Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW811168X

Inchikey : WKJFLAJZSWRICW-FOKLQQMPSA-N

ChemSpider : 7879067

Pubchem CID : 9604948

ChEMBL : CHEMBL66292

	DRx	RBC	Metz	Millipore	GPCR
bioactivity	Kd (nM)	Remain Activity (%)	Ki (nM)	Remain Activity (%)	Inhibition (%)
active criteria	<3000nM	<50%	<1000nM	<50%	>50%

TK

Test Member No. in Family
Family	no. Member on 518kinase	GPCR
JakA	4	4
Fer	2	2
Abl	2	2
Csk	2	1
Tec	5	5
Src	11	10
Eph	14	6
FAK	2	1
Syk	2	2
ALK	2	2
Sev	1	1
InsR	3	3
DDR	2	1
Musk	1	1
Trk	3	3
Met	2	2
Axl	3	3
Ret	1	1
FGFR	4	4
VEGFR	3	3
PDGFR	5	5
Tie	2	1
Ack	2	2
EGFR	4	3

TK - JakA

Bioactivity
Kinase	GPCR
JAK1	inactive (6.92%)
TYK2	inactive (1.37%)
JAK2	inactive (11.53%)
JAK3	inactive (5.53%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (2.49%)
FES	inactive (0.07%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	active (72.99%)
ABL2	active (61.67%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (18.19%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (30.74%)
BTK	inactive (-3.39%)
TXK	inactive (12.45%)
TEC	inactive (10.42%)
ITK	inactive (0.29%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (26.8%)
SRM	inactive (17.77%)
FRK	inactive (3.05%)
BLK	inactive (38.36%)
LCK	active (73.92%)
HCK	active (55.7%)
FGR	active (64.02%)
FYN	active (69.82%)
SRC	active (77.37%)
YES	active (57.39%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (1.45%)
EphA4	inactive (11.74%)
EphA3	inactive (-1.2%)
EphB4	inactive (6.93%)
EphB3	inactive (-2.08%)
EphB2	inactive (11.49%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (5.9%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-1.66%)
ZAP70	inactive (1.31%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (2.05%)
ALK	inactive (-1.6%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (27.18%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (1.06%)
IGF1R	inactive (-5.27%)
IRR	inactive (0.63%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (7.83%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (23.28%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (5.3%)
TRKB	inactive (19.34%)
TRKC	inactive (22.32%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (44.28%)
MET	inactive (47.61%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (1.34%)
MER	inactive (28.3%)
TYRO3	inactive (22.39%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (30.73%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (0.92%)
FGFR2	inactive (4.85%)
FGFR3	inactive (4.08%)
FGFR4	inactive (-1.16%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (18.81%)
KDR	active (66.43%)
FLT4	inactive (31.4%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (22.46%)
KIT	active (61.65%)
FLT3	inactive (27.85%)
PDGFRa	active (77.81%)
PDGFRb	active (78.14%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (31.43%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (1.96%)
TNK1	inactive (20.01%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (22.65%)
ErbB2	inactive (3.96%)
ErbB4	inactive (7.9%)

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 (1.12%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (16.37%)

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 (0.9%)
MST1	inactive (4.3%)
MST2	inactive (2.91%)
MST4	inactive (2.58%)
HGK	active (59.4%)
MINK	active (50.32%)
LOK	inactive (16.3%)
PAK1	inactive (3.02%)
PAK3	inactive (1.53%)
PAK2	inactive (-0.47%)
PAK5	inactive (10.06%)
PAK6	inactive (5.24%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (1.58%)

CK1

Test Member No. in Family
Family	no. Member on 518kinase	GPCR
CK1	7	4

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (5.91%)
CK1g2	inactive (-0.73%)
CK1g1	inactive (-0.99%)
CK1g3	inactive (-2.43%)

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 (0.92%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (42.41%)
AurC	inactive (12.22%)
AurA	inactive (28.41%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (5.16%)
NEK2	inactive (1.84%)
NEK9	inactive (1.23%)
NEK7	inactive (2.28%)
NEK6	inactive (-0.32%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (7.99%)
IKKe	inactive (8.64%)
IKKb	inactive (-0.15%)
IKKa	inactive (-0.62%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (-19.19%)

AGC

Test Member No. in Family
Family	no. Member on 518kinase	GPCR
GRK	7	2
PDK1	1	1
RSK	8	7
Akt	3	3
SGK	3	3
PKC	9	5
PKG	2	2
PKA	5	1
DMPK	7	4

AGC - GRK

Bioactivity
Kinase	GPCR
GPRK7	inactive (0.56%)
GPRK6	inactive (-1.78%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (5.75%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (-0.55%)
MSK2	inactive (2.04%)
RSK1	inactive (0.53%)
RSK2	inactive (0.98%)
RSK4	inactive (3.2%)
RSK3	inactive (4.48%)
p70S6K	inactive (5.85%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (-2.73%)
AKT1	inactive (-2.91%)
AKT3	inactive (-3.66%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (10.12%)
SGK3	inactive (2.6%)
SGK2	inactive (4.33%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (2.85%)
PKCg	inactive (3.18%)
PKCa	inactive (-0.59%)
PKCt	inactive (1.19%)
PKCi	inactive (0.98%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (1.79%)
PKG1	inactive (1.69%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (1.61%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (1.16%)
ROCK2	inactive (1.85%)
MRCKb	inactive (0.16%)
MRCKa	inactive (-0.45%)

CAMK

Test Member No. in Family
Family	no. Member on 518kinase	GPCR
RAD53	1	1
DCAMKL	3	1
CAMK1	5	2
PHK	2	2
CAMK2	4	2
MAPKAPK	5	5
PKD	3	3
CAMKL	20	13
TSSK	5	2
DAPK	5	1
PIM	3	3

CAMK - RAD53

Bioactivity
Kinase	GPCR
CHK2	inactive (0.05%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (-3.25%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (0.23%)
CaMK1d	inactive (0.51%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (2.63%)
PHKg2	inactive (2.21%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (4.11%)
CaMK2a	inactive (1.01%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (0.26%)
MAPKAPK2	inactive (-0.87%)
MAPKAPK3	inactive (-1.31%)
MNK2	inactive (23.95%)
MNK1	inactive (34.18%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (-2.38%)
PKD1	inactive (-1.45%)
PKD2	inactive (-2.8%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (3.52%)
MARK3	inactive (4.26%)
MARK1	inactive (4.83%)
QIK	inactive (29.94%)
SIK	inactive (26%)
NuaK1	inactive (37.42%)
BRSK1	active (52.46%)
BRSK2	active (60.79%)
MELK	inactive (4.85%)
CHK1	inactive (-1.03%)
PASK	inactive (0.02%)
AMPKa1	inactive (2%)
AMPKa2	inactive (4.43%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (0.31%)
TSSK1	inactive (-0.61%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (-2.35%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (-2.5%)
PIM3	inactive (2.23%)
PIM1	inactive (1.73%)

CMGC

Test Member No. in Family
Family	no. Member on 518kinase	GPCR
MAPK	14	6
GSK	2	2
SRPK	3	2
CLK	4	2
DYRK	10	5
CK2	3	1

CMGC - MAPK

Bioactivity
Kinase	GPCR
JNK2	inactive (4.9%)
p38a	inactive (4.7%)
p38b	inactive (1.99%)
p38d	inactive (6.79%)
Erk2	inactive (1.93%)
Erk1	inactive (1.55%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	active (80.61%)
GSK3B	active (78.96%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (0.02%)
MSSK1	inactive (1%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (13.51%)
CLK2	inactive (18.37%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	active (64.34%)
HIPK4	active (60.58%)
DYRK1B	inactive (47.3%)
DYRK1A	active (64.28%)
DYRK2	inactive (24.95%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (39.12%)