Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW709042A

Inchikey : LMWATHMMGRFQHI-UHFFFAOYSA-N

ChemSpider : 28484518

Pubchem CID : 57403317

ChEMBL : CHEMBL1909374

	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 (7.18%)
TYK2	inactive (-0.97%)
JAK2	inactive (4.06%)
JAK3	inactive (9.29%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (7.9%)
FES	inactive (2.49%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	active (62.3%)
ABL2	active (65.89%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (11.72%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (2.54%)
BTK	inactive (3.03%)
TXK	inactive (6.27%)
TEC	inactive (8.67%)
ITK	inactive (2.09%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (8.39%)
SRM	inactive (4.56%)
FRK	inactive (2.1%)
BLK	inactive (4.59%)
LCK	inactive (14.42%)
HCK	inactive (21.76%)
FGR	inactive (7.53%)
FYN	inactive (21.46%)
SRC	inactive (11.2%)
YES	inactive (7.23%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (26.02%)
EphA4	active (64.17%)
EphA3	inactive (8.94%)
EphB4	inactive (27.48%)
EphB3	inactive (8.33%)
EphB2	active (61.76%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (14.21%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-0.11%)
ZAP70	inactive (1.65%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (3.76%)
ALK	inactive (6.42%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (11.42%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (2.26%)
IGF1R	inactive (7.91%)
IRR	inactive (3.55%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	active (78.72%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	active (63.89%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	active (52.19%)
TRKB	inactive (35.06%)
TRKC	inactive (40.98%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (5.31%)
MET	inactive (19.23%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (19.21%)
MER	inactive (3.74%)
TYRO3	inactive (16.84%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	active (90.21%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (6.8%)
FGFR2	inactive (18.76%)
FGFR3	inactive (6.31%)
FGFR4	inactive (0.83%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (39.3%)
KDR	active (68.13%)
FLT4	inactive (36.22%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (48.12%)
KIT	active (85.06%)
FLT3	active (53.36%)
PDGFRa	active (78.43%)
PDGFRb	inactive (31.14%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	active (60.52%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (4.59%)
TNK1	inactive (39.99%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (1.11%)
ErbB2	inactive (4.41%)
ErbB4	inactive (9.12%)

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 (2.09%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (33.38%)

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 (18.98%)
MST1	inactive (10.57%)
MST2	inactive (8.42%)
MST4	inactive (-0.48%)
HGK	inactive (5.89%)
MINK	inactive (4.54%)
LOK	active (50.16%)
PAK1	inactive (5.94%)
PAK3	inactive (2.99%)
PAK2	inactive (2.3%)
PAK5	inactive (4.86%)
PAK6	inactive (3.44%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (2.61%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (3.79%)
CK1g2	inactive (2.09%)
CK1g1	inactive (2.88%)
CK1g3	inactive (2.93%)

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 (1.84%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (13.86%)
AurC	inactive (40.77%)
AurA	inactive (12.45%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (2.89%)
NEK2	inactive (3.11%)
NEK9	inactive (10.32%)
NEK7	inactive (4.36%)
NEK6	inactive (1.7%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (4.56%)
IKKe	inactive (3.04%)
IKKb	inactive (2.88%)
IKKa	inactive (-0.85%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (19.16%)

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 (-2.78%)
GPRK6	inactive (4.7%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (1.14%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (5.67%)
MSK2	inactive (3.01%)
RSK1	inactive (5.03%)
RSK2	inactive (1.47%)
RSK4	inactive (2.72%)
RSK3	inactive (20.49%)
p70S6K	inactive (36.4%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (1.18%)
AKT1	inactive (1.04%)
AKT3	inactive (1.51%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (3.96%)
SGK3	inactive (2.24%)
SGK2	inactive (4.13%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (4.58%)
PKCg	inactive (3.66%)
PKCa	inactive (1.8%)
PKCt	inactive (2.18%)
PKCi	inactive (0.93%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (2.23%)
PKG1	inactive (3.65%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (1.09%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (6.36%)
ROCK2	inactive (8.83%)
MRCKb	inactive (-0.22%)
MRCKa	inactive (1%)

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 (3.89%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (-0.03%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-0.86%)
CaMK1d	inactive (1.95%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (7.47%)
PHKg2	inactive (4.6%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (4.57%)
CaMK2a	inactive (2.85%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (0.98%)
MAPKAPK2	inactive (1.81%)
MAPKAPK3	inactive (16.7%)
MNK2	inactive (22.05%)
MNK1	inactive (21.03%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (3.63%)
PKD1	inactive (3.41%)
PKD2	inactive (4.25%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (3.1%)
MARK3	inactive (22.88%)
MARK1	inactive (5.14%)
QIK	inactive (6.45%)
SIK	inactive (9.55%)
NuaK1	inactive (3.05%)
BRSK1	inactive (0.16%)
BRSK2	inactive (2.83%)
MELK	inactive (2.36%)
CHK1	inactive (5.63%)
PASK	inactive (0.73%)
AMPKa1	inactive (2.98%)
AMPKa2	inactive (4.55%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (0.74%)
TSSK1	inactive (0.69%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (5.19%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (-0.13%)
PIM3	inactive (-0.27%)
PIM1	inactive (0.07%)

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 (6.62%)
p38a	inactive (39.99%)
p38b	inactive (32.54%)
p38d	inactive (3.87%)
Erk2	inactive (2.7%)
Erk1	inactive (3.58%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (8.16%)
GSK3B	inactive (7.73%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (7.91%)
MSSK1	active (50.69%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (3.71%)
CLK2	inactive (1.05%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (0.17%)
HIPK4	inactive (47.68%)
DYRK1B	inactive (3.47%)
DYRK1A	inactive (4.75%)
DYRK2	inactive (3.65%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (4.99%)