Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW734508X

Inchikey : LOQFPSAYBYTGOA-UHFFFAOYSA-N

ChemSpider : 23323865

Pubchem CID : 25093474

ChEMBL : CHEMBL257113

	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 (9.78%)
TYK2	inactive (-4.07%)
JAK2	inactive (2.79%)
JAK3	inactive (0.46%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (3.05%)
FES	inactive (4.25%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (9.95%)
ABL2	inactive (9.01%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (7.37%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (5.89%)
BTK	inactive (1.05%)
TXK	inactive (3.16%)
TEC	inactive (6.71%)
ITK	inactive (2.05%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (7.36%)
SRM	inactive (2.96%)
FRK	inactive (3.45%)
BLK	inactive (1.41%)
LCK	inactive (2.64%)
HCK	inactive (8.3%)
FGR	inactive (2.02%)
FYN	inactive (0.54%)
SRC	inactive (10.22%)
YES	inactive (7.53%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (0.66%)
EphA4	inactive (10.77%)
EphA3	inactive (6.16%)
EphB4	inactive (2.08%)
EphB3	inactive (5.58%)
EphB2	inactive (9.32%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (9.85%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-0.72%)
ZAP70	inactive (7.42%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (4.76%)
ALK	inactive (5.21%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (6.04%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (5.71%)
IGF1R	inactive (6.53%)
IRR	inactive (3.22%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (3.42%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (6.37%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (1.38%)
TRKB	inactive (4.55%)
TRKC	inactive (3.95%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (8.29%)
MET	inactive (7.87%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-8.4%)
MER	inactive (0.56%)
TYRO3	inactive (4.17%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (7.32%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (0.61%)
FGFR2	inactive (5.08%)
FGFR3	inactive (6.22%)
FGFR4	inactive (0.59%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (1.49%)
KDR	inactive (9.47%)
FLT4	inactive (-1.03%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (1.96%)
KIT	inactive (9.77%)
FLT3	inactive (4.66%)
PDGFRa	inactive (15.21%)
PDGFRb	inactive (8.15%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (2.87%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (2.25%)
TNK1	inactive (11.35%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (3.25%)
ErbB2	inactive (5.51%)
ErbB4	inactive (12.53%)

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 (2.66%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (6.82%)

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 (3.14%)
MST1	inactive (9.93%)
MST2	inactive (10.42%)
MST4	inactive (0.39%)
HGK	inactive (14.06%)
MINK	inactive (14.74%)
LOK	inactive (7.39%)
PAK1	inactive (10.49%)
PAK3	inactive (5.35%)
PAK2	inactive (3.86%)
PAK5	inactive (2.3%)
PAK6	inactive (-1.37%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (4.7%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (5.86%)
CK1g2	inactive (4.15%)
CK1g1	inactive (4.29%)
CK1g3	inactive (3.17%)

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 (3.89%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (3.09%)
AurC	inactive (-4.74%)
AurA	inactive (7.79%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (4%)
NEK2	inactive (5.41%)
NEK9	inactive (7.69%)
NEK7	inactive (4.11%)
NEK6	inactive (6.86%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (6.92%)
IKKe	inactive (8.77%)
IKKb	inactive (5.6%)
IKKa	inactive (-3.16%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (0.98%)

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 (6.04%)
GPRK6	inactive (10.42%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (2.56%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (3.95%)
MSK2	inactive (3.75%)
RSK1	inactive (4.92%)
RSK2	inactive (1.76%)
RSK4	inactive (2.8%)
RSK3	inactive (2.85%)
p70S6K	inactive (3.46%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (1.84%)
AKT1	inactive (1.35%)
AKT3	inactive (1.48%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (10.79%)
SGK3	inactive (7.89%)
SGK2	inactive (7.09%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (6.75%)
PKCg	inactive (5.25%)
PKCa	inactive (1.45%)
PKCt	inactive (5.18%)
PKCi	inactive (1.94%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (3.44%)
PKG1	inactive (5.43%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (4.63%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (2.23%)
ROCK2	inactive (6.19%)
MRCKb	inactive (-0.8%)
MRCKa	inactive (2.11%)

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 (4.86%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (4.29%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-2.97%)
CaMK1d	inactive (0.22%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (5.91%)
PHKg2	inactive (7.38%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (6.04%)
CaMK2a	inactive (3.99%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (4.28%)
MAPKAPK2	inactive (2.7%)
MAPKAPK3	inactive (6.73%)
MNK2	inactive (6.05%)
MNK1	inactive (6.32%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (7.35%)
PKD1	inactive (9.11%)
PKD2	inactive (7.93%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (2.85%)
MARK3	inactive (7.47%)
MARK1	inactive (6.5%)
QIK	inactive (5.76%)
SIK	inactive (10.69%)
NuaK1	inactive (2.61%)
BRSK1	inactive (2.35%)
BRSK2	inactive (3.96%)
MELK	inactive (6.34%)
CHK1	inactive (5.14%)
PASK	inactive (0.76%)
AMPKa1	inactive (6.56%)
AMPKa2	inactive (4.4%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (3.75%)
TSSK1	inactive (5.87%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (6.03%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (1.27%)
PIM3	inactive (5.19%)
PIM1	inactive (1.97%)

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 (6.68%)
p38a	inactive (12.25%)
p38b	inactive (7.35%)
p38d	inactive (3.54%)
Erk2	inactive (5.62%)
Erk1	inactive (6.64%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (14.78%)
GSK3B	inactive (11.57%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (2.29%)
MSSK1	inactive (-0.94%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (2.8%)
CLK2	inactive (1.14%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (4.32%)
HIPK4	inactive (-0.47%)
DYRK1B	inactive (1.06%)
DYRK1A	inactive (6.39%)
DYRK2	inactive (5.04%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (8.99%)