Compound Information
Test on : GPCR
Compound Name : SB-253226
Inchikey : INPGJMSTKSQOMI-UHFFFAOYSA-N
ChemSpider : 13469674
Pubchem CID : 15872407
ChEMBL : CHEMBL275666
|
DRx |
RBC |
Metz |
Millipore |
GPCR |
bioactivity |
Kd (nM) |
Remain Activity (%) |
Ki (nM) |
Remain Activity (%) |
Inhibition (%) |
active criteria |
<3000nM |
<50% |
<1000nM |
<50% |
>50% |
TK
TK - JakA
Bioactivity |
---|
Kinase | GPCR |
---|
JAK1 | inactive (7.58%) |
TYK2 | inactive (-2.19%) |
JAK2 | inactive (0.05%) |
JAK3 | inactive (2.36%) |
TK - Fer
Bioactivity |
---|
Kinase | GPCR |
---|
FER | inactive (3.43%) |
FES | inactive (4.61%) |
TK - Abl
Bioactivity |
---|
Kinase | GPCR |
---|
ABL1 | inactive (7.86%) |
ABL2 | inactive (8.03%) |
TK - Csk
Bioactivity |
---|
Kinase | GPCR |
---|
CSK | inactive (5.55%) |
TK - Tec
Bioactivity |
---|
Kinase | GPCR |
---|
BMX | inactive (4.97%) |
BTK | inactive (2.74%) |
TXK | inactive (5.97%) |
TEC | inactive (7.26%) |
ITK | inactive (2.14%) |
TK - Src
Bioactivity |
---|
Kinase | GPCR |
---|
BRK | inactive (7.39%) |
SRM | inactive (0.72%) |
FRK | inactive (4.39%) |
BLK | inactive (5.32%) |
LCK | inactive (7.84%) |
HCK | inactive (8.66%) |
FGR | inactive (6.39%) |
FYN | inactive (6.48%) |
SRC | inactive (7.46%) |
YES | inactive (3.28%) |
TK - Eph
Bioactivity |
---|
Kinase | GPCR |
---|
EphA2 | inactive (1.66%) |
EphA4 | inactive (12.22%) |
EphA3 | inactive (4.31%) |
EphB4 | inactive (3.51%) |
EphB3 | inactive (4.25%) |
EphB2 | inactive (10.62%) |
TK - FAK
Bioactivity |
---|
Kinase | GPCR |
---|
PYK2 | inactive (6.56%) |
TK - Syk
Bioactivity |
---|
Kinase | GPCR |
---|
SYK | inactive (-3.7%) |
ZAP70 | inactive (2.23%) |
TK - ALK
Bioactivity |
---|
Kinase | GPCR |
---|
LTK | inactive (4.42%) |
ALK | inactive (5.34%) |
TK - Sev
Bioactivity |
---|
Kinase | GPCR |
---|
ROS | inactive (7.94%) |
TK - InsR
Bioactivity |
---|
Kinase | GPCR |
---|
INSR | inactive (3.65%) |
IGF1R | inactive (6.06%) |
IRR | inactive (3.68%) |
TK - DDR
Bioactivity |
---|
Kinase | GPCR |
---|
DDR2 | inactive (2.26%) |
TK - Musk
Bioactivity |
---|
Kinase | GPCR |
---|
MUSK | inactive (-1.08%) |
TK - Trk
Bioactivity |
---|
Kinase | GPCR |
---|
TRKA | inactive (0.88%) |
TRKB | inactive (2.43%) |
TRKC | inactive (2.38%) |
TK - Met
Bioactivity |
---|
Kinase | GPCR |
---|
RON | inactive (3.73%) |
MET | inactive (6.95%) |
TK - Axl
Bioactivity |
---|
Kinase | GPCR |
---|
AXL | inactive (-6.06%) |
MER | inactive (-0.63%) |
TYRO3 | inactive (0.95%) |
TK - Ret
Bioactivity |
---|
Kinase | GPCR |
---|
RET | inactive (6.72%) |
TK - FGFR
Bioactivity |
---|
Kinase | GPCR |
---|
FGFR1 | inactive (5.84%) |
FGFR2 | inactive (11.04%) |
FGFR3 | inactive (7.98%) |
FGFR4 | inactive (1.92%) |
TK - VEGFR
Bioactivity |
---|
Kinase | GPCR |
---|
FLT1 | inactive (1.06%) |
KDR | inactive (7.38%) |
FLT4 | inactive (5.6%) |
TK - PDGFR
Bioactivity |
---|
Kinase | GPCR |
---|
FMS | inactive (10.25%) |
KIT | inactive (-6.01%) |
FLT3 | inactive (5.18%) |
PDGFRa | inactive (14.61%) |
PDGFRb | inactive (9.63%) |
TK - Tie
Bioactivity |
---|
Kinase | GPCR |
---|
TIE2 | inactive (6.06%) |
TK - Ack
Bioactivity |
---|
Kinase | GPCR |
---|
ACK | inactive (1.64%) |
TNK1 | inactive (6.8%) |
TK - EGFR
Bioactivity |
---|
Kinase | GPCR |
---|
EGFR | inactive (5.74%) |
ErbB2 | inactive (5.77%) |
ErbB4 | inactive (14.13%) |
TKL
TKL
Test Member No. in Family |
---|
Family | no. Member on 518kinase | GPCR |
---|
IRAK | 4 | 1 |
RAF | 5 | 1 |
TKL - IRAK
Bioactivity |
---|
Kinase | GPCR |
---|
IRAK4 | inactive (2.24%) |
TKL - RAF
Bioactivity |
---|
Kinase | GPCR |
---|
BRAF | inactive (9.1%) |
STE
STE
Test Member No. in Family |
---|
Family | no. Member on 518kinase | GPCR |
---|
STE20 | 31 | 12 |
STE7 | 7 | 1 |
STE - STE20
Bioactivity |
---|
Kinase | GPCR |
---|
GCK | inactive (4.65%) |
MST1 | inactive (5.74%) |
MST2 | inactive (7.64%) |
MST4 | inactive (4.79%) |
HGK | inactive (8.02%) |
MINK | inactive (8.63%) |
LOK | inactive (11.94%) |
PAK1 | inactive (7.76%) |
PAK3 | inactive (5.85%) |
PAK2 | inactive (2.63%) |
PAK5 | inactive (1.97%) |
PAK6 | inactive (-4.55%) |
STE - STE7
Bioactivity |
---|
Kinase | GPCR |
---|
MAP2K1 | inactive (5.27%) |
CK1
CK1
Test Member No. in Family |
---|
Family | no. Member on 518kinase | GPCR |
---|
CK1 | 7 | 4 |
CK1 - CK1
Bioactivity |
---|
Kinase | GPCR |
---|
CK1a | inactive (21.08%) |
CK1g2 | inactive (8.41%) |
CK1g1 | inactive (12.7%) |
CK1g3 | inactive (18.39%) |
Other
Other
Test Member No. in Family |
---|
Family | no. Member on 518kinase | GPCR |
---|
PLK | 4 | 1 |
Aur | 3 | 3 |
NEK | 11 | 5 |
IKK | 4 | 4 |
TTK | 1 | 1 |
Other - PLK
Bioactivity |
---|
Kinase | GPCR |
---|
PLK1 | inactive (3.12%) |
Other - Aur
Bioactivity |
---|
Kinase | GPCR |
---|
AurB | inactive (5.56%) |
AurC | inactive (3.96%) |
AurA | inactive (5.75%) |
Other - NEK
Bioactivity |
---|
Kinase | GPCR |
---|
NEK1 | inactive (3.2%) |
NEK2 | inactive (6.98%) |
NEK9 | inactive (4.49%) |
NEK7 | inactive (6.62%) |
NEK6 | inactive (2.74%) |
Other - IKK
Bioactivity |
---|
Kinase | GPCR |
---|
TBK1 | inactive (3.82%) |
IKKe | inactive (6.98%) |
IKKb | inactive (8.48%) |
IKKa | inactive (4.69%) |
Other - TTK
Bioactivity |
---|
Kinase | GPCR |
---|
TTK | inactive (14.65%) |
AGC
AGC - GRK
Bioactivity |
---|
Kinase | GPCR |
---|
GPRK7 | inactive (2.14%) |
GPRK6 | inactive (3.94%) |
AGC - PDK1
Bioactivity |
---|
Kinase | GPCR |
---|
PDK1 | inactive (0.46%) |
AGC - RSK
Bioactivity |
---|
Kinase | GPCR |
---|
MSK1 | inactive (2.67%) |
MSK2 | inactive (1.93%) |
RSK1 | inactive (5.59%) |
RSK2 | inactive (-0.14%) |
RSK4 | inactive (0.63%) |
RSK3 | inactive (2.82%) |
p70S6K | inactive (2.87%) |
AGC - Akt
Bioactivity |
---|
Kinase | GPCR |
---|
AKT2 | inactive (3.94%) |
AKT1 | inactive (1.68%) |
AKT3 | inactive (6.2%) |
AGC - SGK
Bioactivity |
---|
Kinase | GPCR |
---|
SGK1 | inactive (3.32%) |
SGK3 | inactive (5.02%) |
SGK2 | inactive (5.28%) |
AGC - PKC
Bioactivity |
---|
Kinase | GPCR |
---|
PKCh | inactive (3.59%) |
PKCg | inactive (3.52%) |
PKCa | inactive (3.09%) |
PKCt | inactive (2.89%) |
PKCi | inactive (3.51%) |
AGC - PKG
Bioactivity |
---|
Kinase | GPCR |
---|
PKG2 | inactive (3.81%) |
PKG1 | inactive (3.98%) |
AGC - PKA
Bioactivity |
---|
Kinase | GPCR |
---|
PRKX | inactive (3.28%) |
AGC - DMPK
Bioactivity |
---|
Kinase | GPCR |
---|
ROCK1 | inactive (3.13%) |
ROCK2 | inactive (3.72%) |
MRCKb | inactive (-0.47%) |
MRCKa | inactive (0.21%) |
CAMK
CAMK - RAD53
Bioactivity |
---|
Kinase | GPCR |
---|
CHK2 | inactive (1.85%) |
CAMK - DCAMKL
Bioactivity |
---|
Kinase | GPCR |
---|
DCLK2 | inactive (3.67%) |
CAMK - CAMK1
Bioactivity |
---|
Kinase | GPCR |
---|
CaMK4 | inactive (1.47%) |
CaMK1d | inactive (0.93%) |
CAMK - PHK
Bioactivity |
---|
Kinase | GPCR |
---|
PHKg1 | inactive (7.21%) |
PHKg2 | inactive (7.18%) |
CAMK - CAMK2
Bioactivity |
---|
Kinase | GPCR |
---|
CaMK2d | inactive (5.24%) |
CaMK2a | inactive (2.6%) |
CAMK - MAPKAPK
Bioactivity |
---|
Kinase | GPCR |
---|
MAPKAPK5 | inactive (2.15%) |
MAPKAPK2 | inactive (1.85%) |
MAPKAPK3 | inactive (28.95%) |
MNK2 | inactive (0.21%) |
MNK1 | inactive (2.55%) |
CAMK - PKD
Bioactivity |
---|
Kinase | GPCR |
---|
PKD3 | inactive (5.25%) |
PKD1 | inactive (7.95%) |
PKD2 | inactive (4.6%) |
CAMK - CAMKL
Bioactivity |
---|
Kinase | GPCR |
---|
MARK4 | inactive (2.99%) |
MARK3 | inactive (4.6%) |
MARK1 | inactive (3.58%) |
QIK | inactive (9.11%) |
SIK | inactive (10.13%) |
NuaK1 | inactive (-0.11%) |
BRSK1 | inactive (2.06%) |
BRSK2 | inactive (3.08%) |
MELK | inactive (5.2%) |
CHK1 | inactive (8.71%) |
PASK | inactive (0.95%) |
AMPKa1 | inactive (4.51%) |
AMPKa2 | inactive (3.9%) |
CAMK - TSSK
Bioactivity |
---|
Kinase | GPCR |
---|
TSSK2 | inactive (2.98%) |
TSSK1 | inactive (5.46%) |
CAMK - DAPK
Bioactivity |
---|
Kinase | GPCR |
---|
DAPK1 | inactive (7.45%) |
CAMK - PIM
Bioactivity |
---|
Kinase | GPCR |
---|
PIM2 | inactive (0.36%) |
PIM3 | inactive (1.37%) |
PIM1 | inactive (1.39%) |
CMGC
CMGC - MAPK
Bioactivity |
---|
Kinase | GPCR |
---|
JNK2 | inactive (5.84%) |
p38a | active (70.95%) |
p38b | inactive (20.19%) |
p38d | inactive (4.72%) |
Erk2 | inactive (8.71%) |
Erk1 | inactive (5.11%) |
CMGC - GSK
Bioactivity |
---|
Kinase | GPCR |
---|
GSK3A | inactive (3.44%) |
GSK3B | inactive (2.16%) |
CMGC - SRPK
Bioactivity |
---|
Kinase | GPCR |
---|
SRPK1 | inactive (-2.22%) |
MSSK1 | inactive (-0.93%) |
CMGC - CLK
Bioactivity |
---|
Kinase | GPCR |
---|
CLK3 | inactive (1.46%) |
CLK2 | inactive (0.21%) |
CMGC - DYRK
Bioactivity |
---|
Kinase | GPCR |
---|
HIPK1 | inactive (-0.28%) |
HIPK4 | inactive (0.14%) |
DYRK1B | inactive (-0.35%) |
DYRK1A | inactive (4.13%) |
DYRK2 | inactive (2.66%) |
CMGC - CK2
Bioactivity |
---|
Kinase | GPCR |
---|
CK2a1 | inactive (6.22%) |