Compound Information
Test on : GPCR
Compound Name : GSK1173862A
Inchikey : LZOWLPPKVLNYEG-UHFFFAOYSA-N
ChemSpider : 24696892
Pubchem CID : 25218600
ChEMBL : CHEMBL477069
|
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 (-0.81%) |
TYK2 | inactive (-3.62%) |
JAK2 | inactive (2.51%) |
JAK3 | inactive (-3.27%) |
TK - Fer
Bioactivity |
---|
Kinase | GPCR |
---|
FER | active (84.4%) |
FES | active (81.27%) |
TK - Abl
Bioactivity |
---|
Kinase | GPCR |
---|
ABL1 | inactive (9.3%) |
ABL2 | inactive (3.99%) |
TK - Csk
Bioactivity |
---|
Kinase | GPCR |
---|
CSK | inactive (4.58%) |
TK - Tec
Bioactivity |
---|
Kinase | GPCR |
---|
BMX | inactive (5.71%) |
BTK | inactive (-1.31%) |
TXK | inactive (6.47%) |
TEC | inactive (9.82%) |
ITK | inactive (6%) |
TK - Src
Bioactivity |
---|
Kinase | GPCR |
---|
BRK | active (67.76%) |
SRM | inactive (22.11%) |
FRK | inactive (20.54%) |
BLK | inactive (6.81%) |
LCK | inactive (6.22%) |
HCK | inactive (11.88%) |
FGR | inactive (7.28%) |
FYN | inactive (16.13%) |
SRC | inactive (14.55%) |
YES | inactive (9.04%) |
TK - Eph
Bioactivity |
---|
Kinase | GPCR |
---|
EphA2 | inactive (-1.1%) |
EphA4 | inactive (4.53%) |
EphA3 | inactive (4.27%) |
EphB4 | inactive (4.67%) |
EphB3 | inactive (-1.82%) |
EphB2 | inactive (15.82%) |
TK - FAK
Bioactivity |
---|
Kinase | GPCR |
---|
PYK2 | active (97.69%) |
TK - Syk
Bioactivity |
---|
Kinase | GPCR |
---|
SYK | active (75.8%) |
ZAP70 | inactive (28.67%) |
TK - ALK
Bioactivity |
---|
Kinase | GPCR |
---|
LTK | active (95.51%) |
ALK | active (86.26%) |
TK - Sev
Bioactivity |
---|
Kinase | GPCR |
---|
ROS | active (81.24%) |
TK - InsR
Bioactivity |
---|
Kinase | GPCR |
---|
INSR | active (96.2%) |
IGF1R | active (94.8%) |
IRR | active (97.04%) |
TK - DDR
Bioactivity |
---|
Kinase | GPCR |
---|
DDR2 | inactive (4.82%) |
TK - Musk
Bioactivity |
---|
Kinase | GPCR |
---|
MUSK | inactive (12.22%) |
TK - Trk
Bioactivity |
---|
Kinase | GPCR |
---|
TRKA | inactive (5.65%) |
TRKB | inactive (6.11%) |
TRKC | inactive (5.51%) |
TK - Met
Bioactivity |
---|
Kinase | GPCR |
---|
RON | inactive (13.12%) |
MET | inactive (20.57%) |
TK - Axl
Bioactivity |
---|
Kinase | GPCR |
---|
AXL | active (57.43%) |
MER | inactive (14.14%) |
TYRO3 | inactive (7.19%) |
TK - Ret
Bioactivity |
---|
Kinase | GPCR |
---|
RET | inactive (20.86%) |
TK - FGFR
Bioactivity |
---|
Kinase | GPCR |
---|
FGFR1 | inactive (3.44%) |
FGFR2 | inactive (5.74%) |
FGFR3 | inactive (4.56%) |
FGFR4 | inactive (12.23%) |
TK - VEGFR
Bioactivity |
---|
Kinase | GPCR |
---|
FLT1 | inactive (0.66%) |
KDR | inactive (16.55%) |
FLT4 | inactive (4.1%) |
TK - PDGFR
Bioactivity |
---|
Kinase | GPCR |
---|
FMS | active (78.58%) |
KIT | inactive (13.1%) |
FLT3 | inactive (13.14%) |
PDGFRa | inactive (38.29%) |
PDGFRb | inactive (32.21%) |
TK - Tie
Bioactivity |
---|
Kinase | GPCR |
---|
TIE2 | inactive (4.28%) |
TK - Ack
Bioactivity |
---|
Kinase | GPCR |
---|
ACK | inactive (41.13%) |
TNK1 | active (81.05%) |
TK - EGFR
Bioactivity |
---|
Kinase | GPCR |
---|
EGFR | inactive (38.05%) |
ErbB2 | inactive (3.37%) |
ErbB4 | active (75.04%) |
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 (3.34%) |
TKL - RAF
Bioactivity |
---|
Kinase | GPCR |
---|
BRAF | inactive (40.11%) |
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 (48.92%) |
MST1 | inactive (41.02%) |
MST2 | inactive (10.57%) |
MST4 | inactive (-1.5%) |
HGK | active (80.79%) |
MINK | active (71.68%) |
LOK | inactive (24.81%) |
PAK1 | inactive (9.12%) |
PAK3 | inactive (5.56%) |
PAK2 | inactive (3.33%) |
PAK5 | inactive (6.67%) |
PAK6 | inactive (-5.69%) |
STE - STE7
Bioactivity |
---|
Kinase | GPCR |
---|
MAP2K1 | inactive (33.41%) |
CK1
CK1
Test Member No. in Family |
---|
Family | no. Member on 518kinase | GPCR |
---|
CK1 | 7 | 4 |
CK1 - CK1
Bioactivity |
---|
Kinase | GPCR |
---|
CK1a | active (78.48%) |
CK1g2 | active (78.63%) |
CK1g1 | active (77.98%) |
CK1g3 | active (83.49%) |
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 (48.15%) |
Other - Aur
Bioactivity |
---|
Kinase | GPCR |
---|
AurB | inactive (3.45%) |
AurC | inactive (5.81%) |
AurA | inactive (7.44%) |
Other - NEK
Bioactivity |
---|
Kinase | GPCR |
---|
NEK1 | inactive (21.64%) |
NEK2 | inactive (11.1%) |
NEK9 | inactive (12.78%) |
NEK7 | inactive (7.03%) |
NEK6 | inactive (3.03%) |
Other - IKK
Bioactivity |
---|
Kinase | GPCR |
---|
TBK1 | inactive (11.5%) |
IKKe | inactive (8.28%) |
IKKb | inactive (4.25%) |
IKKa | inactive (4.21%) |
Other - TTK
Bioactivity |
---|
Kinase | GPCR |
---|
TTK | active (79.59%) |
AGC
AGC - GRK
Bioactivity |
---|
Kinase | GPCR |
---|
GPRK7 | inactive (16.65%) |
GPRK6 | inactive (25.3%) |
AGC - PDK1
Bioactivity |
---|
Kinase | GPCR |
---|
PDK1 | inactive (2.33%) |
AGC - RSK
Bioactivity |
---|
Kinase | GPCR |
---|
MSK1 | inactive (5.31%) |
MSK2 | inactive (7.01%) |
RSK1 | active (72.45%) |
RSK2 | inactive (40.16%) |
RSK4 | active (54.1%) |
RSK3 | inactive (37.97%) |
p70S6K | inactive (4.24%) |
AGC - Akt
Bioactivity |
---|
Kinase | GPCR |
---|
AKT2 | inactive (1.92%) |
AKT1 | inactive (0.27%) |
AKT3 | inactive (2.18%) |
AGC - SGK
Bioactivity |
---|
Kinase | GPCR |
---|
SGK1 | inactive (4.78%) |
SGK3 | inactive (0.16%) |
SGK2 | inactive (6.37%) |
AGC - PKC
Bioactivity |
---|
Kinase | GPCR |
---|
PKCh | inactive (1.44%) |
PKCg | inactive (21.98%) |
PKCa | inactive (15.88%) |
PKCt | inactive (4.89%) |
PKCi | inactive (2.93%) |
AGC - PKG
Bioactivity |
---|
Kinase | GPCR |
---|
PKG2 | inactive (26.31%) |
PKG1 | inactive (32.93%) |
AGC - PKA
Bioactivity |
---|
Kinase | GPCR |
---|
PRKX | inactive (0.52%) |
AGC - DMPK
Bioactivity |
---|
Kinase | GPCR |
---|
ROCK1 | active (67.65%) |
ROCK2 | active (71.27%) |
MRCKb | inactive (13.01%) |
MRCKa | inactive (17.9%) |
CAMK
CAMK - RAD53
Bioactivity |
---|
Kinase | GPCR |
---|
CHK2 | active (79.08%) |
CAMK - DCAMKL
Bioactivity |
---|
Kinase | GPCR |
---|
DCLK2 | inactive (7.08%) |
CAMK - CAMK1
Bioactivity |
---|
Kinase | GPCR |
---|
CaMK4 | inactive (36.1%) |
CaMK1d | active (61.13%) |
CAMK - PHK
Bioactivity |
---|
Kinase | GPCR |
---|
PHKg1 | active (77.79%) |
PHKg2 | active (67.56%) |
CAMK - CAMK2
Bioactivity |
---|
Kinase | GPCR |
---|
CaMK2d | active (72.84%) |
CaMK2a | inactive (44.93%) |
CAMK - MAPKAPK
Bioactivity |
---|
Kinase | GPCR |
---|
MAPKAPK5 | inactive (33.18%) |
MAPKAPK2 | inactive (3.54%) |
MAPKAPK3 | inactive (17.33%) |
MNK2 | inactive (2.51%) |
MNK1 | inactive (5.92%) |
CAMK - PKD
Bioactivity |
---|
Kinase | GPCR |
---|
PKD3 | active (72.7%) |
PKD1 | active (79.51%) |
PKD2 | active (81.13%) |
CAMK - CAMKL
Bioactivity |
---|
Kinase | GPCR |
---|
MARK4 | inactive (40.74%) |
MARK3 | active (68.34%) |
MARK1 | active (52.91%) |
QIK | inactive (11.04%) |
SIK | inactive (10.17%) |
NuaK1 | active (59.68%) |
BRSK1 | inactive (1.82%) |
BRSK2 | inactive (2.9%) |
MELK | active (75.16%) |
CHK1 | inactive (8.07%) |
PASK | inactive (8.59%) |
AMPKa1 | inactive (20.29%) |
AMPKa2 | inactive (10.66%) |
CAMK - TSSK
Bioactivity |
---|
Kinase | GPCR |
---|
TSSK2 | active (86.04%) |
TSSK1 | active (92.59%) |
CAMK - DAPK
Bioactivity |
---|
Kinase | GPCR |
---|
DAPK1 | inactive (47.15%) |
CAMK - PIM
Bioactivity |
---|
Kinase | GPCR |
---|
PIM2 | inactive (7.35%) |
PIM3 | inactive (40.83%) |
PIM1 | active (50.76%) |
CMGC
CMGC - MAPK
Bioactivity |
---|
Kinase | GPCR |
---|
JNK2 | active (91.29%) |
p38a | inactive (17.15%) |
p38b | inactive (14.48%) |
p38d | inactive (7.07%) |
Erk2 | inactive (36.54%) |
Erk1 | inactive (9.65%) |
CMGC - GSK
Bioactivity |
---|
Kinase | GPCR |
---|
GSK3A | inactive (2.99%) |
GSK3B | inactive (4.25%) |
CMGC - SRPK
Bioactivity |
---|
Kinase | GPCR |
---|
SRPK1 | inactive (7.5%) |
MSSK1 | inactive (28.24%) |
CMGC - CLK
Bioactivity |
---|
Kinase | GPCR |
---|
CLK3 | inactive (22.31%) |
CLK2 | active (93.79%) |
CMGC - DYRK
Bioactivity |
---|
Kinase | GPCR |
---|
HIPK1 | active (79.48%) |
HIPK4 | active (84.29%) |
DYRK1B | active (82.44%) |
DYRK1A | active (82.65%) |
DYRK2 | active (82.33%) |
CMGC - CK2
Bioactivity |
---|
Kinase | GPCR |
---|
CK2a1 | active (66.18%) |