Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW794607X

Inchikey : UUZWUKJJOLIQMT-BRJLIKDPSA-N

ChemSpider : 7879045

Pubchem CID : 9604926

ChEMBL : CHEMBL67241

	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 (11.66%)
TYK2	inactive (4.3%)
JAK2	inactive (14.68%)
JAK3	inactive (8.21%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (9.15%)
FES	inactive (5.6%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	active (75.33%)
ABL2	active (61.86%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (12.07%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (13.36%)
BTK	inactive (4.2%)
TXK	inactive (8.54%)
TEC	inactive (7.76%)
ITK	inactive (10.77%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	active (51.03%)
SRM	inactive (7.86%)
FRK	inactive (3.14%)
BLK	active (62.91%)
LCK	active (68.34%)
HCK	inactive (35.84%)
FGR	active (51.98%)
FYN	active (52.81%)
SRC	active (81.78%)
YES	active (82.84%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (5.31%)
EphA4	inactive (17.41%)
EphA3	inactive (3.12%)
EphB4	inactive (5.77%)
EphB3	inactive (1.75%)
EphB2	inactive (9.31%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (12.24%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-2.86%)
ZAP70	inactive (3.95%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (4.23%)
ALK	inactive (3.35%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (33.41%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (0.96%)
IGF1R	inactive (-0.01%)
IRR	inactive (1.63%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (7.68%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (49.94%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (7.34%)
TRKB	inactive (33.89%)
TRKC	inactive (36.78%)

TK - Met

Bioactivity
Kinase	GPCR
RON	active (57.91%)
MET	inactive (48.99%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (13.16%)
MER	inactive (25.61%)
TYRO3	inactive (42.78%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	active (54.73%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (3.31%)
FGFR2	inactive (19.35%)
FGFR3	inactive (8.88%)
FGFR4	inactive (3.38%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (19.7%)
KDR	active (64.93%)
FLT4	inactive (40.68%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (17.55%)
KIT	inactive (23.7%)
FLT3	inactive (17.6%)
PDGFRa	active (78.39%)
PDGFRb	active (78.83%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (36.19%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (3.51%)
TNK1	inactive (47.95%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (33.47%)
ErbB2	inactive (4.49%)
ErbB4	inactive (42.97%)

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 (0.71%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (1.5%)

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 (3.57%)
MST1	inactive (12.31%)
MST2	inactive (9.89%)
MST4	inactive (-1.3%)
HGK	inactive (44.14%)
MINK	inactive (35.91%)
LOK	inactive (28.42%)
PAK1	inactive (-0.69%)
PAK3	inactive (1.61%)
PAK2	inactive (-0.31%)
PAK5	inactive (5.05%)
PAK6	inactive (2.09%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (2.07%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (1.89%)
CK1g2	inactive (1.01%)
CK1g1	inactive (1.57%)
CK1g3	inactive (0.9%)

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 (0.93%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (43.75%)
AurC	active (58.52%)
AurA	active (70.67%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (7.87%)
NEK2	inactive (0.85%)
NEK9	inactive (0.45%)
NEK7	inactive (-0.91%)
NEK6	inactive (2.63%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (20.19%)
IKKe	inactive (13.41%)
IKKb	inactive (3.19%)
IKKa	inactive (0.68%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (15.69%)

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 (4.45%)
GPRK6	inactive (3.97%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (10.31%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (-2.6%)
MSK2	inactive (2.6%)
RSK1	inactive (4.72%)
RSK2	inactive (4.75%)
RSK4	inactive (3.54%)
RSK3	inactive (2.43%)
p70S6K	inactive (8.74%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (-0.08%)
AKT1	inactive (-0.51%)
AKT3	inactive (-1.08%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (13.57%)
SGK3	inactive (5.07%)
SGK2	inactive (10.93%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (2.92%)
PKCg	inactive (5.49%)
PKCa	inactive (1.45%)
PKCt	inactive (2.98%)
PKCi	inactive (12.49%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (4.72%)
PKG1	inactive (2.57%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (4.42%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (13.68%)
ROCK2	inactive (28.15%)
MRCKb	inactive (0.92%)
MRCKa	inactive (5.18%)

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 (0.34%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (2.98%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-3.1%)
CaMK1d	inactive (1.66%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (19.53%)
PHKg2	inactive (7.69%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (1.17%)
CaMK2a	inactive (3.36%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (1.6%)
MAPKAPK2	inactive (-2.37%)
MAPKAPK3	inactive (-4.82%)
MNK2	active (72.19%)
MNK1	active (69.11%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (0.02%)
PKD1	inactive (1.22%)
PKD2	inactive (1.21%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (9.44%)
MARK3	inactive (9.23%)
MARK1	inactive (10.3%)
QIK	inactive (21.13%)
SIK	inactive (9.54%)
NuaK1	inactive (36.34%)
BRSK1	inactive (24.68%)
BRSK2	inactive (29.03%)
MELK	inactive (3.93%)
CHK1	inactive (-5.65%)
PASK	inactive (3.05%)
AMPKa1	inactive (3.53%)
AMPKa2	inactive (2.07%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (3.17%)
TSSK1	inactive (6.17%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (-8.41%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (0.32%)
PIM3	inactive (4.06%)
PIM1	inactive (1.01%)

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 (6.14%)
p38a	inactive (7.62%)
p38b	inactive (25.53%)
p38d	inactive (3.1%)
Erk2	inactive (1.54%)
Erk1	inactive (3.62%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	active (71.83%)
GSK3B	active (68.7%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (3.51%)
MSSK1	inactive (0.97%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (9.87%)
CLK2	inactive (10.94%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (13.5%)
HIPK4	inactive (27.67%)
DYRK1B	inactive (9.45%)
DYRK1A	inactive (20.55%)
DYRK2	inactive (14.23%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (14.12%)