Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW784752X

Inchikey : PVIMTNAWPMEBAK-LSHDLFTRSA-N

ChemSpider : 7879030

Pubchem CID : 9604911

ChEMBL : CHEMBL306865

	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 (15.31%)
TYK2	inactive (0.71%)
JAK2	inactive (13.5%)
JAK3	inactive (10.56%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (11.74%)
FES	inactive (5.85%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	active (89.02%)
ABL2	active (82.83%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (16.81%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (46.65%)
BTK	inactive (2.16%)
TXK	inactive (18.56%)
TEC	inactive (17.23%)
ITK	inactive (5.47%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (23.14%)
SRM	inactive (14.3%)
FRK	inactive (5.75%)
BLK	active (63.6%)
LCK	active (84.02%)
HCK	active (59.23%)
FGR	active (69.98%)
FYN	active (73.76%)
SRC	active (87.26%)
YES	active (72.97%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (15.76%)
EphA4	inactive (35.45%)
EphA3	inactive (6.97%)
EphB4	inactive (13.66%)
EphB3	inactive (3.82%)
EphB2	inactive (30.38%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (16.46%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (9.95%)
ZAP70	inactive (3.98%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (6.38%)
ALK	inactive (7.96%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	active (75.95%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (7.36%)
IGF1R	inactive (4.88%)
IRR	inactive (5.33%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (9.37%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (45.56%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (12.79%)
TRKB	inactive (37.59%)
TRKC	inactive (36.94%)

TK - Met

Bioactivity
Kinase	GPCR
RON	active (60.85%)
MET	inactive (49.47%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (6.36%)
MER	inactive (39.16%)
TYRO3	inactive (41.58%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	active (50.26%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (8.02%)
FGFR2	inactive (14.54%)
FGFR3	inactive (11.94%)
FGFR4	inactive (7.56%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (27.61%)
KDR	active (69.23%)
FLT4	inactive (38.42%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (30.18%)
KIT	active (57.21%)
FLT3	inactive (28.27%)
PDGFRa	active (79.52%)
PDGFRb	active (81.18%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (37.53%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (9.3%)
TNK1	active (52.29%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (28.81%)
ErbB2	inactive (5.53%)
ErbB4	inactive (20.85%)

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 (4.07%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (21.51%)

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 (7.06%)
MST1	inactive (12.78%)
MST2	inactive (10.69%)
MST4	inactive (7.18%)
HGK	active (67.7%)
MINK	active (55.4%)
LOK	inactive (33.51%)
PAK1	inactive (7.75%)
PAK3	inactive (5.78%)
PAK2	inactive (2.37%)
PAK5	inactive (6.09%)
PAK6	inactive (-8.53%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (7.23%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (11.18%)
CK1g2	inactive (9.79%)
CK1g1	inactive (7.48%)
CK1g3	inactive (6.59%)

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 (3.32%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (43.09%)
AurC	active (61.4%)
AurA	active (73.77%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (12.5%)
NEK2	inactive (5.47%)
NEK9	inactive (6.71%)
NEK7	inactive (3.46%)
NEK6	inactive (3.93%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (13.1%)
IKKe	inactive (9.13%)
IKKb	inactive (4.07%)
IKKa	inactive (1.71%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (18.53%)

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 (5.17%)
GPRK6	inactive (1.85%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (8.82%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (4.1%)
MSK2	inactive (4.26%)
RSK1	inactive (7.17%)
RSK2	inactive (4.26%)
RSK4	inactive (4.33%)
RSK3	inactive (4.92%)
p70S6K	inactive (7.24%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (-0.44%)
AKT1	inactive (-0.78%)
AKT3	inactive (0.47%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (16.05%)
SGK3	inactive (6.6%)
SGK2	inactive (11.95%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (2.1%)
PKCg	inactive (7.85%)
PKCa	inactive (8.07%)
PKCt	inactive (5.71%)
PKCi	inactive (13.06%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (6.05%)
PKG1	-

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (2.86%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (9.67%)
ROCK2	inactive (19.39%)
MRCKb	inactive (0.77%)
MRCKa	inactive (3.78%)

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 (4.89%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (1.8%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-1.96%)
CaMK1d	inactive (2.43%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (17.64%)
PHKg2	inactive (7.43%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (12.82%)
CaMK2a	inactive (6.87%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (3.04%)
MAPKAPK2	inactive (1.87%)
MAPKAPK3	inactive (4.56%)
MNK2	active (59.25%)
MNK1	active (70.42%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (9.03%)
PKD1	inactive (10.09%)
PKD2	inactive (9.06%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (5.01%)
MARK3	inactive (7.7%)
MARK1	inactive (9.17%)
QIK	active (54.05%)
SIK	inactive (27.85%)
NuaK1	active (54.58%)
BRSK1	active (52.5%)
BRSK2	active (60.07%)
MELK	inactive (6.51%)
CHK1	inactive (5.7%)
PASK	inactive (0.25%)
AMPKa1	inactive (9.15%)
AMPKa2	inactive (7.87%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (2.48%)
TSSK1	inactive (5.05%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (4.53%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (1.69%)
PIM3	inactive (4.38%)
PIM1	inactive (3.36%)

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 (11.24%)
p38a	inactive (16.39%)
p38b	inactive (10.85%)
p38d	inactive (43.32%)
Erk2	inactive (7.16%)
Erk1	inactive (7.65%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	active (90.03%)
GSK3B	active (89.21%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (4.65%)
MSSK1	inactive (1.8%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (19.29%)
CLK2	inactive (34.97%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	active (69.85%)
HIPK4	active (61.3%)
DYRK1B	active (53.88%)
DYRK1A	active (72.26%)
DYRK2	active (58.94%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	active (59.73%)