Compound Information
Test on : DRx
Compound Name : Fedratinib
Inchikey : JOOXLOJCABQBSG-UHFFFAOYSA-N
ChemSpider : 17626393
Pubchem CID : 16722836
ChEMBL : CHEMBL1287853
|
DRx |
RBC |
Metz |
Millipore |
GPCR |
| bioactivity |
Kd (nM) |
Remain Activity (%) |
Ki (nM) |
Remain Activity (%) |
Inhibition (%) |
| active criteria |
<3000nM |
<50% |
<1000nM |
<50% |
>50% |
Other
Other - NAK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| AAK1 | active (35nM) |
| BIKE | active (32nM) |
| GAK | active (1.1nM) |
| MPSK1 | active (6.6nM) |
Other - Aur
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| AurA | inactive (4400nM) |
| AurB | active (490nM) |
| AurC | active (350nM) |
Other - CAMKK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| CaMKK1 | active (1800nM) |
| CaMKK2 | inactive (4000nM) |
Other - PEK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| HRI | active (1000nM) |
| PKR | active (1100nM) |
Other - IRE
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| IRE1 | active (1200nM) |
Other - IKK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| IKKa | active (830nM) |
| IKKb | active (360nM) |
| IKKe | active (360nM) |
| TBK1 | active (92nM) |
Other - NEK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| NEK1 | inactive (3400nM) |
| NEK11 | active (1200nM) |
| NEK2 | active (1700nM) |
| NEK3 | active (640nM) |
| NEK4 | active (1600nM) |
| NEK5 | active (570nM) |
| NEK6 | active (120nM) |
| NEK7 | active (160nM) |
| NEK9 | active (150nM) |
Other - WEE
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| MYT1 | inactive (10001nM) |
| Wee1 | active (390nM) |
| Wee1B | inactive (6000nM) |
Other - PLK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| PLK1 | active (280nM) |
| PLK2 | active (2400nM) |
| PLK3 | active (1600nM) |
| PLK4 | active (96nM) |
Other - SgK496
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| SgK496 | active (1700nM) |
Other - NKF1
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| SBK | active (790nM) |
| SgK110 | active (2900nM) |
Other - NKF4
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| CLIK1 | inactive (10001nM) |
Other - ULK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| Fused | active (870nM) |
| ULK1 | active (270nM) |
| ULK2 | active (79nM) |
| ULK3 | active (290nM) |
Other - TLK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| TLK1 | active (1300nM) |
| TLK2 | active (2000nM) |
Other - TTK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| TTK | active (450nM) |
TK
TK - Abl
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| ABL1 | active (180nM) |
| ABL2 | active (570nM) |
TK - ALK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| ALK | active (650nM) |
| LTK | inactive (6300nM) |
TK - Axl
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| AXL | active (160nM) |
| MER | active (820nM) |
| TYRO3 | inactive (10001nM) |
TK - Src
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| BLK | active (650nM) |
| BRK | active (1200nM) |
| FGR | active (82nM) |
| FRK | active (200nM) |
| FYN | active (38nM) |
| HCK | active (2100nM) |
| LCK | active (72nM) |
| LYN | active (500nM) |
| SRC | active (75nM) |
| SRM | inactive (5000nM) |
| YES | active (120nM) |
TK - Tec
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| BMX | active (1200nM) |
| BTK | active (850nM) |
| ITK | active (490nM) |
| TEC | inactive (10001nM) |
| TXK | active (1500nM) |
TK - PDGFR
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| FMS | active (620nM) |
| FLT3 | active (13nM) |
| KIT | active (130nM) |
| PDGFRa | active (2700nM) |
| PDGFRb | active (45nM) |
TK - Csk
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| CSK | inactive (5900nM) |
| CTK | active (1700nM) |
TK - DDR
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| DDR1 | active (1900nM) |
| DDR2 | active (950nM) |
TK - EGFR
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| EGFR | inactive (3400nM) |
| ErbB2 | inactive (10001nM) |
| ErbB3 | inactive (10001nM) |
| ErbB4 | active (2000nM) |
TK - Eph
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| EphA1 | active (730nM) |
| EphA2 | inactive (4400nM) |
| EphA3 | inactive (7100nM) |
| EphA4 | inactive (4000nM) |
| EphA5 | inactive (10001nM) |
| EphA6 | inactive (3900nM) |
| EphA7 | inactive (6500nM) |
| EphA8 | inactive (7700nM) |
| EphB1 | active (1700nM) |
| EphB2 | inactive (3900nM) |
| EphB3 | inactive (10001nM) |
| EphB4 | active (2100nM) |
| EphB6 | active (300nM) |
TK - FAK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| FAK | active (42nM) |
| PYK2 | active (220nM) |
TK - Fer
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| FER | active (1100nM) |
| FES | active (530nM) |
TK - FGFR
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| FGFR1 | active (280nM) |
| FGFR2 | active (470nM) |
| FGFR3 | active (360nM) |
| FGFR4 | active (2000nM) |
TK - VEGFR
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| FLT1 | inactive (4300nM) |
| FLT4 | active (2000nM) |
| KDR | inactive (5200nM) |
TK - InsR
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| IGF1R | active (2200nM) |
| INSR | active (850nM) |
| IRR | active (1600nM) |
TK - JakA
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| JAK1 | active (18nM) |
| JAK2 | active (1.1nM) |
| JAK3 | active (74nM) |
| TYK2 | active (21nM) |
TK - Met
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| MET | inactive (8500nM) |
| RON | inactive (10001nM) |
TK - Musk
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| MUSK | active (800nM) |
TK - Ret
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| RET | active (130nM) |
TK - Sev
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| ROS | active (600nM) |
TK - Syk
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| SYK | active (2700nM) |
| ZAP70 | inactive (3800nM) |
TK - Tie
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| TIE1 | active (700nM) |
| TIE2 | active (1900nM) |
TK - Ack
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| TNK1 | active (360nM) |
| ACK | active (64nM) |
TK - Trk
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| TRKA | active (840nM) |
| TRKB | inactive (3100nM) |
| TRKC | inactive (8600nM) |
TKL
TKL - STKR
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| ALK2 | active (150nM) |
| ALK4 | inactive (6700nM) |
| ACTR2 | inactive (10001nM) |
| ACTR2B | inactive (10001nM) |
| ALK1 | active (2400nM) |
| BMPR1A | inactive (10001nM) |
| BMPR1B | active (410nM) |
| BMPR2 | active (2900nM) |
| TGFbR1 | inactive (10001nM) |
| TGFbR2 | active (1100nM) |
TKL - RIPK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| SgK288 | inactive (4300nM) |
| RIPK1 | inactive (5300nM) |
| RIPK2 | inactive (6100nM) |
| ANKRD3 | inactive (9800nM) |
TKL - RAF
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| BRAF | inactive (9800nM) |
| RAF1 | inactive (10001nM) |
TKL - MLK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| DLK | inactive (6300nM) |
| LZK | active (590nM) |
| MLK1 | inactive (3200nM) |
| MLK2 | inactive (6900nM) |
| MLK3 | inactive (3100nM) |
| TAK1 | inactive (3100nM) |
| HH498 | active (1800nM) |
| ZAK | active (650nM) |
TKL - IRAK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| IRAK1 | active (220nM) |
| IRAK3 | active (120nM) |
| IRAK4 | active (1200nM) |
TKL - LISK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| LIMK1 | active (940nM) |
| LIMK2 | inactive (7900nM) |
| TESK1 | inactive (3200nM) |
TKL - LRRK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| LRRK2 | active (870nM) |
Atypical
Atypical
| Test Member No. in Family |
|---|
| Family | no. Member on 518kinase | DRx |
|---|
| ABC1 | 5 | 2 |
| PIKK | 6 | 1 |
| RIO | 3 | 3 |
| Alpha | 6 | 1 |
Atypical - ABC1
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| ADCK3 | inactive (7000nM) |
| ADCK4 | active (300nM) |
Atypical - PIKK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| FRAP | inactive (10001nM) |
Atypical - RIO
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| RIOK1 | active (100nM) |
| RIOK2 | active (2600nM) |
| RIOK3 | active (91nM) |
Atypical - Alpha
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| ChaK2 | inactive (10001nM) |
AGC
AGC - Akt
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| AKT1 | inactive (10001nM) |
| AKT2 | inactive (10001nM) |
| AKT3 | inactive (10001nM) |
AGC - DMPK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| CRIK | active (140nM) |
| DMPK1 | active (1000nM) |
| DMPK2 | inactive (10001nM) |
| MRCKa | inactive (10001nM) |
| MRCKb | inactive (10001nM) |
| ROCK1 | active (2100nM) |
| ROCK2 | active (2200nM) |
AGC - GRK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| RHOK | inactive (10001nM) |
| GPRK4 | active (170nM) |
| GPRK7 | active (2600nM) |
AGC - NDR
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| LATS1 | inactive (10001nM) |
| LATS2 | inactive (8000nM) |
| NDR1 | inactive (5800nM) |
| NDR2 | inactive (10001nM) |
AGC - MAST
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| MAST1 | inactive (10001nM) |
AGC - PDK1
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| PDK1 | inactive (10001nM) |
AGC - PKA
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| PKACa | inactive (10001nM) |
| PKACb | inactive (10001nM) |
| PRKX | inactive (10001nM) |
AGC - PKN
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| PKN1 | active (1100nM) |
| PKN2 | inactive (10001nM) |
AGC - PKC
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| PKCd | inactive (10001nM) |
| PKCe | inactive (8100nM) |
| PKCh | inactive (10001nM) |
| PKCi | inactive (10001nM) |
| PKCt | inactive (10001nM) |
AGC - PKG
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| PKG1 | inactive (3800nM) |
| PKG2 | active (1600nM) |
AGC - RSK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| p70S6K | active (2000nM) |
AGC - SGK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| SGK3 | active (2500nM) |
AGC - YANK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| YANK1 | inactive (10001nM) |
| YANK2 | inactive (10001nM) |
| YANK3 | inactive (10001nM) |
CAMK
CAMK - CAMKL
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| AMPKa1 | active (2400nM) |
| AMPKa2 | inactive (4700nM) |
| NuaK1 | active (34nM) |
| BRSK1 | inactive (10001nM) |
| BRSK2 | inactive (10001nM) |
| CHK1 | inactive (3800nM) |
| HUNK | inactive (10001nM) |
| LKB1 | active (310nM) |
| MARK1 | active (700nM) |
| MARK2 | inactive (3100nM) |
| MARK3 | active (300nM) |
| MARK4 | active (970nM) |
| MELK | active (2600nM) |
| NIM1 | inactive (4400nM) |
| QSK | active (1900nM) |
| SIK | active (39nM) |
| QIK | active (98nM) |
| NuaK2 | active (49nM) |
| SNRK | active (230nM) |
CAMK - CAMK1
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| CaMK1a | active (1600nM) |
| CaMK1d | active (460nM) |
| CaMK1g | inactive (3200nM) |
| CaMK4 | inactive (10001nM) |
CAMK - CAMK2
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| CaMK2a | active (300nM) |
| CaMK2b | inactive (6800nM) |
| CaMK2d | active (590nM) |
| CaMK2g | active (540nM) |
CAMK - CASK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| CASK | active (2800nM) |
CAMK - RAD53
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| CHK2 | inactive (10001nM) |
CAMK - DAPK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| DAPK1 | active (16nM) |
| DAPK2 | active (29nM) |
| DAPK3 | active (1.2nM) |
| DRAK1 | active (610nM) |
| DRAK2 | active (45nM) |
CAMK - DCAMKL
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| DCLK1 | active (190nM) |
| DCLK2 | active (870nM) |
| DCLK3 | active (13nM) |
CAMK - MAPKAPK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| MAPKAPK2 | inactive (10001nM) |
| MAPKAPK5 | inactive (10001nM) |
| MNK1 | inactive (7300nM) |
| MNK2 | active (380nM) |
CAMK - MLCK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| caMLCK | inactive (9700nM) |
| smMLCK | active (520nM) |
| skMLCK | active (3000nM) |
| SgK085 | active (130nM) |
CAMK - PHK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| PHKg1 | active (330nM) |
| PHKg2 | active (1600nM) |
CAMK - PIM
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| PIM1 | inactive (10001nM) |
| PIM2 | inactive (10001nM) |
| PIM3 | inactive (10001nM) |
CAMK - PKD
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| PKD1 | inactive (10001nM) |
| PKD2 | inactive (10001nM) |
| PKD3 | inactive (9600nM) |
CAMK - STK33
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| STK33 | active (220nM) |
CAMK - TSSK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| TSSK1 | active (1300nM) |
STE
STE
| Test Member No. in Family |
|---|
| Family | no. Member on 518kinase | DRx |
|---|
| STE11 | 8 | 8 |
| STE20 | 31 | 27 |
| STE7 | 7 | 7 |
STE - STE11
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| MAP3K5 | inactive (10001nM) |
| MAP3K6 | inactive (10001nM) |
| MAP3K1 | inactive (10001nM) |
| MAP3K7 | inactive (10001nM) |
| MAP3K2 | active (580nM) |
| MAP3K3 | active (1300nM) |
| MAP3K4 | inactive (4100nM) |
| MAP3K8 | active (19nM) |
STE - STE20
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| HPK1 | active (1300nM) |
| LOK | active (2900nM) |
| GCK | active (2100nM) |
| KHS2 | active (1800nM) |
| HGK | inactive (10001nM) |
| KHS1 | inactive (10001nM) |
| MINK | inactive (8900nM) |
| MST1 | inactive (10001nM) |
| MST2 | inactive (10001nM) |
| MST3 | inactive (10001nM) |
| MST4 | inactive (7500nM) |
| MYO3A | inactive (10001nM) |
| MYO3B | inactive (10001nM) |
| OSR1 | inactive (10001nM) |
| PAK1 | inactive (3100nM) |
| PAK2 | inactive (6000nM) |
| PAK3 | inactive (10001nM) |
| PAK4 | inactive (3800nM) |
| PAK6 | inactive (6900nM) |
| PAK5 | active (1200nM) |
| SLK | active (680nM) |
| STLK3 | active (1600nM) |
| TAO1 | active (1300nM) |
| TAO2 | active (760nM) |
| TAO3 | active (1900nM) |
| TNIK | inactive (10001nM) |
| YSK1 | inactive (7200nM) |
STE - STE7
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| MAP2K1 | inactive (5100nM) |
| MAP2K2 | inactive (3100nM) |
| MAP2K3 | inactive (3500nM) |
| MAP2K4 | inactive (9900nM) |
| MAP2K5 | active (360nM) |
| MAP2K6 | inactive (10001nM) |
| MAP2K7 | inactive (10001nM) |
CMGC
CMGC - CDK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| PITSLRE | inactive (10001nM) |
| CHED | inactive (10001nM) |
| CDK11 | inactive (10001nM) |
| PCTAIRE1 | inactive (3100nM) |
| PCTAIRE2 | active (350nM) |
| PCTAIRE3 | active (2700nM) |
| PFTAIRE2 | inactive (8600nM) |
| PFTAIRE1 | active (2600nM) |
CMGC - CDKL
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| CDKL1 | inactive (10001nM) |
| CDKL2 | active (1300nM) |
| CDKL3 | inactive (10001nM) |
| CDKL5 | inactive (7300nM) |
CMGC - CLK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| CLK1 | active (2500nM) |
| CLK2 | active (2300nM) |
| CLK3 | inactive (10001nM) |
| CLK4 | active (2000nM) |
CMGC - CK2
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| CK2a1 | active (920nM) |
| CK2a2 | active (120nM) |
CMGC - DYRK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| DYRK1A | inactive (10001nM) |
| DYRK1B | inactive (9500nM) |
| DYRK2 | inactive (10001nM) |
| HIPK1 | active (860nM) |
| HIPK2 | active (1000nM) |
| HIPK3 | active (1300nM) |
| HIPK4 | active (220nM) |
| PRP4 | active (390nM) |
CMGC - MAPK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| Erk1 | inactive (10001nM) |
| Erk2 | inactive (10001nM) |
| Erk3 | active (1200nM) |
| Erk4 | inactive (10001nM) |
| Erk5 | active (66nM) |
| Erk7 | active (510nM) |
| JNK1 | active (260nM) |
| JNK2 | active (240nM) |
| JNK3 | active (200nM) |
| NLK | inactive (10001nM) |
| p38a | inactive (10001nM) |
| p38b | inactive (10001nM) |
| p38d | inactive (10001nM) |
| p38g | inactive (10001nM) |
CMGC - GSK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| GSK3A | inactive (10001nM) |
| GSK3B | inactive (10001nM) |
CMGC - RCK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| ICK | active (1900nM) |
| MAK | inactive (10001nM) |
CMGC - SRPK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| SRPK1 | active (160nM) |
| SRPK2 | active (100nM) |
| MSSK1 | active (170nM) |
CK1
CK1
| Test Member No. in Family |
|---|
| Family | no. Member on 518kinase | DRx |
|---|
| CK1 | 7 | 7 |
| VRK | 3 | 1 |
CK1 - CK1
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| CK1a | inactive (10001nM) |
| CK1a2 | inactive (10001nM) |
| CK1d | inactive (10001nM) |
| CK1e | inactive (10001nM) |
| CK1g1 | inactive (10001nM) |
| CK1g2 | inactive (10001nM) |
| CK1g3 | inactive (10001nM) |
CK1 - VRK
| Bioactivity |
|---|
| Kinase | DRx |
|---|
| VRK2 | inactive (10001nM) |
