Compound Information
Test on : GPCR
Compound Name : GSK466317A
Inchikey : OYNBTBJATZVIGH-UHFFFAOYSA-N
ChemSpider : 9925970
Pubchem CID : 11751266
ChEMBL : CHEMBL427058
|
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 | active (51.52%) |
TYK2 | inactive (-1.04%) |
JAK2 | inactive (29.24%) |
JAK3 | inactive (42.3%) |
TK - Fer
Bioactivity |
---|
Kinase | GPCR |
---|
FER | inactive (3.32%) |
FES | inactive (2.33%) |
TK - Abl
Bioactivity |
---|
Kinase | GPCR |
---|
ABL1 | inactive (1.72%) |
ABL2 | inactive (3.51%) |
TK - Csk
Bioactivity |
---|
Kinase | GPCR |
---|
CSK | inactive (2.47%) |
TK - Tec
Bioactivity |
---|
Kinase | GPCR |
---|
BMX | inactive (4.11%) |
BTK | inactive (0.33%) |
TXK | inactive (1.68%) |
TEC | inactive (6.05%) |
ITK | inactive (2.35%) |
TK - Src
Bioactivity |
---|
Kinase | GPCR |
---|
BRK | inactive (10.34%) |
SRM | inactive (3.11%) |
FRK | inactive (7.85%) |
BLK | inactive (33.18%) |
LCK | inactive (27.1%) |
HCK | inactive (6.23%) |
FGR | inactive (4.88%) |
FYN | inactive (4.45%) |
SRC | inactive (30.79%) |
YES | inactive (27.44%) |
TK - Eph
Bioactivity |
---|
Kinase | GPCR |
---|
EphA2 | inactive (-2.1%) |
EphA4 | inactive (6.71%) |
EphA3 | inactive (2.48%) |
EphB4 | inactive (0.29%) |
EphB3 | inactive (2.94%) |
EphB2 | inactive (6.01%) |
TK - FAK
Bioactivity |
---|
Kinase | GPCR |
---|
PYK2 | inactive (9.35%) |
TK - Syk
Bioactivity |
---|
Kinase | GPCR |
---|
SYK | inactive (1.05%) |
ZAP70 | inactive (3.9%) |
TK - ALK
Bioactivity |
---|
Kinase | GPCR |
---|
LTK | inactive (3.88%) |
ALK | inactive (2.26%) |
TK - Sev
Bioactivity |
---|
Kinase | GPCR |
---|
ROS | inactive (6.5%) |
TK - InsR
Bioactivity |
---|
Kinase | GPCR |
---|
INSR | inactive (6.02%) |
IGF1R | inactive (2.67%) |
IRR | inactive (1.79%) |
TK - DDR
Bioactivity |
---|
Kinase | GPCR |
---|
DDR2 | inactive (1.35%) |
TK - Musk
Bioactivity |
---|
Kinase | GPCR |
---|
MUSK | inactive (9.6%) |
TK - Trk
Bioactivity |
---|
Kinase | GPCR |
---|
TRKA | inactive (2.71%) |
TRKB | inactive (3.55%) |
TRKC | inactive (6.01%) |
TK - Met
Bioactivity |
---|
Kinase | GPCR |
---|
RON | inactive (11.36%) |
MET | inactive (4.94%) |
TK - Axl
Bioactivity |
---|
Kinase | GPCR |
---|
AXL | inactive (-2.18%) |
MER | inactive (0.92%) |
TYRO3 | inactive (5.41%) |
TK - Ret
Bioactivity |
---|
Kinase | GPCR |
---|
RET | inactive (15.23%) |
TK - FGFR
Bioactivity |
---|
Kinase | GPCR |
---|
FGFR1 | inactive (2.9%) |
FGFR2 | inactive (3.56%) |
FGFR3 | inactive (3.77%) |
FGFR4 | inactive (2.25%) |
TK - VEGFR
Bioactivity |
---|
Kinase | GPCR |
---|
FLT1 | inactive (-1.53%) |
KDR | inactive (6.91%) |
FLT4 | inactive (-1.34%) |
TK - PDGFR
Bioactivity |
---|
Kinase | GPCR |
---|
FMS | inactive (1.8%) |
KIT | inactive (0.36%) |
FLT3 | inactive (3.1%) |
PDGFRa | inactive (8.87%) |
PDGFRb | inactive (3.69%) |
TK - Tie
Bioactivity |
---|
Kinase | GPCR |
---|
TIE2 | inactive (5.04%) |
TK - Ack
Bioactivity |
---|
Kinase | GPCR |
---|
ACK | inactive (2.37%) |
TNK1 | inactive (3.87%) |
TK - EGFR
Bioactivity |
---|
Kinase | GPCR |
---|
EGFR | inactive (5.03%) |
ErbB2 | inactive (1.78%) |
ErbB4 | inactive (31.2%) |
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 (1.44%) |
TKL - RAF
Bioactivity |
---|
Kinase | GPCR |
---|
BRAF | inactive (35.71%) |
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 (3.92%) |
MST1 | inactive (5.19%) |
MST2 | inactive (4.7%) |
MST4 | inactive (8.39%) |
HGK | inactive (10.16%) |
MINK | inactive (9.18%) |
LOK | inactive (7.45%) |
PAK1 | inactive (4.55%) |
PAK3 | inactive (3.69%) |
PAK2 | inactive (2.32%) |
PAK5 | inactive (4.84%) |
PAK6 | inactive (-3.39%) |
STE - STE7
Bioactivity |
---|
Kinase | GPCR |
---|
MAP2K1 | inactive (35.54%) |
CK1
CK1
Test Member No. in Family |
---|
Family | no. Member on 518kinase | GPCR |
---|
CK1 | 7 | 4 |
CK1 - CK1
Bioactivity |
---|
Kinase | GPCR |
---|
CK1a | inactive (2.49%) |
CK1g2 | inactive (3.61%) |
CK1g1 | inactive (3.25%) |
CK1g3 | inactive (2.92%) |
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 (4.12%) |
Other - Aur
Bioactivity |
---|
Kinase | GPCR |
---|
AurB | inactive (10.01%) |
AurC | inactive (7.15%) |
AurA | inactive (16.61%) |
Other - NEK
Bioactivity |
---|
Kinase | GPCR |
---|
NEK1 | inactive (3.61%) |
NEK2 | inactive (4.83%) |
NEK9 | inactive (8.4%) |
NEK7 | inactive (3.32%) |
NEK6 | inactive (2.6%) |
Other - IKK
Bioactivity |
---|
Kinase | GPCR |
---|
TBK1 | inactive (3.48%) |
IKKe | inactive (5.11%) |
IKKb | inactive (5.73%) |
IKKa | inactive (4.34%) |
Other - TTK
Bioactivity |
---|
Kinase | GPCR |
---|
TTK | inactive (5.07%) |
AGC
AGC - GRK
Bioactivity |
---|
Kinase | GPCR |
---|
GPRK7 | inactive (16.39%) |
GPRK6 | inactive (13.38%) |
AGC - PDK1
Bioactivity |
---|
Kinase | GPCR |
---|
PDK1 | inactive (1.86%) |
AGC - RSK
Bioactivity |
---|
Kinase | GPCR |
---|
MSK1 | active (81.72%) |
MSK2 | active (68.94%) |
RSK1 | active (68.74%) |
RSK2 | active (65.47%) |
RSK4 | inactive (36.41%) |
RSK3 | active (53.37%) |
p70S6K | inactive (41.73%) |
AGC - Akt
Bioactivity |
---|
Kinase | GPCR |
---|
AKT2 | inactive (3.66%) |
AKT1 | inactive (5.71%) |
AKT3 | inactive (22.07%) |
AGC - SGK
Bioactivity |
---|
Kinase | GPCR |
---|
SGK1 | inactive (17.89%) |
SGK3 | inactive (34.43%) |
SGK2 | inactive (12.49%) |
AGC - PKC
Bioactivity |
---|
Kinase | GPCR |
---|
PKCh | inactive (39.09%) |
PKCg | inactive (3.46%) |
PKCa | inactive (1.52%) |
PKCt | inactive (28.33%) |
PKCi | inactive (1.11%) |
AGC - PKG
Bioactivity |
---|
Kinase | GPCR |
---|
PKG2 | active (59.72%) |
PKG1 | active (67.91%) |
AGC - PKA
Bioactivity |
---|
Kinase | GPCR |
---|
PRKX | active (79.71%) |
AGC - DMPK
Bioactivity |
---|
Kinase | GPCR |
---|
ROCK1 | active (83.98%) |
ROCK2 | active (85.84%) |
MRCKb | active (65.51%) |
MRCKa | active (64.57%) |
CAMK
CAMK - RAD53
Bioactivity |
---|
Kinase | GPCR |
---|
CHK2 | inactive (7.48%) |
CAMK - DCAMKL
Bioactivity |
---|
Kinase | GPCR |
---|
DCLK2 | inactive (2.36%) |
CAMK - CAMK1
Bioactivity |
---|
Kinase | GPCR |
---|
CaMK4 | inactive (0.15%) |
CaMK1d | inactive (1.73%) |
CAMK - PHK
Bioactivity |
---|
Kinase | GPCR |
---|
PHKg1 | inactive (6.61%) |
PHKg2 | inactive (4.01%) |
CAMK - CAMK2
Bioactivity |
---|
Kinase | GPCR |
---|
CaMK2d | inactive (4.42%) |
CaMK2a | inactive (1.21%) |
CAMK - MAPKAPK
Bioactivity |
---|
Kinase | GPCR |
---|
MAPKAPK5 | inactive (2.73%) |
MAPKAPK2 | inactive (4.3%) |
MAPKAPK3 | inactive (9.12%) |
MNK2 | inactive (5.02%) |
MNK1 | inactive (7.79%) |
CAMK - PKD
Bioactivity |
---|
Kinase | GPCR |
---|
PKD3 | inactive (7.2%) |
PKD1 | inactive (6.51%) |
PKD2 | inactive (7.46%) |
CAMK - CAMKL
Bioactivity |
---|
Kinase | GPCR |
---|
MARK4 | inactive (3.1%) |
MARK3 | inactive (9.91%) |
MARK1 | inactive (6.87%) |
QIK | inactive (11.76%) |
SIK | inactive (8.58%) |
NuaK1 | inactive (5.4%) |
BRSK1 | inactive (3.03%) |
BRSK2 | inactive (8.61%) |
MELK | inactive (7.81%) |
CHK1 | inactive (11.36%) |
PASK | inactive (0.16%) |
AMPKa1 | active (62.18%) |
AMPKa2 | inactive (16.28%) |
CAMK - TSSK
Bioactivity |
---|
Kinase | GPCR |
---|
TSSK2 | inactive (1.37%) |
TSSK1 | inactive (3.9%) |
CAMK - DAPK
Bioactivity |
---|
Kinase | GPCR |
---|
DAPK1 | inactive (10.04%) |
CAMK - PIM
Bioactivity |
---|
Kinase | GPCR |
---|
PIM2 | inactive (-0.24%) |
PIM3 | inactive (-0.25%) |
PIM1 | inactive (0.15%) |
CMGC
CMGC - MAPK
Bioactivity |
---|
Kinase | GPCR |
---|
JNK2 | inactive (2.16%) |
p38a | inactive (6.81%) |
p38b | inactive (2.31%) |
p38d | inactive (4.12%) |
Erk2 | inactive (35.4%) |
Erk1 | inactive (21.83%) |
CMGC - GSK
Bioactivity |
---|
Kinase | GPCR |
---|
GSK3A | inactive (-1.53%) |
GSK3B | inactive (2.19%) |
CMGC - SRPK
Bioactivity |
---|
Kinase | GPCR |
---|
SRPK1 | inactive (-1.39%) |
MSSK1 | inactive (-2.71%) |
CMGC - CLK
Bioactivity |
---|
Kinase | GPCR |
---|
CLK3 | inactive (1.64%) |
CLK2 | inactive (4.84%) |
CMGC - DYRK
Bioactivity |
---|
Kinase | GPCR |
---|
HIPK1 | inactive (-0.78%) |
HIPK4 | inactive (2.16%) |
DYRK1B | inactive (-0.06%) |
DYRK1A | inactive (2.44%) |
DYRK2 | inactive (2.68%) |
CMGC - CK2
Bioactivity |
---|
Kinase | GPCR |
---|
CK2a1 | inactive (1.13%) |