Table 5. Selectivity of 1, 2, and 3 over SRC Family Kinases.
| kinase | compd 1 IC50 (nM) (fold selectivity) | compd 2 IC50 (nM) (fold selectivity) | compd 3 IC50 (nM) (fold selectivity) |
|---|---|---|---|
| BTK | 0.27 | 0.32 | 0.31 |
| BLK | 84 (311) | 42 (131) | 20 (65) |
| BMX | 28 (104) | 20 (62) | 11 (34) |
| CSK | ND | 253 (791) | 201 (648) |
| ERBB4 | 118 (437) | 81 (253) | 65 (203) |
| FGR | ND | 55 (172) | 37 (116) |
| FRK | 361 (1337) | 187 (584) | 111 (347) |
| FYN | ND | 322 (1006) | 198 (619) |
| ITK | ND | 921 (2878) | 1200 (3750) |
| LCK | 36 (133) | 22 (69) | 12 (38) |
| LYNB | 399 (1478) | 184 (575) | 131 (423) |
| PTK6 | 66 (244) | 63 (197) | 60 (194) |
| SRC | ND | 116 (362) | 89 (287) |
| SRMS | 32 (119) | 24 (75) | 23 (74) |
| TEC | 167 (619) | 69 (216) | 63 (203) |
| TXK | 49 (181) | 32 (100) | 33 (106) |
| YES1 | ND | 43 (134) | 21 (68) |