Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW814408X

Inchikey : YMOZGQKWFWKZJV-YSURURNPSA-N

ChemSpider : 7879031

Pubchem CID : 9604912

ChEMBL : CHEMBL206010

	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 (15.32%)
TYK2	inactive (10.47%)
JAK2	inactive (15.08%)
JAK3	inactive (24.85%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (8.57%)
FES	inactive (2.81%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	active (81.67%)
ABL2	active (78.58%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (17.28%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (45.13%)
BTK	inactive (2.48%)
TXK	inactive (16.8%)
TEC	inactive (16.46%)
ITK	inactive (3.59%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (4.81%)
SRM	inactive (11.77%)
FRK	inactive (3.28%)
BLK	active (57.86%)
LCK	active (81.95%)
HCK	active (51.84%)
FGR	active (54.17%)
FYN	active (58.66%)
SRC	active (77.26%)
YES	active (65.19%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (14.61%)
EphA4	inactive (30.5%)
EphA3	inactive (6.01%)
EphB4	inactive (13.46%)
EphB3	inactive (-5.7%)
EphB2	inactive (25.94%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (9.78%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (4.79%)
ZAP70	inactive (1.55%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (2.09%)
ALK	inactive (1.19%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (14.38%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (3.79%)
IGF1R	inactive (2.22%)
IRR	inactive (2.79%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (14.78%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (48.84%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (7.45%)
TRKB	inactive (19.4%)
TRKC	inactive (23.31%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (42.38%)
MET	inactive (27.34%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (3.21%)
MER	inactive (15.71%)
TYRO3	inactive (38.01%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (37.93%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (6.34%)
FGFR2	inactive (9.49%)
FGFR3	inactive (8.05%)
FGFR4	inactive (2.46%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (18.41%)
KDR	active (60.96%)
FLT4	inactive (29.48%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	active (68.6%)
KIT	active (87.95%)
FLT3	inactive (39.02%)
PDGFRa	active (82.77%)
PDGFRb	active (81.13%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (27.53%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (15.3%)
TNK1	inactive (41.74%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (41.87%)
ErbB2	inactive (2.47%)
ErbB4	inactive (21.92%)

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 (5.06%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (11.04%)

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 (11.86%)
MST1	inactive (15.21%)
MST2	inactive (13.16%)
MST4	inactive (20.26%)
HGK	active (74.53%)
MINK	active (61.89%)
LOK	inactive (35.39%)
PAK1	inactive (1.11%)
PAK3	inactive (2.84%)
PAK2	inactive (0.74%)
PAK5	inactive (0.73%)
PAK6	inactive (-1.79%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (6.21%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (7.98%)
CK1g2	inactive (4.26%)
CK1g1	inactive (4.05%)
CK1g3	inactive (4.42%)

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 (1.97%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	active (55.37%)
AurC	active (90.25%)
AurA	inactive (37.74%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (10.55%)
NEK2	inactive (2.88%)
NEK9	inactive (5.28%)
NEK7	inactive (3.62%)
NEK6	inactive (-1.66%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (34.58%)
IKKe	inactive (16.78%)
IKKb	inactive (1.73%)
IKKa	inactive (9.01%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (10.57%)

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 (-6.92%)
GPRK6	inactive (-7.11%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (27.99%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (9.82%)
MSK2	inactive (4.13%)
RSK1	inactive (7.19%)
RSK2	inactive (7.47%)
RSK4	inactive (10.63%)
RSK3	inactive (11.73%)
p70S6K	inactive (8.54%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (-0.06%)
AKT1	inactive (0.32%)
AKT3	inactive (-0.22%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (19.14%)
SGK3	inactive (1.84%)
SGK2	inactive (18.2%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (1.53%)
PKCg	inactive (7.65%)
PKCa	inactive (4.24%)
PKCt	inactive (0.99%)
PKCi	inactive (20.31%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (8.58%)
PKG1	inactive (4.69%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (-0.16%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (7.68%)
ROCK2	inactive (11.7%)
MRCKb	inactive (5.25%)
MRCKa	inactive (6.35%)

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 (6.91%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (8.13%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (4.18%)
CaMK1d	inactive (4.07%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (12.11%)
PHKg2	inactive (1.52%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (15.22%)
CaMK2a	inactive (6.66%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (-1.66%)
MAPKAPK2	inactive (3.56%)
MAPKAPK3	inactive (11.07%)
MNK2	active (51.07%)
MNK1	active (57.1%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (5.38%)
PKD1	inactive (6.07%)
PKD2	inactive (5.96%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (7.5%)
MARK3	inactive (11.84%)
MARK1	inactive (8.15%)
QIK	active (67.41%)
SIK	inactive (48.86%)
NuaK1	inactive (38.5%)
BRSK1	inactive (21.4%)
BRSK2	inactive (29.77%)
MELK	inactive (4.88%)
CHK1	inactive (11.26%)
PASK	inactive (-0.58%)
AMPKa1	inactive (6.84%)
AMPKa2	inactive (7.68%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (-2.11%)
TSSK1	inactive (-0.71%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (11.17%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (1.1%)
PIM3	inactive (2.78%)
PIM1	inactive (5.38%)

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 (8.51%)
p38a	inactive (13.32%)
p38b	inactive (7.25%)
p38d	inactive (38.18%)
Erk2	inactive (5.09%)
Erk1	inactive (6.39%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	active (83.48%)
GSK3B	active (83.51%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-1.68%)
MSSK1	inactive (1.67%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (14.01%)
CLK2	inactive (20.45%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (41.66%)
HIPK4	inactive (43.23%)
DYRK1B	active (50.48%)
DYRK1A	active (58.47%)
DYRK2	active (57.8%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (43.74%)