Compound Information
Test on : GPCR
Compound Name : SB-278539
Inchikey : ZTUCRQHYVRNKFG-UHFFFAOYSA-N
ChemSpider : 13279848
Pubchem CID : 18536627
ChEMBL : CHEMBL275168
|
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 (0.39%) |
TYK2 | inactive (-2.89%) |
JAK2 | inactive (-1.29%) |
JAK3 | inactive (-0.37%) |
TK - Fer
Bioactivity |
---|
Kinase | GPCR |
---|
FER | inactive (9.05%) |
FES | inactive (0.02%) |
TK - Abl
Bioactivity |
---|
Kinase | GPCR |
---|
ABL1 | inactive (0.8%) |
ABL2 | inactive (-0.16%) |
TK - Csk
Bioactivity |
---|
Kinase | GPCR |
---|
CSK | inactive (-0.81%) |
TK - Tec
Bioactivity |
---|
Kinase | GPCR |
---|
BMX | inactive (1.7%) |
BTK | inactive (1.2%) |
TXK | inactive (1.21%) |
TEC | inactive (0.25%) |
ITK | inactive (1.14%) |
TK - Src
Bioactivity |
---|
Kinase | GPCR |
---|
BRK | inactive (1.01%) |
SRM | inactive (-2.37%) |
FRK | inactive (1.55%) |
BLK | inactive (1.92%) |
LCK | inactive (2.31%) |
HCK | inactive (-0.6%) |
FGR | inactive (2.83%) |
FYN | inactive (3.05%) |
SRC | inactive (2.18%) |
YES | inactive (0.1%) |
TK - Eph
Bioactivity |
---|
Kinase | GPCR |
---|
EphA2 | inactive (-2.87%) |
EphA4 | inactive (2.11%) |
EphA3 | inactive (-1.43%) |
EphB4 | inactive (1.29%) |
EphB3 | inactive (2.14%) |
EphB2 | inactive (3.26%) |
TK - FAK
Bioactivity |
---|
Kinase | GPCR |
---|
PYK2 | inactive (8.77%) |
TK - Syk
Bioactivity |
---|
Kinase | GPCR |
---|
SYK | inactive (0.42%) |
ZAP70 | inactive (-2.6%) |
TK - ALK
Bioactivity |
---|
Kinase | GPCR |
---|
LTK | inactive (0.46%) |
ALK | inactive (1.34%) |
TK - Sev
Bioactivity |
---|
Kinase | GPCR |
---|
ROS | inactive (2.37%) |
TK - InsR
Bioactivity |
---|
Kinase | GPCR |
---|
INSR | inactive (2.85%) |
IGF1R | inactive (5.66%) |
IRR | inactive (-1.6%) |
TK - DDR
Bioactivity |
---|
Kinase | GPCR |
---|
DDR2 | inactive (0.47%) |
TK - Musk
Bioactivity |
---|
Kinase | GPCR |
---|
MUSK | inactive (1.51%) |
TK - Trk
Bioactivity |
---|
Kinase | GPCR |
---|
TRKA | inactive (3.02%) |
TRKB | inactive (0.87%) |
TRKC | inactive (0.67%) |
TK - Met
Bioactivity |
---|
Kinase | GPCR |
---|
RON | inactive (0.73%) |
MET | inactive (-0.9%) |
TK - Axl
Bioactivity |
---|
Kinase | GPCR |
---|
AXL | inactive (0.46%) |
MER | inactive (4.01%) |
TYRO3 | inactive (1.63%) |
TK - Ret
Bioactivity |
---|
Kinase | GPCR |
---|
RET | inactive (0.73%) |
TK - FGFR
Bioactivity |
---|
Kinase | GPCR |
---|
FGFR1 | inactive (-0.19%) |
FGFR2 | inactive (-0.95%) |
FGFR3 | inactive (-0.04%) |
FGFR4 | inactive (-1.06%) |
TK - VEGFR
Bioactivity |
---|
Kinase | GPCR |
---|
FLT1 | inactive (-2.3%) |
KDR | inactive (2%) |
FLT4 | inactive (1.05%) |
TK - PDGFR
Bioactivity |
---|
Kinase | GPCR |
---|
FMS | inactive (0.01%) |
KIT | inactive (2.73%) |
FLT3 | inactive (8.91%) |
PDGFRa | inactive (4.67%) |
PDGFRb | inactive (4.24%) |
TK - Tie
Bioactivity |
---|
Kinase | GPCR |
---|
TIE2 | inactive (0.87%) |
TK - Ack
Bioactivity |
---|
Kinase | GPCR |
---|
ACK | inactive (0.56%) |
TNK1 | inactive (1.53%) |
TK - EGFR
Bioactivity |
---|
Kinase | GPCR |
---|
EGFR | inactive (7.82%) |
ErbB2 | inactive (5.43%) |
ErbB4 | inactive (9.2%) |
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 (0.58%) |
TKL - RAF
Bioactivity |
---|
Kinase | GPCR |
---|
BRAF | inactive (2.82%) |
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 (5.84%) |
MST1 | inactive (0.91%) |
MST2 | inactive (0.79%) |
MST4 | - |
HGK | inactive (1.49%) |
MINK | inactive (1.27%) |
LOK | inactive (3.91%) |
PAK1 | inactive (3.96%) |
PAK3 | inactive (1.84%) |
PAK2 | inactive (-0.01%) |
PAK5 | inactive (0.8%) |
PAK6 | inactive (-10.65%) |
STE - STE7
Bioactivity |
---|
Kinase | GPCR |
---|
MAP2K1 | inactive (3.05%) |
CK1
CK1
Test Member No. in Family |
---|
Family | no. Member on 518kinase | GPCR |
---|
CK1 | 7 | 4 |
CK1 - CK1
Bioactivity |
---|
Kinase | GPCR |
---|
CK1a | inactive (18.38%) |
CK1g2 | inactive (2.65%) |
CK1g1 | inactive (3.97%) |
CK1g3 | inactive (7.47%) |
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 (2.24%) |
Other - Aur
Bioactivity |
---|
Kinase | GPCR |
---|
AurB | inactive (2.45%) |
AurC | inactive (-1.12%) |
AurA | inactive (0.17%) |
Other - NEK
Bioactivity |
---|
Kinase | GPCR |
---|
NEK1 | inactive (1.21%) |
NEK2 | inactive (1.4%) |
NEK9 | inactive (3.47%) |
NEK7 | inactive (4.4%) |
NEK6 | inactive (3.17%) |
Other - IKK
Bioactivity |
---|
Kinase | GPCR |
---|
TBK1 | inactive (1.95%) |
IKKe | inactive (-0.24%) |
IKKb | inactive (0.18%) |
IKKa | inactive (-0.06%) |
Other - TTK
Bioactivity |
---|
Kinase | GPCR |
---|
TTK | inactive (4.46%) |
AGC
AGC - GRK
Bioactivity |
---|
Kinase | GPCR |
---|
GPRK7 | inactive (-5.01%) |
GPRK6 | inactive (0.67%) |
AGC - PDK1
Bioactivity |
---|
Kinase | GPCR |
---|
PDK1 | inactive (-0.86%) |
AGC - RSK
Bioactivity |
---|
Kinase | GPCR |
---|
MSK1 | inactive (-8.03%) |
MSK2 | inactive (0.3%) |
RSK1 | inactive (-0.6%) |
RSK2 | inactive (-0.44%) |
RSK4 | inactive (0.04%) |
RSK3 | inactive (2.01%) |
p70S6K | inactive (1.78%) |
AGC - Akt
Bioactivity |
---|
Kinase | GPCR |
---|
AKT2 | inactive (0.86%) |
AKT1 | inactive (-0.24%) |
AKT3 | inactive (5.21%) |
AGC - SGK
Bioactivity |
---|
Kinase | GPCR |
---|
SGK1 | inactive (0.8%) |
SGK3 | inactive (-0.05%) |
SGK2 | inactive (1.38%) |
AGC - PKC
Bioactivity |
---|
Kinase | GPCR |
---|
PKCh | inactive (3.69%) |
PKCg | inactive (1.3%) |
PKCa | inactive (2.11%) |
PKCt | inactive (2.16%) |
PKCi | inactive (1.94%) |
AGC - PKG
Bioactivity |
---|
Kinase | GPCR |
---|
PKG2 | inactive (1.44%) |
PKG1 | inactive (0.89%) |
AGC - PKA
Bioactivity |
---|
Kinase | GPCR |
---|
PRKX | inactive (1.04%) |
AGC - DMPK
Bioactivity |
---|
Kinase | GPCR |
---|
ROCK1 | inactive (2.5%) |
ROCK2 | inactive (0.87%) |
MRCKb | inactive (1.34%) |
MRCKa | inactive (2.44%) |
CAMK
CAMK - RAD53
Bioactivity |
---|
Kinase | GPCR |
---|
CHK2 | inactive (-6.53%) |
CAMK - DCAMKL
Bioactivity |
---|
Kinase | GPCR |
---|
DCLK2 | inactive (0.56%) |
CAMK - CAMK1
Bioactivity |
---|
Kinase | GPCR |
---|
CaMK4 | inactive (0.11%) |
CaMK1d | inactive (0.97%) |
CAMK - PHK
Bioactivity |
---|
Kinase | GPCR |
---|
PHKg1 | inactive (4.85%) |
PHKg2 | inactive (-2.67%) |
CAMK - CAMK2
Bioactivity |
---|
Kinase | GPCR |
---|
CaMK2d | inactive (1.18%) |
CaMK2a | inactive (-1.84%) |
CAMK - MAPKAPK
Bioactivity |
---|
Kinase | GPCR |
---|
MAPKAPK5 | inactive (0.27%) |
MAPKAPK2 | inactive (-3.38%) |
MAPKAPK3 | inactive (29.99%) |
MNK2 | inactive (2.75%) |
MNK1 | inactive (2.51%) |
CAMK - PKD
Bioactivity |
---|
Kinase | GPCR |
---|
PKD3 | inactive (1.49%) |
PKD1 | inactive (1.79%) |
PKD2 | inactive (1.15%) |
CAMK - CAMKL
Bioactivity |
---|
Kinase | GPCR |
---|
MARK4 | inactive (1.32%) |
MARK3 | inactive (-0.77%) |
MARK1 | inactive (2.02%) |
QIK | inactive (-0.03%) |
SIK | inactive (7.66%) |
NuaK1 | inactive (-0.41%) |
BRSK1 | inactive (-0.05%) |
BRSK2 | inactive (1.96%) |
MELK | inactive (4.47%) |
CHK1 | inactive (-7.06%) |
PASK | inactive (0.41%) |
AMPKa1 | inactive (-0.04%) |
AMPKa2 | inactive (0.55%) |
CAMK - TSSK
Bioactivity |
---|
Kinase | GPCR |
---|
TSSK2 | inactive (0.7%) |
TSSK1 | inactive (0.67%) |
CAMK - DAPK
Bioactivity |
---|
Kinase | GPCR |
---|
DAPK1 | inactive (-10.38%) |
CAMK - PIM
Bioactivity |
---|
Kinase | GPCR |
---|
PIM2 | inactive (1.13%) |
PIM3 | inactive (1.65%) |
PIM1 | inactive (1.92%) |
CMGC
CMGC - MAPK
Bioactivity |
---|
Kinase | GPCR |
---|
JNK2 | inactive (6.17%) |
p38a | active (89.01%) |
p38b | inactive (42.5%) |
p38d | inactive (0.44%) |
Erk2 | inactive (3.48%) |
Erk1 | inactive (2.88%) |
CMGC - GSK
Bioactivity |
---|
Kinase | GPCR |
---|
GSK3A | inactive (2.27%) |
GSK3B | inactive (1.86%) |
CMGC - SRPK
Bioactivity |
---|
Kinase | GPCR |
---|
SRPK1 | inactive (-0.3%) |
MSSK1 | inactive (0.55%) |
CMGC - CLK
Bioactivity |
---|
Kinase | GPCR |
---|
CLK3 | inactive (0.05%) |
CLK2 | inactive (0.74%) |
CMGC - DYRK
Bioactivity |
---|
Kinase | GPCR |
---|
HIPK1 | inactive (-1.71%) |
HIPK4 | inactive (0.62%) |
DYRK1B | inactive (0.73%) |
DYRK1A | inactive (1.2%) |
DYRK2 | inactive (0.96%) |
CMGC - CK2
Bioactivity |
---|
Kinase | GPCR |
---|
CK2a1 | inactive (0.7%) |