Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW780056X

Inchikey : DQKZVZRKPRQVEU-UHFFFAOYSA-N

ChemSpider : 8391268

Pubchem CID : 10215776

ChEMBL : CHEMBL1882194

	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 (4.83%)
TYK2	inactive (11.6%)
JAK2	inactive (20.85%)
JAK3	inactive (14.2%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (15.49%)
FES	inactive (28.01%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (29.54%)
ABL2	inactive (22.19%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (8.18%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (10.78%)
BTK	inactive (-0.83%)
TXK	inactive (1.91%)
TEC	inactive (3.21%)
ITK	inactive (-0.21%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (15.72%)
SRM	inactive (0.74%)
FRK	inactive (3.76%)
BLK	inactive (1.7%)
LCK	inactive (15.33%)
HCK	inactive (13.49%)
FGR	inactive (11.35%)
FYN	inactive (5.04%)
SRC	inactive (38.22%)
YES	inactive (22.47%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (-5.2%)
EphA4	inactive (15.21%)
EphA3	inactive (0.69%)
EphB4	inactive (8.4%)
EphB3	inactive (0.55%)
EphB2	inactive (27.23%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	active (81.34%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-0.45%)
ZAP70	inactive (-4.19%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (9.98%)
ALK	inactive (24.4%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	active (70.49%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	active (73.22%)
IGF1R	active (54.57%)
IRR	inactive (7.36%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (4.24%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (30.52%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (12.07%)
TRKB	inactive (7.47%)
TRKC	inactive (5.86%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (22.4%)
MET	inactive (10.42%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (16.34%)
MER	inactive (9.85%)
TYRO3	inactive (18.21%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (12.78%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (11.55%)
FGFR2	inactive (8.8%)
FGFR3	inactive (5.35%)
FGFR4	inactive (-3.39%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (16.2%)
KDR	inactive (39.09%)
FLT4	inactive (0.13%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	active (68.87%)
KIT	active (93.11%)
FLT3	inactive (47.68%)
PDGFRa	active (55.53%)
PDGFRb	active (71.78%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (12.18%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (3.2%)
TNK1	inactive (32.04%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (-1.76%)
ErbB2	inactive (3.96%)
ErbB4	inactive (5.17%)

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 (3.85%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (17.71%)

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 (21.17%)
MST1	inactive (15.95%)
MST2	inactive (9.79%)
MST4	inactive (0.74%)
HGK	inactive (20.35%)
MINK	inactive (17.02%)
LOK	inactive (18.02%)
PAK1	inactive (9.08%)
PAK3	inactive (6%)
PAK2	inactive (3.41%)
PAK5	inactive (5.43%)
PAK6	inactive (-2.98%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (13.13%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	active (54.28%)
CK1g2	inactive (13.74%)
CK1g1	inactive (6.01%)
CK1g3	inactive (10.55%)

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 (8.15%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	active (63.66%)
AurC	active (84.58%)
AurA	inactive (34.31%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (4.48%)
NEK2	inactive (3.41%)
NEK9	inactive (13.69%)
NEK7	inactive (9.4%)
NEK6	inactive (-0.16%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (12.29%)
IKKe	inactive (17.81%)
IKKb	inactive (17.5%)
IKKa	inactive (34.86%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (29.36%)

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 (3.71%)
GPRK6	inactive (1.08%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (2.98%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (2.51%)
MSK2	inactive (7.32%)
RSK1	inactive (2.52%)
RSK2	inactive (2.49%)
RSK4	inactive (9.62%)
RSK3	inactive (3.81%)
p70S6K	inactive (7.85%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (-2.22%)
AKT1	inactive (-1.93%)
AKT3	inactive (-1.26%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (7.61%)
SGK3	inactive (2.8%)
SGK2	inactive (4.57%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (7.25%)
PKCg	inactive (7.9%)
PKCa	inactive (17.76%)
PKCt	inactive (4.84%)
PKCi	inactive (2.03%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (13.71%)
PKG1	inactive (14.91%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (4.27%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (9.36%)
ROCK2	inactive (13.71%)
MRCKb	inactive (4.53%)
MRCKa	inactive (4.32%)

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 (7.56%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (1.64%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (0.34%)
CaMK1d	inactive (4.23%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (28.18%)
PHKg2	inactive (15.29%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (14.34%)
CaMK2a	inactive (4.21%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (2.13%)
MAPKAPK2	inactive (2.01%)
MAPKAPK3	inactive (3.32%)
MNK2	inactive (8.84%)
MNK1	inactive (9.82%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	active (62.61%)
PKD1	active (65.58%)
PKD2	active (64.4%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (18.94%)
MARK3	inactive (24.71%)
MARK1	inactive (20.88%)
QIK	inactive (47.16%)
SIK	inactive (24.05%)
NuaK1	active (84.33%)
BRSK1	inactive (3.16%)
BRSK2	inactive (10.61%)
MELK	active (55.42%)
CHK1	inactive (11.62%)
PASK	inactive (-0.46%)
AMPKa1	inactive (9.99%)
AMPKa2	inactive (12.74%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (2.16%)
TSSK1	inactive (26.46%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (1.28%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (-0.59%)
PIM3	inactive (37.22%)
PIM1	inactive (23.02%)

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 (30.94%)
p38a	inactive (13.08%)
p38b	inactive (4.99%)
p38d	inactive (9.25%)
Erk2	inactive (15.76%)
Erk1	inactive (7.61%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	active (65.75%)
GSK3B	active (62.32%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-1.36%)
MSSK1	inactive (-0.22%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (5.2%)
CLK2	active (91.72%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	active (71.86%)
HIPK4	active (59.04%)
DYRK1B	active (69.19%)
DYRK1A	active (87.98%)
DYRK2	inactive (25.66%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (31.11%)