Table 1.
IC50 values for inhibition of kinase activity by BTKB66
| Kinase | IC50, nM | ||
|---|---|---|---|
| Btk | 13.3 | ||
|
| |||
| TEC | 195 | ||
|
| |||
| BLK | 325 | ||
|
| |||
| FGR | 469 | ||
|
| |||
| PTK6 (Brk) | 493 | ||
|
| |||
| ABL1 | FRK (PTK5) | PAK1 | >1000 |
| ACVR1B (ALK4) | FYN | PAK2 (PAK65) | |
| ADCK3 | GSK3B | PAK4 | |
| AKT1 (PKB alpha) | HCK | PDGFRA | |
| AKT2 (PKB beta) | IGF1R | PDGFRB | |
| ALK | IKBKB | PDK1 Direct | |
| AURKA (Aurora A) | INSR | PIK3C2B | |
| AURKB (Aurora B) | ITK | PIK3CA/PIK3R1 | |
| AXL | JAK1 | PIK3CG | |
| BMPR2 | JAK2 | PIM1 | |
| BRAF | JAK3 | PIM2 | |
| CDK11 | KDR (VEGFR2) | PIM3 | |
| CDK16 | KIT | PLK1 | |
| CDK2/cyclin A | LCK | PRKACA (PKA) | |
| CDK3/cyclin E1 | LYN A | PRKCE | |
| CDK7/cyclin H | MAP2K1 (MEK1) | PTK2 (FAK) | |
| CDK9/cyclin T1 | MAP2K2 (MEK2) | RAF1 (cRAF) | |
| CHEK1 (CHK1) | MAP3K9 (MLK1) | RET | |
| CHUK (IKK alpha) | MAPK10 (JNK3) | RIPK2 | |
| CSF1R (FMS) | MAPK14 (p38 alpha) | ROCK2 | |
| CSK | MAPK3 (ERK1) | RPS6KA1 (RSK1) | |
| CSNK1D | MAPK8 (JNK1) | SRC | |
| CSNK1G2 | MAPK9 (JNK2) | STK22D (TSSK1) | |
| DCAMKL1 | MAPKAPK2 | STK32C (YANK3) | |
| DYRK1B | MARK3 | SYK | |
| EGFR (ErbB1) | MET (cMet) | TEK (Tie2) | |
| EPHA2 | MKNK1 | TGFBR1 (ALK5) | |
| ERBB2 (HER2) | MKNK2 | TYK2 | |
| FER | NEK2 | ULK2 | |
| FGFR2 | NTRK1 (TRKA) | YES1 | |
| FGFR3 | NUAK2 | ZAP70 | |
| FLT3 | |||