Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW680191X

Inchikey : WLLKPDBSPXZCTG-UHFFFAOYSA-N

ChemSpider : 4486640

Pubchem CID : 5329489

ChEMBL : CHEMBL517907

	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 (13.37%)
TYK2	inactive (-1.47%)
JAK2	inactive (0.71%)
JAK3	inactive (-3.57%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (3.37%)
FES	inactive (6.01%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (26.77%)
ABL2	inactive (14.79%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (8.24%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (5.57%)
BTK	inactive (1.2%)
TXK	inactive (7.94%)
TEC	inactive (9.84%)
ITK	inactive (-2.14%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (10.25%)
SRM	inactive (5.07%)
FRK	inactive (4.16%)
BLK	inactive (3.96%)
LCK	inactive (13.51%)
HCK	inactive (20.52%)
FGR	inactive (15.54%)
FYN	inactive (2.18%)
SRC	inactive (17.85%)
YES	inactive (12.33%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (-2.32%)
EphA4	inactive (15.32%)
EphA3	inactive (5.15%)
EphB4	inactive (-1.52%)
EphB3	inactive (0.73%)
EphB2	inactive (19.37%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (10.32%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (0.39%)
ZAP70	inactive (-2.29%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (28.49%)
ALK	inactive (31.9%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (8.09%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (4.34%)
IGF1R	inactive (-2.48%)
IRR	inactive (2.49%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (9.88%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (2.93%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (1.9%)
TRKB	inactive (2.28%)
TRKC	inactive (4.94%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (7.33%)
MET	inactive (8.4%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-7.98%)
MER	inactive (5.14%)
TYRO3	inactive (8.46%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (18.91%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (0.98%)
FGFR2	inactive (2.36%)
FGFR3	inactive (3.33%)
FGFR4	inactive (-1.61%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (4.95%)
KDR	inactive (19.64%)
FLT4	inactive (-12.97%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (2.93%)
KIT	inactive (7.12%)
FLT3	inactive (2.94%)
PDGFRa	inactive (30.42%)
PDGFRb	inactive (20.53%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (12.49%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (7.01%)
TNK1	inactive (20.87%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	active (85.43%)
ErbB2	inactive (29.88%)
ErbB4	active (63.8%)

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 (2.41%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (6.4%)

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 (5.3%)
MST1	inactive (7.8%)
MST2	inactive (7.49%)
MST4	inactive (-0.45%)
HGK	inactive (19.56%)
MINK	inactive (17.6%)
LOK	active (75.42%)
PAK1	inactive (7.48%)
PAK3	inactive (5.67%)
PAK2	inactive (1.48%)
PAK5	inactive (4.31%)
PAK6	inactive (-2.58%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (4.96%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (7.93%)
CK1g2	inactive (1.61%)
CK1g1	inactive (1.77%)
CK1g3	inactive (0.33%)

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 (2.68%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (2.47%)
AurC	inactive (-5.69%)
AurA	inactive (-0.05%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (8.52%)
NEK2	inactive (6.09%)
NEK9	inactive (10.22%)
NEK7	inactive (3.44%)
NEK6	inactive (3.84%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (8.32%)
IKKe	inactive (9.33%)
IKKb	inactive (9.06%)
IKKa	inactive (12.15%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (9.83%)

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 (8.97%)
GPRK6	inactive (6.6%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (2.25%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (1.8%)
MSK2	inactive (3.4%)
RSK1	inactive (5.51%)
RSK2	inactive (3.87%)
RSK4	inactive (3.55%)
RSK3	inactive (4.55%)
p70S6K	inactive (3.29%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (-2.09%)
AKT1	inactive (-3.06%)
AKT3	inactive (-0.78%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (5.99%)
SGK3	inactive (4.46%)
SGK2	inactive (4.33%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (4.94%)
PKCg	inactive (7.74%)
PKCa	inactive (0.29%)
PKCt	inactive (5.27%)
PKCi	inactive (1.19%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (8.83%)
PKG1	inactive (7.37%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (4.38%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (2.52%)
ROCK2	inactive (6.92%)
MRCKb	inactive (1.44%)
MRCKa	inactive (7.35%)

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 (7.73%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (-4.44%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-2.02%)
CaMK1d	inactive (0.48%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (19.03%)
PHKg2	inactive (6.86%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (5.51%)
CaMK2a	inactive (3.33%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (2.73%)
MAPKAPK2	inactive (1.98%)
MAPKAPK3	inactive (4.44%)
MNK2	inactive (31.77%)
MNK1	inactive (46.69%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (15.01%)
PKD1	inactive (25.03%)
PKD2	inactive (26.66%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (3.56%)
MARK3	inactive (6.08%)
MARK1	inactive (8.02%)
QIK	inactive (27.51%)
SIK	inactive (38.71%)
NuaK1	inactive (12.9%)
BRSK1	inactive (7.62%)
BRSK2	inactive (10.01%)
MELK	inactive (8.09%)
CHK1	inactive (4.94%)
PASK	inactive (4.19%)
AMPKa1	inactive (6.4%)
AMPKa2	inactive (4.43%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (2.71%)
TSSK1	inactive (6.34%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (2.74%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (-1.09%)
PIM3	inactive (36.17%)
PIM1	inactive (39.51%)

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 (4.58%)
p38a	inactive (13.89%)
p38b	inactive (7.25%)
p38d	inactive (4.8%)
Erk2	inactive (5.46%)
Erk1	inactive (5.78%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (1.81%)
GSK3B	inactive (1.89%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-0.94%)
MSSK1	inactive (-2.44%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (-1.87%)
CLK2	inactive (1.36%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (-1.22%)
HIPK4	inactive (24.91%)
DYRK1B	inactive (-1.25%)
DYRK1A	inactive (4.86%)
DYRK2	inactive (7.08%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (9.21%)