Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW450241X

Inchikey : NLOKJGFIQFVGNZ-MDZDMXLPSA-N

ChemSpider : 23278136

Pubchem CID : 44418546

ChEMBL : CHEMBL385426

	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 (-10.06%)
TYK2	inactive (-3.91%)
JAK2	inactive (1.71%)
JAK3	inactive (0.86%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (1.64%)
FES	inactive (2.33%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (45.85%)
ABL2	inactive (12.91%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (0.54%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (4.87%)
BTK	inactive (2.98%)
TXK	inactive (8.4%)
TEC	inactive (7.25%)
ITK	inactive (2.29%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (3.98%)
SRM	inactive (-0.17%)
FRK	inactive (2.05%)
BLK	inactive (4.46%)
LCK	inactive (4.94%)
HCK	inactive (10.03%)
FGR	inactive (11.65%)
FYN	inactive (3.44%)
SRC	inactive (10.25%)
YES	inactive (-1.48%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (2.3%)
EphA4	inactive (5.6%)
EphA3	inactive (2.85%)
EphB4	inactive (1.84%)
EphB3	inactive (2.63%)
EphB2	inactive (11.11%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (5.62%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-0.49%)
ZAP70	inactive (0.77%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (0.4%)
ALK	inactive (4.03%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (4.93%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (1.65%)
IGF1R	inactive (3.86%)
IRR	inactive (2.06%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (6.62%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (0.76%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (1.65%)
TRKB	inactive (3.79%)
TRKC	inactive (3.49%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (6%)
MET	inactive (1.69%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-1.28%)
MER	inactive (4.08%)
TYRO3	inactive (2.78%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (7.18%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (11.78%)
FGFR2	inactive (9.23%)
FGFR3	inactive (9.45%)
FGFR4	inactive (0.35%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (2.13%)
KDR	inactive (8.91%)
FLT4	inactive (2.42%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (6.91%)
KIT	inactive (0.22%)
FLT3	inactive (4.49%)
PDGFRa	inactive (7.82%)
PDGFRb	inactive (9.24%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (3.17%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (2.37%)
TNK1	inactive (10.21%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (6.32%)
ErbB2	inactive (-1.35%)
ErbB4	inactive (14.13%)

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 (1.51%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (2.6%)

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 (0.32%)
MST1	inactive (5.19%)
MST2	inactive (3.95%)
MST4	inactive (-4.27%)
HGK	inactive (7.49%)
MINK	inactive (6.06%)
LOK	inactive (5.08%)
PAK1	inactive (2.08%)
PAK3	inactive (3.43%)
PAK2	inactive (1.76%)
PAK5	inactive (-1.06%)
PAK6	inactive (11.52%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (2.68%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (6.21%)
CK1g2	inactive (5.11%)
CK1g1	inactive (5.44%)
CK1g3	inactive (4.99%)

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 (1.99%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (6.73%)
AurC	inactive (11.66%)
AurA	inactive (6.42%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (1.92%)
NEK2	inactive (3.05%)
NEK9	inactive (-1.94%)
NEK7	inactive (2.39%)
NEK6	inactive (0.68%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (1.52%)
IKKe	inactive (3.78%)
IKKb	inactive (2.91%)
IKKa	inactive (-5.51%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (-0.69%)

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 (-8.54%)
GPRK6	inactive (-0.96%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (0.35%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (2.79%)
MSK2	inactive (2.52%)
RSK1	inactive (0.95%)
RSK2	inactive (-0.37%)
RSK4	inactive (1.72%)
RSK3	inactive (0.74%)
p70S6K	inactive (0.41%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (1.3%)
AKT1	inactive (0.8%)
AKT3	inactive (1.32%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (-0.86%)
SGK3	inactive (0.72%)
SGK2	inactive (-2.52%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (-0.26%)
PKCg	inactive (2.81%)
PKCa	inactive (3.13%)
PKCt	inactive (-0.25%)
PKCi	inactive (3.47%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (1.83%)
PKG1	inactive (2.71%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (-1.34%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (1.22%)
ROCK2	inactive (-0.13%)
MRCKb	inactive (1.46%)
MRCKa	inactive (0.07%)

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 (1.85%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (1.19%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (13.93%)
CaMK1d	inactive (1.99%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (3.16%)
PHKg2	inactive (0.53%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (2.2%)
CaMK2a	inactive (3.51%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (-0.1%)
MAPKAPK2	inactive (0.99%)
MAPKAPK3	inactive (3.44%)
MNK2	inactive (1.79%)
MNK1	inactive (3.27%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (7.02%)
PKD1	inactive (6.44%)
PKD2	inactive (7.18%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (1.03%)
MARK3	inactive (0.43%)
MARK1	inactive (1.27%)
QIK	inactive (-1.33%)
SIK	inactive (6.26%)
NuaK1	inactive (6.57%)
BRSK1	inactive (0.96%)
BRSK2	inactive (0.3%)
MELK	inactive (3.83%)
CHK1	inactive (2.13%)
PASK	inactive (-0.71%)
AMPKa1	inactive (1.48%)
AMPKa2	inactive (2.36%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (-3.19%)
TSSK1	inactive (0.1%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (4.2%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (-0.07%)
PIM3	inactive (-2.15%)
PIM1	inactive (1.26%)

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 (7.37%)
p38a	inactive (8.94%)
p38b	inactive (4.99%)
p38d	inactive (4.25%)
Erk2	inactive (1%)
Erk1	inactive (1.29%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (6.98%)
GSK3B	inactive (7.96%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-2.98%)
MSSK1	inactive (0.49%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (1.66%)
CLK2	inactive (3.8%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (7.03%)
HIPK4	inactive (4.82%)
DYRK1B	inactive (3.49%)
DYRK1A	inactive (5.03%)
DYRK2	inactive (2.5%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (-1.26%)