Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : SB-358518

Inchikey : QOJSERWVVHZZPL-UHFFFAOYSA-N

ChemSpider : 5021953

Pubchem CID : 6539487

ChEMBL : CHEMBL352222

	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 (4.63%)
TYK2	inactive (2.74%)
JAK2	inactive (-0.7%)
JAK3	inactive (24.46%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (0.45%)
FES	inactive (0.99%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (0.82%)
ABL2	inactive (3.78%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (0.7%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (0.42%)
BTK	inactive (1.62%)
TXK	inactive (0.63%)
TEC	inactive (5.27%)
ITK	inactive (0.8%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (2.07%)
SRM	inactive (0.6%)
FRK	inactive (0.95%)
BLK	inactive (1.36%)
LCK	inactive (3.48%)
HCK	inactive (0.75%)
FGR	inactive (3.7%)
FYN	inactive (0.6%)
SRC	inactive (-0.12%)
YES	inactive (3.65%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (-0.45%)
EphA4	inactive (1.76%)
EphA3	inactive (1.24%)
EphB4	inactive (1.7%)
EphB3	inactive (3.06%)
EphB2	inactive (0.02%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (5.27%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-2.48%)
ZAP70	inactive (0.91%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (1.2%)
ALK	inactive (3.11%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (4.51%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (1.56%)
IGF1R	inactive (-0.5%)
IRR	inactive (0.1%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (1.09%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (-3.35%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (-0.43%)
TRKB	inactive (0.97%)
TRKC	inactive (1.33%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (0.58%)
MET	inactive (6.2%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (1.02%)
MER	inactive (0.18%)
TYRO3	inactive (1.3%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (3.36%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (7.05%)
FGFR2	inactive (21.66%)
FGFR3	inactive (14.53%)
FGFR4	inactive (0.22%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (1.09%)
KDR	inactive (8.59%)
FLT4	inactive (2.54%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (27.01%)
KIT	inactive (-0.5%)
FLT3	inactive (3.35%)
PDGFRa	inactive (4.4%)
PDGFRb	inactive (4.95%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (4.76%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (-0.08%)
TNK1	inactive (16.71%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (1.18%)
ErbB2	inactive (2.08%)
ErbB4	inactive (9.81%)

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 (0.63%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (3.75%)

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 (5.47%)
MST1	active (56.46%)
MST2	active (50.67%)
MST4	inactive (10.47%)
HGK	inactive (4.07%)
MINK	inactive (2.65%)
LOK	inactive (13.62%)
PAK1	inactive (-0.91%)
PAK3	inactive (0.99%)
PAK2	inactive (-1%)
PAK5	inactive (-2.87%)
PAK6	inactive (3.31%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (2.69%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (-0.13%)
CK1g2	inactive (1.13%)
CK1g1	inactive (1.75%)
CK1g3	inactive (2.61%)

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 (-1.62%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (3.34%)
AurC	inactive (6.2%)
AurA	inactive (7.69%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (1.19%)
NEK2	inactive (0.86%)
NEK9	inactive (4.74%)
NEK7	inactive (0.43%)
NEK6	inactive (1.08%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (47.44%)
IKKe	inactive (15.25%)
IKKb	inactive (4.99%)
IKKa	inactive (-1.55%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (3.3%)

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 (4.27%)
GPRK6	inactive (0.24%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (0.78%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (-1.6%)
MSK2	inactive (1.45%)
RSK1	inactive (3.34%)
RSK2	inactive (9.07%)
RSK4	inactive (11.19%)
RSK3	inactive (10.8%)
p70S6K	inactive (0.65%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (1.26%)
AKT1	inactive (0.14%)
AKT3	inactive (0.95%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (0.49%)
SGK3	inactive (1.23%)
SGK2	inactive (-0.94%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (1.81%)
PKCg	inactive (1.14%)
PKCa	inactive (1.77%)
PKCt	inactive (0.93%)
PKCi	inactive (-1.31%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (3.19%)
PKG1	inactive (1.99%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (2.86%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (-0.21%)
ROCK2	inactive (0.12%)
MRCKb	inactive (0.29%)
MRCKa	inactive (-0.25%)

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 (0.98%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (1.71%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (0.54%)
CaMK1d	inactive (0.37%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (4.24%)
PHKg2	inactive (2.81%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (1.23%)
CaMK2a	inactive (-0.51%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (0.55%)
MAPKAPK2	inactive (0.31%)
MAPKAPK3	inactive (1.9%)
MNK2	inactive (2.79%)
MNK1	inactive (3.09%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (3.53%)
PKD1	inactive (1.22%)
PKD2	inactive (2.21%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (6.06%)
MARK3	inactive (6.69%)
MARK1	inactive (6.27%)
QIK	inactive (5.17%)
SIK	inactive (3.71%)
NuaK1	inactive (13.69%)
BRSK1	inactive (4.78%)
BRSK2	inactive (3.68%)
MELK	inactive (-3.64%)
CHK1	inactive (1.06%)
PASK	inactive (1.32%)
AMPKa1	inactive (5.09%)
AMPKa2	inactive (4.91%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (0.2%)
TSSK1	inactive (0.86%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (1.81%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (1.61%)
PIM3	inactive (0.87%)
PIM1	inactive (1.59%)

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 (1.1%)
p38a	inactive (6.98%)
p38b	inactive (1.62%)
p38d	inactive (-0.48%)
Erk2	inactive (4.35%)
Erk1	inactive (2.24%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	active (85.02%)
GSK3B	active (80.72%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-1.65%)
MSSK1	inactive (-0.59%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (2.15%)
CLK2	inactive (12.52%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (-1.52%)
HIPK4	inactive (1.09%)
DYRK1B	inactive (10.52%)
DYRK1A	inactive (20.12%)
DYRK2	inactive (-1.6%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (-1.15%)