Compound Information
Test on : GPCR
Compound Name : GSK2186269A
Inchikey : MUCIWJFQZDAZJT-UHFFFAOYSA-N
ChemSpider : 24690585
Pubchem CID : 44581222
ChEMBL : CHEMBL458415
|
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 (-3.36%) |
TYK2 | inactive (-2.82%) |
JAK2 | inactive (0.18%) |
JAK3 | inactive (0.18%) |
TK - Fer
Bioactivity |
---|
Kinase | GPCR |
---|
FER | active (85.23%) |
FES | active (62.33%) |
TK - Abl
Bioactivity |
---|
Kinase | GPCR |
---|
ABL1 | inactive (7.27%) |
ABL2 | inactive (5.11%) |
TK - Csk
Bioactivity |
---|
Kinase | GPCR |
---|
CSK | inactive (0.41%) |
TK - Tec
Bioactivity |
---|
Kinase | GPCR |
---|
BMX | inactive (4.16%) |
BTK | inactive (2.65%) |
TXK | inactive (7.54%) |
TEC | inactive (7.6%) |
ITK | inactive (1.52%) |
TK - Src
Bioactivity |
---|
Kinase | GPCR |
---|
BRK | inactive (0.03%) |
SRM | inactive (-1.29%) |
FRK | inactive (0.69%) |
BLK | inactive (4.28%) |
LCK | inactive (6%) |
HCK | inactive (10.02%) |
FGR | inactive (3.44%) |
FYN | inactive (1.51%) |
SRC | inactive (8.12%) |
YES | inactive (-1.83%) |
TK - Eph
Bioactivity |
---|
Kinase | GPCR |
---|
EphA2 | inactive (2.11%) |
EphA4 | inactive (6.36%) |
EphA3 | inactive (0.93%) |
EphB4 | inactive (0.73%) |
EphB3 | inactive (0.49%) |
EphB2 | inactive (9.31%) |
TK - FAK
Bioactivity |
---|
Kinase | GPCR |
---|
PYK2 | active (89.96%) |
TK - Syk
Bioactivity |
---|
Kinase | GPCR |
---|
SYK | inactive (-0.01%) |
ZAP70 | - |
TK - ALK
Bioactivity |
---|
Kinase | GPCR |
---|
LTK | active (89.91%) |
ALK | active (85.32%) |
TK - Sev
Bioactivity |
---|
Kinase | GPCR |
---|
ROS | active (79.19%) |
TK - InsR
Bioactivity |
---|
Kinase | GPCR |
---|
INSR | active (91.02%) |
IGF1R | active (98.39%) |
IRR | active (90.28%) |
TK - DDR
Bioactivity |
---|
Kinase | GPCR |
---|
DDR2 | inactive (0.74%) |
TK - Musk
Bioactivity |
---|
Kinase | GPCR |
---|
MUSK | inactive (4.18%) |
TK - Trk
Bioactivity |
---|
Kinase | GPCR |
---|
TRKA | inactive (3.52%) |
TRKB | inactive (2.75%) |
TRKC | inactive (5.17%) |
TK - Met
Bioactivity |
---|
Kinase | GPCR |
---|
RON | inactive (4.66%) |
MET | inactive (-6.58%) |
TK - Axl
Bioactivity |
---|
Kinase | GPCR |
---|
AXL | inactive (21.37%) |
MER | inactive (0.11%) |
TYRO3 | inactive (1.54%) |
TK - Ret
Bioactivity |
---|
Kinase | GPCR |
---|
RET | inactive (9.16%) |
TK - FGFR
Bioactivity |
---|
Kinase | GPCR |
---|
FGFR1 | inactive (-1.36%) |
FGFR2 | inactive (6.55%) |
FGFR3 | inactive (0.84%) |
FGFR4 | inactive (0.78%) |
TK - VEGFR
Bioactivity |
---|
Kinase | GPCR |
---|
FLT1 | inactive (2.02%) |
KDR | inactive (0.21%) |
FLT4 | inactive (13.67%) |
TK - PDGFR
Bioactivity |
---|
Kinase | GPCR |
---|
FMS | inactive (2.14%) |
KIT | inactive (5.18%) |
FLT3 | inactive (-1.35%) |
PDGFRa | inactive (3.64%) |
PDGFRb | inactive (3.27%) |
TK - Tie
Bioactivity |
---|
Kinase | GPCR |
---|
TIE2 | inactive (1.37%) |
TK - Ack
Bioactivity |
---|
Kinase | GPCR |
---|
ACK | inactive (1.93%) |
TNK1 | inactive (12.04%) |
TK - EGFR
Bioactivity |
---|
Kinase | GPCR |
---|
EGFR | inactive (1.28%) |
ErbB2 | inactive (-0.36%) |
ErbB4 | inactive (6.14%) |
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 (0.98%) |
TKL - RAF
Bioactivity |
---|
Kinase | GPCR |
---|
BRAF | inactive (2.22%) |
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 (3.15%) |
MST1 | inactive (6.86%) |
MST2 | inactive (5.22%) |
MST4 | inactive (4.16%) |
HGK | inactive (2.27%) |
MINK | inactive (-0.01%) |
LOK | inactive (1.24%) |
PAK1 | inactive (4.36%) |
PAK3 | inactive (2.24%) |
PAK2 | inactive (1.19%) |
PAK5 | inactive (-1.41%) |
PAK6 | inactive (-0.54%) |
STE - STE7
Bioactivity |
---|
Kinase | GPCR |
---|
MAP2K1 | inactive (2.14%) |
CK1
CK1
Test Member No. in Family |
---|
Family | no. Member on 518kinase | GPCR |
---|
CK1 | 7 | 4 |
CK1 - CK1
Bioactivity |
---|
Kinase | GPCR |
---|
CK1a | inactive (2.45%) |
CK1g2 | inactive (2.57%) |
CK1g1 | inactive (3.55%) |
CK1g3 | inactive (4.52%) |
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 (25.39%) |
Other - Aur
Bioactivity |
---|
Kinase | GPCR |
---|
AurB | inactive (3.08%) |
AurC | inactive (8.2%) |
AurA | inactive (2.61%) |
Other - NEK
Bioactivity |
---|
Kinase | GPCR |
---|
NEK1 | inactive (1%) |
NEK2 | inactive (3.53%) |
NEK9 | inactive (0.78%) |
NEK7 | inactive (3.29%) |
NEK6 | inactive (-0.68%) |
Other - IKK
Bioactivity |
---|
Kinase | GPCR |
---|
TBK1 | inactive (5.19%) |
IKKe | inactive (-0.46%) |
IKKb | inactive (-1.42%) |
IKKa | inactive (0.37%) |
Other - TTK
Bioactivity |
---|
Kinase | GPCR |
---|
TTK | inactive (25.12%) |
AGC
AGC - GRK
Bioactivity |
---|
Kinase | GPCR |
---|
GPRK7 | inactive (-6.08%) |
GPRK6 | inactive (-3.01%) |
AGC - PDK1
Bioactivity |
---|
Kinase | GPCR |
---|
PDK1 | inactive (0.29%) |
AGC - RSK
Bioactivity |
---|
Kinase | GPCR |
---|
MSK1 | inactive (4.71%) |
MSK2 | inactive (1.75%) |
RSK1 | inactive (0.41%) |
RSK2 | inactive (-1.32%) |
RSK4 | inactive (0.95%) |
RSK3 | inactive (0.48%) |
p70S6K | inactive (0.46%) |
AGC - Akt
Bioactivity |
---|
Kinase | GPCR |
---|
AKT2 | inactive (1.42%) |
AKT1 | inactive (1.39%) |
AKT3 | inactive (1.23%) |
AGC - SGK
Bioactivity |
---|
Kinase | GPCR |
---|
SGK1 | inactive (1.07%) |
SGK3 | inactive (-0.59%) |
SGK2 | inactive (2.34%) |
AGC - PKC
Bioactivity |
---|
Kinase | GPCR |
---|
PKCh | inactive (-0.3%) |
PKCg | inactive (5.19%) |
PKCa | inactive (1.9%) |
PKCt | inactive (-0.74%) |
PKCi | inactive (3.35%) |
AGC - PKG
Bioactivity |
---|
Kinase | GPCR |
---|
PKG2 | inactive (2.75%) |
PKG1 | inactive (2.75%) |
AGC - PKA
Bioactivity |
---|
Kinase | GPCR |
---|
PRKX | inactive (-1.42%) |
AGC - DMPK
Bioactivity |
---|
Kinase | GPCR |
---|
ROCK1 | inactive (1.14%) |
ROCK2 | inactive (-1.46%) |
MRCKb | inactive (1.27%) |
MRCKa | inactive (-1.14%) |
CAMK
CAMK - RAD53
Bioactivity |
---|
Kinase | GPCR |
---|
CHK2 | inactive (7.08%) |
CAMK - DCAMKL
Bioactivity |
---|
Kinase | GPCR |
---|
DCLK2 | inactive (-1.1%) |
CAMK - CAMK1
Bioactivity |
---|
Kinase | GPCR |
---|
CaMK4 | inactive (3.69%) |
CaMK1d | inactive (2.58%) |
CAMK - PHK
Bioactivity |
---|
Kinase | GPCR |
---|
PHKg1 | inactive (3.14%) |
PHKg2 | inactive (0.08%) |
CAMK - CAMK2
Bioactivity |
---|
Kinase | GPCR |
---|
CaMK2d | inactive (2.99%) |
CaMK2a | inactive (4.08%) |
CAMK - MAPKAPK
Bioactivity |
---|
Kinase | GPCR |
---|
MAPKAPK5 | inactive (-1.65%) |
MAPKAPK2 | inactive (1.57%) |
MAPKAPK3 | inactive (0.18%) |
MNK2 | inactive (7.67%) |
MNK1 | inactive (5.08%) |
CAMK - PKD
Bioactivity |
---|
Kinase | GPCR |
---|
PKD3 | inactive (4.37%) |
PKD1 | inactive (3.76%) |
PKD2 | inactive (3.6%) |
CAMK - CAMKL
Bioactivity |
---|
Kinase | GPCR |
---|
MARK4 | inactive (1.93%) |
MARK3 | inactive (6.25%) |
MARK1 | inactive (3.15%) |
QIK | inactive (-3.15%) |
SIK | inactive (7.48%) |
NuaK1 | inactive (-4.13%) |
BRSK1 | inactive (0.61%) |
BRSK2 | inactive (1.3%) |
MELK | inactive (2.27%) |
CHK1 | inactive (3.74%) |
PASK | inactive (-0.16%) |
AMPKa1 | inactive (0.36%) |
AMPKa2 | inactive (3.8%) |
CAMK - TSSK
Bioactivity |
---|
Kinase | GPCR |
---|
TSSK2 | inactive (13.64%) |
TSSK1 | inactive (19.17%) |
CAMK - DAPK
Bioactivity |
---|
Kinase | GPCR |
---|
DAPK1 | inactive (5.32%) |
CAMK - PIM
Bioactivity |
---|
Kinase | GPCR |
---|
PIM2 | inactive (0.38%) |
PIM3 | inactive (-1.08%) |
PIM1 | inactive (-0.15%) |
CMGC
CMGC - MAPK
Bioactivity |
---|
Kinase | GPCR |
---|
JNK2 | inactive (1.82%) |
p38a | inactive (3.7%) |
p38b | inactive (1.85%) |
p38d | inactive (2.2%) |
Erk2 | inactive (2.12%) |
Erk1 | inactive (1.51%) |
CMGC - GSK
Bioactivity |
---|
Kinase | GPCR |
---|
GSK3A | inactive (1.16%) |
GSK3B | inactive (0.72%) |
CMGC - SRPK
Bioactivity |
---|
Kinase | GPCR |
---|
SRPK1 | inactive (-3.76%) |
MSSK1 | inactive (1.46%) |
CMGC - CLK
Bioactivity |
---|
Kinase | GPCR |
---|
CLK3 | inactive (2.24%) |
CLK2 | inactive (44.39%) |
CMGC - DYRK
Bioactivity |
---|
Kinase | GPCR |
---|
HIPK1 | inactive (2.7%) |
HIPK4 | inactive (2.99%) |
DYRK1B | inactive (2.3%) |
DYRK1A | inactive (3.98%) |
DYRK2 | inactive (2.02%) |
CMGC - CK2
Bioactivity |
---|
Kinase | GPCR |
---|
CK2a1 | inactive (-9.3%) |