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Binding Assay Kinase Selectivity Data

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Binding Assay Kinase Selectivity Data SelectScreen® Kinase Profiling Service Binding Assay Selectivity Data Kinase Selectivity Results - % Inhibition Compound (1X concentration) BAY-43-9006 BIRB-796 BMS-354825 Gleevec ® Go-6983 H-89 Iressa ® NH125 PI-103 PP2 Kinase (10,000 nM) (10,000 nM) (10,000 nM) (10,000 nM) (10,000 nM) (10,000 nM) (10,000 nM) (10,000 nM) (10,000 nM) (10,000 nM) ACVR1 (ALK2) 7 6 98 14 12 6 29 69 6 99 ACVR2B 35 15 99 13 -12 -15 3 128 -8 88 BMPR1A (ALK3) 10 8 99 7 -2 2 3 122 8 102 BRAF 87 63 102 92 8 4 56 86 76 69 BRAF V599E 98 69 101 98 8 6 57 86 78 72 CAMKK1 (CAMKKA) 3 3 21 8 1 3 33 110 -6 7 CAMKK2 (CaMKK beta) 20 10 11 28 32 7 17 53 6 8 CDK8/cyclin C 78761 68168212691892 CDK9/cyclin K 20 2 -4 4 55 41 -3 66 0 16 CLK4 77 20 12 85 93 77 49 85 31 67 DDR1 99 100 100 100 5 -8 40 51 0 63 DDR2 64 98 103 101 -8 -6 11 57 -2 70 DMPK 12 1 87 5 95 11 76 69 -2 5 EPHA3 54 79 104 12 -1 -5 39 91 6 80 EPHA7 101 106 32 9 23 19 94 90 -6 61 KIT V654A 45 8 99 40 -4 1 15 68 6 25 LIMK1 84 10 101 20 11 46 19 86 7 56 LIMK2 57 8 103 17 33 36 9 87 4 23 MAP2K1 (MEK1) 192 782 109 22701487 MAP2K1 (MEK1) S218D S222D 3311789 202721661783 MAP2K2 (MEK2) 163 742 105 13661482 MAP2K3 (MEK3) 27 7 9 15 12 6 -6 83 -19 11 MAP2K6 (MKK6) 12 12 1 1 13 1 -11 66 4 15 MAP2K6 (MKK6) S207E T211E -1 10 9 3 17 6 -7 65 -2 21 MAP3K10 (MLK2) 254 7314412516614 21 MAP3K11 (MLK3) 241 631030138 500 9 MAP3K14 (NIK) 16 4 -1 22 -3 -3 3 82 -10 21 MAP3K2 (MEKK2) 17 2 88 1 65 4 34 69 -6 68 MAP3K3 (MEKK3) 35 2 92 -9 78 -10 32 77 -11 53 MAP3K5 (ASK1) 2 0 -3 2 1 11 0 23 -9 -1 MAP3K7/MAP3K7IP1 (TAK1-TAB1) 83 11 43 21 42 8 1 56 -4 12 MAPK10 (JNK3) 37 86 10 76 35 11 70 57 8 75 MAPK8 (JNK1) 1 231 81180 42861730 MAPK9 (JNK2) 87 104 -5 54 35 4 78 89 12 59 MLCK (MLCK2) 46 20 40 23 16 45 44 53 15 22 MKNK2 (MNK2) 84 42 28 32 8 26 87 76 0 24 MYLK (MLCK) 10 6 4 5 53 3 3 71 29 17 NLK 18 25 101 25 21 22 70 104 14 105 RAF1 (cRAF) Y340D Y341D 99 86 100 97 3 -1 31 85 73 85 RIPK2 73 5 100 37 2 6 100 87 14 100 SLK 25 20 68 6 72 23 81 47 4 31 STK16 (PKL12) 3 -10 8 38 51 2 -1 84 1 44 STK17A (DRAK1) 37 15 11 60 52 39 64 74 1 7 STK33 443 1120888940726 17 TAOK3 (JIK) 74 13 25 15 15 23 -7 63 0 14 TEC 3 -1 99 -6 2 -9 -4 61 -3 28 TGFBR1 (ALK5) 7 4 101 7 69 8 28 83 9 96 TNK2 (ACK) 12 6 101 22 15 1 56 63 6 85 TTK 92 59 -4 14 15 -2 37 80 11 28 WEE1 -6 7 100 10 3 -6 31 107 7 19 WNK2 6 12 101 63 1 -12 7 114 4 57 ZAK 81 42 101 24 6 0 8 67 1 39 0%-40% inhibition TARCEVA® is a registered trademark of OSI Pharmaceuticals, Inc. Gleevec® is a registered trademark of Novartis AG 40%-80% inhibition SUTENT® is a registered trademark of Pfizer, Inc. Iressa® is a registered trademark of Astra Zeneca PLC >80% inhibition 1 June 2010 SelectScreen® Kinase Profiling Service Binding Assay Selectivity Data Kinase Selectivity Results - % Inhibition Compound (1X concentration) BAY-43-9006 BIRB-796 BMS-354825 Gleevec ® Go-6983 H-89 Iressa ® NH125 PI-103 PP2 Kinase (1000 nM) (1000 nM) (1000 nM) (1000 nM) (1000 nM) (1000 nM) (1000 nM) (1000 nM) (1000 nM) (1000 nM) ACVR1 (ALK2) 3679543941094 ACVR2B 17 0 79 41 -7 -8 -10 0 8 83 BMPR1A (ALK3) 4 6 57 5 -2 2 3 19 5 90 BRAF 48 29 94 56 7 1 16 3 67 45 BRAF V599E 59 33 94 67 4 3 15 5 70 45 CAMKK1 (CAMKKA) -3 2 2 -1 -3 -4 0 -7 -6 -1 CAMKK2 (CaMKK beta) 03-146-30703 CDK8/cyclin C 47431 22113613199 68 CDK9/cyclin K 1 0 -3 0 14 6 -1 -3 5 5 CLK4 238 12477431210 5634 DDR1 84 85 100 97 4 2 5 3 1 37 DDR2 42 45 88 74 -1 0 -1 9 0 45 DMPK 1 2 47 0 76 2 30 14 0 0 EPHA3 12 16 104 3 -1 -5 6 -8 0 46 EPHA7 44 95 -2 7 2 5 56 9 -1 26 KIT V654A 24 4 94 12 1 0 5 17 5 9 LIMK1 45 8 86 8 6 11 4 9 2 29 LIMK2 20 4 86 2 8 5 0 12 1 12 MAP2K1 (MEK1) 523610359371 MAP2K1 (MEK1) S218D S222D 15 6 37 6 5 8 5 13 6 55 MAP2K2 (MEK2) 5228332310456 MAP2K3 (MEK3) 10 6 -1 10 1 2 5 4 -16 9 MAP2K6 (MKK6) 4 5 -1 6 -1 0 0 4 -2 6 MAP2K6 (MKK6) S207E T211E 7 12 -2 9 6 0 -1 6 -1 -2 MAP3K10 (MLK2) 202948331308 MAP3K11 (MLK3) 2-22026031021 MAP3K14 (NIK) 35-236102-67 MAP3K2 (MEKK2) 0 -5 47 -4 19 -3 5 -2 -5 35 MAP3K3 (MEKK3) -3 3 69 -9 37 -6 11 -16 -13 28 MAP3K5 (ASK1) 0-2110-21-5-4-2 MAP3K7/MAP3K7IP1 (TAK1-TAB1) 35 -81 7 3 6 1 -2 -2 6 5 MAPK10 (JNK3) 10 51 4 36 10 4 26 4 9 42 MAPK8 (JNK1) -1 8 4 34 2 3 13 14 9 9 MAPK9 (JNK2) 23 99 2 15 5 0 26 11 7 31 MLCK (MLCK2) 58 10 4 3 -2 -1 59 2 0 10 MKNK2 (MNK2) 139 127 9 1112121611 MYLK (MLCK) 2 4 1 2 17 4 0 -1 38 5 NLK 12 13 77 8 3 9 18 16 7 102 RAF1 (cRAF) Y340D Y341D 73 49 92 75 1 -1 10 11 59 69 RIPK2 38 2 100 8 2 1 96 18 14 100 SLK 5 8 29 1 30 6 48 10 3 16 STK16 (PKL12) 0 -5 3 10 10 4 1 -1 9 15 STK17A (DRAK1) 15126 22291021253 -6 STK33 12 1 1 4 50 53 7 4 10 3 TAOK3 (JIK) 4255236-15-23 TEC -4 -5 83 -3 -2 -2 -1 7 -12 7 TGFBR1 (ALK5) 2 4 97 3 24 -1 5 8 3 88 TNK2 (ACK) 1 2 101 5 2 1 13 9 0 59 TTK 36 21 -2 4 1 -3 10 12 8 7 WEE1 -358360-37876 WNK2 1 3 66 14 1 -1 2 19 2 30 ZAK 50 12 97 6 -1 -2 0 10 1 18 0%-40% inhibition TARCEVA® is a registered trademark of OSI Pharmaceuticals, Inc. Gleevec® is a registered trademark of Novartis AG 40%-80% inhibition SUTENT® is a registered trademark of Pfizer, Inc. Iressa® is a registered trademark of Astra Zeneca PLC >80% inhibition 2 June 2010 SelectScreen® Kinase Profiling Service Binding Assay Selectivity Data Kinase Selectivity Results - % Inhibition Compound (1X concentration) PTK-787 Ro-31-8220 Roscovitine SB 202190 Staurosporine Sutent Tarceva Tyrphostin AG1478 Y27632 Kinase (10,000 nM) (10,000 nM) (10,000 nM) (10,000 nM) (10,000 nM) (10,000 nM) (10,000 nM) (10,000 nM) (10,000 nM) ACVR1 (ALK2) 4 47 3 86 94 73 11 66 64 ACVR2B 2-362 8075111255-2 BMPR1A (ALK3) 5 -17 -1 58 85 22 3 37 34 BRAF 65 26 2 101 4 12 45 51 51 BRAF V599E 68443 992714416354 CAMKK1 (CAMKKA) -5239 -29995113229 CAMKK2 (CaMKK beta) -1 82 17 14 94 90 18 28 25 CDK8/cyclin C 43 52 20 64 109 8 6 13 9 CDK9/cyclin K -4 86 83 14 93 55 1 2 0 CLK4 8 8087349796476976 DDR1 55420 7599414275-2 DDR2 28 22 -1 59 95 44 16 34 31 DMPK 0 90 3 32 80 67 71 60 55 EPHA3 2 -1 2 16 102 54 33 47 0 EPHA7 5 3016578592808092 KIT V654A 6217106 6693323224 LIMK1 4 -2 2 16 96 40 15 22 27 LIMK2 3 48 2 13 86 23 9 19 9 MAP2K1 (MEK1) 1 19 3 38 98 98 22 52 51 MAP2K1 (MEK1) S218D S222D 4 33 5 36 100 97 26 41 44 MAP2K2 (MEK2) 1 18 2 40 99 100 19 40 36 MAP2K3 (MEK3) -9 -13 1 -13 52 58 -29 -13 -14 MAP2K6 (MKK6) -2 19 5 6 82 47 0 6 -1 MAP2K6 (MKK6) S207E T211E -10 48 0 4 82 56 -4 10 3 MAP3K10 (MLK2) 3 78 2 80 86 71 50 23 26 MAP3K11 (MLK3) -1620 598489283237 MAP3K14 (NIK) 7 -2 0 7 89 76 5 15 9 MAP3K2 (MEKK2) 9 73 0 4 88 102 -4 65 48 MAP3K3 (MEKK3) 25 46 -8 10 71 109 46 74 62 MAP3K5 (ASK1) -7 -8 1 -7 87 67 -6 5 -2 MAP3K7/MAP3K7IP1 (TAK1-TAB1) 2 724 1 9598171824 MAPK10 (JNK3) 13 60 38 101 90 52 35 67 70 MAPK8 (JNK1) -4 36 10 83 99 44 18 31 36 MAPK9 (JNK2) 11 68 25 101 78 53 49 71 69 MLCK (MLCK2) 3 6813137597475749 MKNK2 (MNK2) 2 5 -1 12 100 52 75 77 27 MYLK (MLCK) 3 90 10 7 95 95 30 54 50 NLK 8 66 6 103 97 18 30 77 75 RAF1 (cRAF) Y340D Y341D 58 17 3 100 15 17 17 35 29 RIPK2 22 24 1 100 90 77 98 99 15 SLK 8 93 7 48 95 90 96 89 85 STK16 (PKL12) -9 72 18 4 98 95 -2 6 1 STK17A (DRAK1) 0 6310275899296769 STK33 1 91 20 16 92 100 24 30 26 TAOK3 (JIK) 18 68 6 8 98 39 1 -1 -6 TEC -6 -18 -3 -5 56 5 6 3 -4 TGFBR1 (ALK5) 7 83 2 93 90 51 29 47 48 TNK2 (ACK) 4 22 5 29 95 74 63 82 79 TTK 18 46 78 39 71 90 37 29 50 WEE1 -3479 279297274335 WNK2 9 7 11 12 86 34 20 25 24 ZAK 44255 482436203122 0%-40% inhibition TARCEVA® is a registered trademark of OSI Pharmaceuticals, Inc.
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