Compound Information
Test on : GPCR
Compound Name : GSK1220512A
Inchikey : IBROMPXLFSIBRF-UHFFFAOYSA-N
ChemSpider : 24690938
Pubchem CID : 25218614
ChEMBL : CHEMBL458865
|
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 (2.03%) |
TYK2 | inactive (-2.61%) |
JAK2 | inactive (2.59%) |
JAK3 | inactive (11.55%) |
TK - Fer
Bioactivity |
---|
Kinase | GPCR |
---|
FER | active (82.85%) |
FES | active (81.72%) |
TK - Abl
Bioactivity |
---|
Kinase | GPCR |
---|
ABL1 | inactive (3.4%) |
ABL2 | inactive (2.78%) |
TK - Csk
Bioactivity |
---|
Kinase | GPCR |
---|
CSK | inactive (0.44%) |
TK - Tec
Bioactivity |
---|
Kinase | GPCR |
---|
BMX | inactive (5.02%) |
BTK | inactive (-0.07%) |
TXK | inactive (5.7%) |
TEC | inactive (3.59%) |
ITK | inactive (5.47%) |
TK - Src
Bioactivity |
---|
Kinase | GPCR |
---|
BRK | inactive (31.17%) |
SRM | inactive (7.98%) |
FRK | inactive (12.66%) |
BLK | inactive (3.73%) |
LCK | inactive (4.79%) |
HCK | inactive (7.94%) |
FGR | inactive (5.03%) |
FYN | inactive (9.69%) |
SRC | inactive (10.45%) |
YES | inactive (7.33%) |
TK - Eph
Bioactivity |
---|
Kinase | GPCR |
---|
EphA2 | inactive (-0.92%) |
EphA4 | inactive (6.43%) |
EphA3 | inactive (1.28%) |
EphB4 | inactive (1.31%) |
EphB3 | inactive (2.03%) |
EphB2 | inactive (1.15%) |
TK - FAK
Bioactivity |
---|
Kinase | GPCR |
---|
PYK2 | active (97.76%) |
TK - Syk
Bioactivity |
---|
Kinase | GPCR |
---|
SYK | inactive (35.91%) |
ZAP70 | inactive (23.46%) |
TK - ALK
Bioactivity |
---|
Kinase | GPCR |
---|
LTK | active (96.04%) |
ALK | active (88.84%) |
TK - Sev
Bioactivity |
---|
Kinase | GPCR |
---|
ROS | active (81.8%) |
TK - InsR
Bioactivity |
---|
Kinase | GPCR |
---|
INSR | active (101.84%) |
IGF1R | active (101.28%) |
IRR | active (96.66%) |
TK - DDR
Bioactivity |
---|
Kinase | GPCR |
---|
DDR2 | inactive (0.35%) |
TK - Musk
Bioactivity |
---|
Kinase | GPCR |
---|
MUSK | inactive (13.17%) |
TK - Trk
Bioactivity |
---|
Kinase | GPCR |
---|
TRKA | inactive (4.26%) |
TRKB | inactive (3.09%) |
TRKC | inactive (-0.43%) |
TK - Met
Bioactivity |
---|
Kinase | GPCR |
---|
RON | inactive (-0.44%) |
MET | inactive (0.66%) |
TK - Axl
Bioactivity |
---|
Kinase | GPCR |
---|
AXL | inactive (42.43%) |
MER | inactive (8.43%) |
TYRO3 | inactive (2.95%) |
TK - Ret
Bioactivity |
---|
Kinase | GPCR |
---|
RET | inactive (9.44%) |
TK - FGFR
Bioactivity |
---|
Kinase | GPCR |
---|
FGFR1 | inactive (2.33%) |
FGFR2 | inactive (3.84%) |
FGFR3 | inactive (3.24%) |
FGFR4 | inactive (7.42%) |
TK - VEGFR
Bioactivity |
---|
Kinase | GPCR |
---|
FLT1 | inactive (0.61%) |
KDR | inactive (15.33%) |
FLT4 | inactive (2.68%) |
TK - PDGFR
Bioactivity |
---|
Kinase | GPCR |
---|
FMS | inactive (48.14%) |
KIT | inactive (4.94%) |
FLT3 | inactive (8.56%) |
PDGFRa | inactive (31.11%) |
PDGFRb | inactive (26.93%) |
TK - Tie
Bioactivity |
---|
Kinase | GPCR |
---|
TIE2 | inactive (3.7%) |
TK - Ack
Bioactivity |
---|
Kinase | GPCR |
---|
ACK | active (61.66%) |
TNK1 | active (74.13%) |
TK - EGFR
Bioactivity |
---|
Kinase | GPCR |
---|
EGFR | - |
ErbB2 | inactive (3.8%) |
ErbB4 | active (76.85%) |
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 (1.94%) |
TKL - RAF
Bioactivity |
---|
Kinase | GPCR |
---|
BRAF | inactive (16.05%) |
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 (31.09%) |
MST1 | inactive (25.22%) |
MST2 | inactive (10.27%) |
MST4 | inactive (2.73%) |
HGK | active (68.1%) |
MINK | active (55.02%) |
LOK | inactive (11.84%) |
PAK1 | inactive (7.46%) |
PAK3 | inactive (6.18%) |
PAK2 | inactive (2.24%) |
PAK5 | inactive (27.44%) |
PAK6 | inactive (3.58%) |
STE - STE7
Bioactivity |
---|
Kinase | GPCR |
---|
MAP2K1 | inactive (15.61%) |
CK1
CK1
Test Member No. in Family |
---|
Family | no. Member on 518kinase | GPCR |
---|
CK1 | 7 | 4 |
CK1 - CK1
Bioactivity |
---|
Kinase | GPCR |
---|
CK1a | active (58.31%) |
CK1g2 | inactive (40.84%) |
CK1g1 | inactive (42.19%) |
CK1g3 | active (58.95%) |
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 | active (64.83%) |
Other - Aur
Bioactivity |
---|
Kinase | GPCR |
---|
AurB | inactive (2.23%) |
AurC | inactive (2.67%) |
AurA | inactive (4.58%) |
Other - NEK
Bioactivity |
---|
Kinase | GPCR |
---|
NEK1 | inactive (11.15%) |
NEK2 | inactive (2.89%) |
NEK9 | inactive (13.47%) |
NEK7 | inactive (7.1%) |
NEK6 | inactive (5.57%) |
Other - IKK
Bioactivity |
---|
Kinase | GPCR |
---|
TBK1 | inactive (6.76%) |
IKKe | inactive (4.36%) |
IKKb | inactive (3.32%) |
IKKa | inactive (-0.19%) |
Other - TTK
Bioactivity |
---|
Kinase | GPCR |
---|
TTK | active (85.6%) |
AGC
AGC - GRK
Bioactivity |
---|
Kinase | GPCR |
---|
GPRK7 | inactive (10.05%) |
GPRK6 | inactive (14.35%) |
AGC - PDK1
Bioactivity |
---|
Kinase | GPCR |
---|
PDK1 | inactive (2.49%) |
AGC - RSK
Bioactivity |
---|
Kinase | GPCR |
---|
MSK1 | inactive (6.61%) |
MSK2 | inactive (7.26%) |
RSK1 | active (65.34%) |
RSK2 | active (56.98%) |
RSK4 | active (54.82%) |
RSK3 | inactive (43.69%) |
p70S6K | inactive (5.41%) |
AGC - Akt
Bioactivity |
---|
Kinase | GPCR |
---|
AKT2 | inactive (3.68%) |
AKT1 | inactive (2.86%) |
AKT3 | inactive (4.8%) |
AGC - SGK
Bioactivity |
---|
Kinase | GPCR |
---|
SGK1 | inactive (1.48%) |
SGK3 | inactive (0.42%) |
SGK2 | inactive (-3.53%) |
AGC - PKC
Bioactivity |
---|
Kinase | GPCR |
---|
PKCh | inactive (3.09%) |
PKCg | inactive (15.65%) |
PKCa | inactive (6.72%) |
PKCt | inactive (4.69%) |
PKCi | inactive (0.42%) |
AGC - PKG
Bioactivity |
---|
Kinase | GPCR |
---|
PKG2 | inactive (25.37%) |
PKG1 | active (55.02%) |
AGC - PKA
Bioactivity |
---|
Kinase | GPCR |
---|
PRKX | inactive (5.35%) |
AGC - DMPK
Bioactivity |
---|
Kinase | GPCR |
---|
ROCK1 | inactive (23.48%) |
ROCK2 | inactive (29.15%) |
MRCKb | inactive (16.41%) |
MRCKa | inactive (19.96%) |
CAMK
CAMK - RAD53
Bioactivity |
---|
Kinase | GPCR |
---|
CHK2 | active (79.11%) |
CAMK - DCAMKL
Bioactivity |
---|
Kinase | GPCR |
---|
DCLK2 | inactive (8.47%) |
CAMK - CAMK1
Bioactivity |
---|
Kinase | GPCR |
---|
CaMK4 | inactive (29.27%) |
CaMK1d | active (52.82%) |
CAMK - PHK
Bioactivity |
---|
Kinase | GPCR |
---|
PHKg1 | active (78.06%) |
PHKg2 | active (64.69%) |
CAMK - CAMK2
Bioactivity |
---|
Kinase | GPCR |
---|
CaMK2d | active (75.11%) |
CaMK2a | active (53.33%) |
CAMK - MAPKAPK
Bioactivity |
---|
Kinase | GPCR |
---|
MAPKAPK5 | inactive (16.03%) |
MAPKAPK2 | inactive (5.03%) |
MAPKAPK3 | inactive (7.11%) |
MNK2 | inactive (8.99%) |
MNK1 | inactive (1.83%) |
CAMK - PKD
Bioactivity |
---|
Kinase | GPCR |
---|
PKD3 | active (79.79%) |
PKD1 | active (84.31%) |
PKD2 | active (83.94%) |
CAMK - CAMKL
Bioactivity |
---|
Kinase | GPCR |
---|
MARK4 | inactive (37.76%) |
MARK3 | active (67.38%) |
MARK1 | inactive (47.69%) |
QIK | inactive (8.56%) |
SIK | inactive (14.33%) |
NuaK1 | active (85.04%) |
BRSK1 | inactive (-0.11%) |
BRSK2 | inactive (1.71%) |
MELK | active (78.28%) |
CHK1 | inactive (27.76%) |
PASK | inactive (2.69%) |
AMPKa1 | inactive (33.53%) |
AMPKa2 | inactive (13.25%) |
CAMK - TSSK
Bioactivity |
---|
Kinase | GPCR |
---|
TSSK2 | active (90.76%) |
TSSK1 | active (95.36%) |
CAMK - DAPK
Bioactivity |
---|
Kinase | GPCR |
---|
DAPK1 | inactive (46.02%) |
CAMK - PIM
Bioactivity |
---|
Kinase | GPCR |
---|
PIM2 | inactive (1.98%) |
PIM3 | inactive (19.88%) |
PIM1 | inactive (25.32%) |
CMGC
CMGC - MAPK
Bioactivity |
---|
Kinase | GPCR |
---|
JNK2 | active (89.08%) |
p38a | inactive (8.96%) |
p38b | inactive (9.48%) |
p38d | inactive (2.28%) |
Erk2 | inactive (15.33%) |
Erk1 | inactive (5.68%) |
CMGC - GSK
Bioactivity |
---|
Kinase | GPCR |
---|
GSK3A | inactive (5.19%) |
GSK3B | inactive (7.27%) |
CMGC - SRPK
Bioactivity |
---|
Kinase | GPCR |
---|
SRPK1 | inactive (1.46%) |
MSSK1 | inactive (4.84%) |
CMGC - CLK
Bioactivity |
---|
Kinase | GPCR |
---|
CLK3 | inactive (13.24%) |
CLK2 | active (88.43%) |
CMGC - DYRK
Bioactivity |
---|
Kinase | GPCR |
---|
HIPK1 | active (73.71%) |
HIPK4 | active (75.09%) |
DYRK1B | active (76.61%) |
DYRK1A | active (86.51%) |
DYRK2 | inactive (36.43%) |
CMGC - CK2
Bioactivity |
---|
Kinase | GPCR |
---|
CK2a1 | active (54.72%) |