL1 ABL1(Q252H) 21 480 890 NP_005148.2 ABL1 ABL1(T315I) 160 140 NP_005148.2 ABL1 ABL1(Y253F) 44 420 950 NP_005149.2 ABL2 ABL2 10 2900 1000 NP_001096.1 ACVR1 ACVR1 NP_004293.1 ACVR1B ACVR1B NP_001607.1 ACVR2A ACVR2A NP_001097.2 ACVR2B ACVR2B NP_000011.2 ACVRL1 ACVRL1 NP_064632.2 CABC1 ADCK3 NP_079152.3 ADCK4 ADCK4 NP_005154.2 AKT1 AKT1 NP_001617.1 AKT2 AKT2 2700 NP_005456.1 AKT3 AKT3 NP_004295.2 ALK ALK 170 BAA36547.1 PRKAA1 AMPK-alpha1 19 NP_006243.2 PRKAA2 AMPK-alpha2 89 NP_848605.1 ANKK1 ANKK1 310 NP_055655.1 NUAK1 ARK5 48 NP_003591.2 AURKA AURKA 1700 AAH00442.2 AURKB AURKB 440 380 AAC77369.1 AURKC AURKC 210 220 NP_001690.2 AXL AXL 4500 9 NP_060063.2 BMP2K BIKE 5.5 NP_001706.2 BLK BLK 520 65 NP_004320.2 BMPR1A BMPR1A NP_001195.2 BMPR2 BMPR2 570 NP_001712.1 BMX BMX NP_004324.2 BRAF BRAF 540 NP_004324.2 BRAF BRAF(V600E) 3300 260 NP_115806.1 BRSK1 BRSK1 3500 NP_003948.2 BRSK2 BRSK2 1100 NP_000052.1 BTK BTK NP_003647.1 CAMK1 CAMK1 970 NP_065130.1 CAMK1D CAMK1D 510 NP_065172.1 CAMK1G CAMK1G 440 NP_741960.1 CAMK2A CAMK2A 80 NP_001211.3 CAMK2B CAMK2B 1400 AAD20442.1 CAMK2D CAMK2D 420 NP_751912.1 CAMK2G CAMK2G 690 NP_001735.1 CAMK4 CAMK4 890 NP_115670.1 CAMKK1 CAMKK1 420 NP_006540.3 CAMKK2 CAMKK2 1500 NP_277023.1 CDC2L1 CDC2L1 NP_076916.1 CDC2L2 CDC2L2 NP_055891.1 CDC2L6 CDK11 5500 250 NP_001789.2 CDK2 CDK2 NP_001249.1 CDK3 CDK3 NP_004926.1 CDK5 CDK5 NP_001790.1 CDK7 CDK7 140 330 NP_001251.1 CDK8 CDK8 310 NP_001252.1 CDK9 CDK9 NP_001265.1 CHEK1 CHEK1 300 NP_009105.1 CIT CIT 6200 3900 AAA61480.1 CLK1 CLK1 4500 22 NP_003984.2 CLK2 CLK2 20 NP_003983.1 CLK3 CLK3 NP_065717.1 CLK4 CLK4 2100 29 NP_005202.2 CSF1R CSF1R 19 28 2 NP_004374.1 CSK CSK NP_660204.1 CSNK1A1L CSNK1A1L 550 NP_620693.1 CSNK1D CSNK1D 15 NP_001885.1 CSNK1E CSNK1E 13 NP_071331.2 CSNK1G1 CSNK1G1 930 NP_001310.2 CSNK1G2 CSNK1G2 110 NP_004375.2 CSNK1G3 CSNK1G3 240 NP_001886.1 CSNK2A1 CSNK2A1 81 NP_001887.1 CSNK2A2 CSNK2A2 370 NP_004929.2 DAPK1 DAPK1 120 NP_055141.2 DAPK2 DAPK2 150 NP_001339.1 DAPK3 DAPK3 22 NP_004725.1 DCAMKL1 DCAMKL1 370 NP_001035351.1 DCAMKL2 DCAMKL2 2700 XP_047355.6 DCAMKL3 DCAMKL3 110 NP_001945.3 DDR1 DDR1 0.7 1.5 2000 CAA52777.1 DDR2 DDR2 15 6.6 NP_006292.2 MAP3K12 DLK 100 NP_004400.4 DMPK DMPK NP_059995.1 CDC42BPG DMPK2 NP_004751.2 STK17A DRAK1 5300 1 NP_004217.1 STK17B DRAK2 110 NP_004705.1 DYRK1B DYRK1B 2300 NP_005219.2 EGFR EGFR NP_005219.2 EGFR EGFR(E746-A750del) NP_005219.2 EGFR EGFR(G719C) 6800 NP_005219.2 EGFR EGFR(G719S) NP_005219.2 EGFR EGFR(L747-E749de 7600 NP_005219.2 EGFR EGFR(L747-S752del, P753S) NP_005219.2 EGFR EGFR(L747-T751del,Sins) NP_005219.2 EGFR EGFR(L858R) NP_005219.2 EGFR EGFR(L861Q) NP_005219.2 EGFR EGFR(S752-I759del) NP_005223.3 EPHA1 EPHA1 3100 NP_004422.2 EPHA2 EPHA2 2000 NP_005224.2 EPHA3 EPHA3 1900 2100 NP_004429.1 EPHA4 EPHA4 3000 NP_004430.3 EPHA5 EPHA5 NP_001073917.1 EPHA6 EPHA6 370 960 NP_004431.1 EPHA7 EPHA7 5300 2400 NP_065387.1 EPHA8 EPHA8 1400 2400 NP_004432.1 EPHB1 EPHB1 3000 480 NP_059145.2 EPHB2 EPHB2 1900 NP_004434.2 EPHB3 EPHB3 NP_004435.3 EPHB4 EPHB4 1800 NP_001005862.1 ERBB2 ERBB2 NP_001036064.1 ERBB4 ERBB4 NP_002737.2 MAPK3 ERK1 NP_620407.1 MAPK1 ERK2 NP_002739.1 MAPK6 ERK3 NP_002738.2 MAPK4 ERK4 NP_002740.2 MAPk7 ERK5 NP_620590.2 MAPK15 ERK8 46 NP_005237.2 FER FER 1100 NP_001996.1 FES FES 960 NP_075593.1 FGFR1 FGFR1 2800 520 NP_075259.2 FGFR2 FGFR2 2700 570 NP_000133.1 FGFR3 FGFR3 290 NP_000133.1 FGFR3 FGFR3(G697C) 5900 1400 NP_075252.2 FGFR4 FGFR4 NP_005239.1 FGR FGR 2400 270 NP_002010.1 FLT1 FLT1 31 1.8 NP_004110.2 FLT3 FLT3 13 0.47 NP_004110.2 FLT3 FLT3(D835H) 30 4.3 NP_004110.2 FLT3 FLT3(D835Y) 82 2.3 NP_004110.2 FLT3 FLT3(ITD) 79 0.99 NP_004110.2 FLT3 FLT3(N841I) 11 2.4 CAA49505.1 FLT4 FLT4 95 50 NP_002022.1 FRK FRK 1500 510 530 NP_694592.1 FYN FYN 3100 520 NP_005246.1 GAK GAK 1000 20 NP_001013725.2 EIF2AK4 GCN2(Kin.Dom.2,S808G) 180 NP_063937.2 GSK3A GSK3A NP_002084.2 GSK3B GSK3B NP_002101.2 HCK HCK 880 NP_000866.1 IGF1R IGF1R 2600 NP_054721.1 IKBKE IKK-epsilon 620 NP_000199.2 INSR INSR 500 NP_055030.1 INSRR INSRR 430 NP_009130.1 IRAK3 IRAK3 940 NP_005537.3 ITK ITK 13 NP_002218.2 JAK1 JAK1(Kin.Dom.1/JH2 - pseudokinase) 49 NP_004963.1 JAK2 JAK2(Kin.Dom.2/JH1 - catalytic) 410 NP_000206.2 JAK3 JAK3(Kin.Dom.2/JH1 - catalytic) 1200 NP_002741.1 MAPK8 JNK1 5000 NP_620707.1 MAPK9 JNK2 NP_002744.1 MAPK10 JNK3 3100 NP_000213.1 KIT KIT 14 31 0.37 NP_000213.1 KIT KIT(D816V) 820 310 380 NP_000213.1 KIT KIT(V559D) 15 16 0.41 NP_000213.1 KIT KIT(V559D,T670I) 2900 18 0.28 NP_000213.1 KIT KIT(V559D,V654A) 71 240 0.21 NP_004681.1 LATS1 LATS1 630 NP_055387.1 LATS2 LATS2 460 NP_005347.3 LCK LCK 40 2700 230 NP_002305.1 LIMK1 LIMK1 1600 NP_005560.1 LIMK2 LIMK2 NP_000446.1 STK11 LKB1 38 BAA35073.1 STK10 LOK 150 19 NP_996844.1 LTK LTK 1800 NP_002341.1 LYN LYN 890 3000 270 NP_005913.2 MAP3K4 MAP3K4 NP_005914.1 MAP3K5 MAP3K5 NP_001036065.1 MAP4K1 MAP4K1 16 NP_003609.2 MAP4K3 MAP4K3 180 NP_663719.1 MAP4K4 MAP4K4 4800 140 NP_006566.2 MAP4K5 MAP4K5 1600 41 NP_116584.2 MAPKAPK2 MAPKAPK2 NP_003659.2 MAPKAPK5 MAPKAPK5 CAH72463.1 MARK1 MARK1 1200 NP_059672.2 MARK2 MARK2 310 NP_002367.4 MARK3 MARK3 410 NP_113605.2 MARK4 MARK4 3600 NP_002746.1 MAP2K1 MEK1 130 NP_109587.1 MAP2K2 MEK2 110 NP_002747.2 MAP2K3 MEK3 NP_003001.1 MAP2K4 MEK4 NP_002749.2 MAP2K6 MEK6 NP_055606.1 MELK MELK 1900 350 AAB60430.1 MERTK MERTK 3600 26 NP_000236.2 MET MET CAI14764.1 MKNK1 MKNK1 230 AAF17226.1 MKNK2 MKNK2 130 NP_872299.1 MLCK MLCK 23 NP_149132.2 MAP3K9 MLK1 3400 NP_002437.2 MAP3K10 MLK2 NP_002410.1 MAP3K11 MLK3 1300 NP_003598.2 CDC42BPA MRCKA NP_006026.3 CDC42BPB MRCKB NP_006273.1 STK4 MST1 19 NP_006272.2 STK3 MST2 56 NP_003567.2 STK24 MST3 63 NP_057626.2 RP6-213H19.1 MST4 340 NP_005583.1 MUSK MUSK 130 490 NP_444254.3 MYLK MYLK 280 NP_149109.1 MYLK2 MYLK2 49 NP_059129.2 MYO3A MYO3A NP_620482.1 MYO3B MYO3B 4500 NP_055815.1 STK38L NDR2 970 NP_036356.1 NEK1 NEK1 NP_002488.1 NEK2 NEK2 1400 NP_954983.1 NEK5 NEK5 NP_055212.2 NEK6 NEK6 NP_598001.1 NEK7 NEK7 4100 NP_149107.3 NEK9 NEK9 NP_057315.2 NLK NLK 640 NP_620581.1 MAPK14 p38-alpha 370 NP_002742.3 MAPK11 p38-beta 230 AAB40118.1 MAPK12 p38-gamma 7600 NP_002567.3^ PAK1 PAK1 NP_002568.2 PAK2 PAK2 NP_002569.1 PAK3 PAK3 16 NP_001014833.1 PAK4 PAK4 2300 NP_064553.1 PAK6 PAK6 2400 NP_065074.1 PAK7 PAK7/PAK5 640 NP_006192.1^ PCTK1 PCTK1 150 CAA47004.1 PCTK2 PCTK2 1600 1200 NP_002587.2 PCTK3 PCTK3 1700 NP_006197.1 PDGFRA PDGFRA 31 62 0.79 NP_002600.1 PDGFRB PDGFRB 14 37 0.075 NP_002604.1 PDPK1 PDPK1 3500 NP_036527.1 PFTK1 PFTK1 2900 270 NP_006204.1 PHKG1 PHKG1 5.5 NP_000285.1 PHKG2 PHKG2 5.9 NP_006209.2 PIK3CA PIK3CA NP_006209.2 PIK3CA PIK3CA(E545K) NP_002639.1 PIM1 PIM1 NP_006866.2 PIM2 PIM2 NP_001001852.1 PIM3 PIM3 2400 AAC50911.1 PIP5K1A PIP5K1A 5400 NP_003550.1 PIP5K2B PIP5K2B 39 NP_002721.1 PRKACA PKAC-alpha NP_002722.1 PRKACB PKAC-beta NP_872629.1 PKMYT1 PKMYT1 NP_998725.1 PKN1 PKN1 710 NP_006247.1 PKN2 PKN2 1300 NP_005021.2 PLK1 PLK1 NP_004064.2 PLK3 PLK3 BAB69958.1 PLK4 PLK4 7800 4500 190 NP_006245.2 PRKCD PRKCD NP_005391.1 PRKCE PRKCE NP_006246.2 PRKCH PRKCH NP_006248.1 PRKCQ PRKCQ 4300 NP_002733.2 PRKD1 PRKD1 310 NP_057541.2 PRKD2 PRKD2 380 NP_005804.1 PRKD3 PRKD3 280 NP_006249.1 PRKG1 PRKG1 NP_006250.1 PRKG2 PRKG2 NP_002750.1 EIF2AK2 PRKR 670 NP_005035.1 PRKX PRKX NP_722560.1 PTK2 PTK2 440 NP_775267.1 PTK2B PTK2B 82 NP_005966.1 PTK6 PTK6 NP_002871.1 RAF1 RAF1 1700 230 NP_065681.1 RET RET 13 12 NP_065681.1 RET RET(M918T) 7.4 19 NP_113668.2 RIOK1 RIOK1 35 NP_003822.2 RIOK3 RIOK3 3800 NP_003795.2 RIPK1 RIPK1 370 NP_003812.1 RIPK2 RIPK2 1300 NP_002935.2 ROS1 ROS1 NP_002944.2 RPS6KA1 RPS6KA1(Kin.Dom.1 - N-terminal) 140 NP_002944.2 RPS6KA1 RPS6KA1(Kin.Dom.2 - C-terminal) 5000 NP_066958.2 RPS6KA2 RPS6KA2(Kin.Dom.1 - N-terminal) 17 NP_001006933.1 RPS6KA2 RPS6KA2(Kin.Dom.2 - C-terminal) 8400 NP_004577.1 RPS6KA3 RPS6KA3(Kin.Dom.1 - N-terminal) 580 NP_001006945.1 RPS6KA4 RPS6KA4(Kin.Dom.1 - N-terminal) 96 NP_003933.1 RPS6KA4 RPS6KA4(Kin.Dom.2 - C-terminal) 2000 NP_872198.1 RPS6KA5 RPS6KA5(Kin.Dom.1 - N-terminal) 28 NP_004746.2 RPS6KA5 RPS6KA5(Kin.Dom.2 - C-terminal) 1700 NP_055311.1 RPS6KA6 RPS6KA6(Kin.Dom.1 - N-terminal) 2400 NP_055311.1 RPS6KA6 RPS6KA6(Kin.Dom.2 - C-terminal) 7500 NP_001012418.1 RP11-145H9.1 SgK085 15 NP_055535.2 SLK SLK 1000 56 NP_112214.1 NUAK2 SNARK 150 NP_775490.2 SNF1LK SNF1LK 3200 NP_056006.1 SNF1LK2 SNF1LK2 580 NP_005408.1 SRC SRC 2100 NP_543013.1 SRMS SRMS 9800 NP_003128.3 SRPK1 SRPK1 250 AAC05299.1 SRPK2 SRPK2 190 CAA06700.1 STK16 STK16 250 NP_112168.1 STK33 STK33 2400 17 NP_056505.1 STK36 STK36 3800 NP_003168.2 SYK SYK NP_003206.1 TEC TEC NP_006276.2 TESK1 TESK1 NP_004603.1 TGFBR1 TGFBR1 NP_003233.4 TGFBR2 TGFBR2 NP_005415.1 TIE1 TIE1 68 NP_000450.2 TEK TIE2 2100 NP_036422.3 TLK1 TLK1 740 AAF03095.1 TLK2 TLK2 330 NP_055843.1 TNIK TNIK 25 AAH35782.1 TNK1 TNK1 2300 680 NP_001010938.1 TNK2 TNK2 8900 NP_057062.1 TNNI3K TNNI3K 4300 280 NP_001012331.1 NTRK1 TRKA 6300 100 NP_006171.2 NTRK2 TRKB 2100 590 AAA75374.1 NTRK3 TRKC 600 5100 NP_114417.1 TSSK1 TSSK1 6300 NP_003309.2 TTK TTK 3500 63 NP_003319.1 TXK TXK CAA38449.1 TYK2 TYK2(Kin.Dom.2/JH1 - catalytic) 1600 NP_006284.2 TYRO3 TYRO3 49 NP_002244.1 KDR VEGFR2 59 1.5 NP_003381.1 WEE1 WEE1 1100 NP_060871.1 STK32B YANK2 NP_775846.2 STK32C YANK3 NP_005424.1 YES1 YES 120 NP_006365.2 STK25 YSK1 290 NP_598407.1 ZAK ZAK 2600 6.3 NP_997402.1 ZAP70 ZAP70 Supp. Table 2 Primer sequences c-KIT Sequence Exons

CKIT-AF GCTTTGCCGCGCTCGCTGCACTTGG Sense 1 - 2 CKIT-AR CCAGCGTGTCGTTGTCTTCTTTCC Anti-sense CKIT-BF CGAATGAGAATAAGCAGAATGAATGG Sense 2 - 4 CKIT-BR GTTGAGTACACAGAACTAGACACATC Anti-sense CKIT-CF CTGTGGACCAGGAGGGCAAGTCAG Sense 3 - 6 CKIT-CR GTGAAGGTTCTGTTCATATAGATCC Anti-sense CKIT-DF CTGGAGTGTTCATGTGTTATGCC Sense 5 - 8 CKIT-DR CCACACATTGGAGCATGCCATTC Anti-sense CKIT-EF CGTAAGTGAACTTCATCTAACGAG Sense 7 - 10 CKIT-ER GGTCAGAATCATCACAATAATGCAC Anti-sense CKIT-KD-AF CTAGTGCATTCAAGCACAATGGCACG Sense 9 - 11 CKIT-KD-AR CCATAAGCAGTTGCCTCAACAACC Anti-sense CKIT-KD-BF GAAACCCATGTATGAAGTACAGTGG Sense 11 - 14 CKIT-KD-BR GCAGCTTCTGCATGATCTTCCTGC Anti-sense CKIT-KD-CF CTACTTGGAGCCTGCACCATTGGAG Sense 13 - 18 CKIT-KD-CR CCACTTCACAGGTAGTCGAGCGTTTCC Anti-sense CKIT-KD-DF CCTCCAAGAATTGTATTCACAGAGAC Sense 16 - 20 CKIT-KD-DR GATTGGTGCTCTCTGAAATCTGCTTC Anti-sense CKIT-KD-EF GATGATCAAGGAAGGCTTCCGGATGC Sense 19 - 22 CKIT-KD-ER GTGTGCTCAGAAAGACAGGATTGCAG Anti-sense

PDGFR-alpha Sequence Exons

PDGFRa-AF2 CCATTACTGTTGGAGCTACAGG Sense 1 - 4 PDGFRa-AR2 GGAGTCTCGGGATCAGTTGTGC Antisense PDGFRa-BF GTGACGGTCTTGGAAGTGAGCAG Sense 3 - 5 PDGFRa-BR GATGCCTTTGCCTTTCACTTCTCC Antisense PDGFRa-CF CTATATCTGTGAGGCCACCGTCAAAG Sense 4 - 7 PDGFRa-CR CCACATCAGTGGTGATCTCAGTGAG Antisense PDGFRa-DF CAGTGGAGATTACGAATGTGCTGC Sense 6 - 10 PDGFRa-DR GTTGGCCAAAATAGTCCAGGAAG Antisense PDGFRa-EF GAAGATGCTGTGAAGAGCTATAC Sense 8 - 12 PDGFRa-ER CCTCCAGCGAATTTCATACCTCG Antisense PDGFRa-11F CTCCTTGGAGCTGAGAACCGAGAGC Sense 10 - 13 PDGFRa-11R CTTCACTGCAACTTTCATGACAGG Antisense PDGFRa-12F GTTTCCAAGAGATGGACTAGTGC Sense 12 - 15 PDGFRa-12R CATAGCTCCGTGTGCTTTCATCAGC Antisense PDGFRa-13F GAATAGGGATAGCTTCCTGAGCCACC Sense 15 - 17 PDGFRa-13R CTTGATAGGTGAAGCTCAACAAATCC Antisense PDGFRa-14F GAAATCTATGTTAGACTCAGAAGTC Sense 16 - 20 PDGFRa-14R GATCTTATTGTAGAAAGTAGAATCC Antisense PDGFRa-15F CTACACCACACTGAGTGATGTCTGG Sense 19 - 22 PDGFRa-15R CACCAATGTATGCATTGTCTGAGTCC Antisense

PDGFR-beta Sequence Exons

PDGFB-5Fb CAGTCTTTCTGATAACTGGGAGAGG Sense 1 - 3 PDGFB-5R CAGTGTGAGCACGCTGGAGAAGG Anti-sense PDGFB-6F GAGCTTGTCCTCAATGTCTCCAGC Sense 3 - 4 PDGFB-6R GTCTGTTACTCGGCATGAATGG Anti-sense PDGFB-7F CTGGAGACCGATGAGCGGAAACG Sense 3 - 5 PDGFB-7R CTCGAAGTTGACCACCTCATTCC Anti-sense PDGFB-8F CTACTATGTCTACAGACTCCAGG Sense 4 - 7 PDGFB-8R GTCCGGCTCCGATGCAGCTCAGC Anti-sense PDGFB-9F GTGACGGAGAGTGTGAATGACC Sense 6 - 9 PDGFB-9R CAGGGACATTGATCTGTAGCTGG Anti-sense PDGFB-10F GTGTCAGAGCTGACACTGGTTCG Sense 8 - 10 PDGFB-10Ra CACCACGATGACCTCCTGCGTGTCC Anti-sense PDGFB-11F GAGGTGGTGAGCACACTGCGTCTGC Sense 10 - 13 PDGFB-11R GAATGGCTCAGGCCATGAGCCGTGG Anti-sense PDGFB-12F CCATGCAGCTGCCCTATGACTCC Sense 12 - 16 PDGFB-12R GTCCATGTAGCCACCGTCGCTCTCC Anti-sense PDGFB-13F CTACCTGCACCGCAACAAACACACC Sense 15 - 18 PDGFB-13R CTCTGTGGACGCAGTTCTTGGAGG Anti-sense PDGFB-14F CTTTGATCAACGAGTCTCCAGTGC Sense 17 - 21 PDGFB-14R CTTCTGCATGATCTCATAGATCTCG Anti-sense PDGFB-15F GGATCCTGCTCTGGGAGATCTTCACC Sense 19 - 22 PDGFB-15R GTATAGAGGACGGAGCTGGTGTCC Anti-sense