Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : SB-734117

Inchikey : JRYCXZUZWFHQPB-UHFFFAOYSA-N

ChemSpider : 23252939

Pubchem CID : 44397032

ChEMBL : CHEMBL189231

	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 (2.81%)
TYK2	inactive (6.77%)
JAK2	inactive (-0.41%)
JAK3	inactive (3.98%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (1.83%)
FES	inactive (-1.92%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (7.12%)
ABL2	inactive (3.74%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (-6.81%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (-1.58%)
BTK	inactive (-0.36%)
TXK	inactive (-0.03%)
TEC	inactive (1.22%)
ITK	inactive (0.48%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (-3%)
SRM	inactive (2.59%)
FRK	inactive (0.75%)
BLK	inactive (0.24%)
LCK	inactive (0.51%)
HCK	inactive (0.66%)
FGR	inactive (6.63%)
FYN	inactive (4.39%)
SRC	inactive (-1.17%)
YES	inactive (3.33%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (-4.85%)
EphA4	inactive (-3.51%)
EphA3	inactive (-1.98%)
EphB4	inactive (-1.63%)
EphB3	inactive (-4.08%)
EphB2	inactive (-8.8%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (-8.39%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-0.01%)
ZAP70	inactive (-0.79%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (2.35%)
ALK	inactive (2.16%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (35.9%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (-0.22%)
IGF1R	inactive (-0.98%)
IRR	inactive (-3.62%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (1.77%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (3.94%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (-1.13%)
TRKB	inactive (-0.84%)
TRKC	inactive (0.67%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (-1.49%)
MET	inactive (7.05%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (4.86%)
MER	inactive (1.5%)
TYRO3	inactive (-0.87%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (9.55%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (-4.22%)
FGFR2	inactive (-0.47%)
FGFR3	inactive (-2.23%)
FGFR4	inactive (-1.15%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (4.33%)
KDR	inactive (46.33%)
FLT4	inactive (16.74%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	active (76.31%)
KIT	inactive (20.62%)
FLT3	inactive (4.32%)
PDGFRa	inactive (18.15%)
PDGFRb	inactive (26.44%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (3.18%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (-1.55%)
TNK1	inactive (20.8%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (7.55%)
ErbB2	inactive (-1.33%)
ErbB4	inactive (-5.19%)

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 (-1.3%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (4.56%)

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 (20.37%)
MST1	inactive (18.46%)
MST2	inactive (13.84%)
MST4	inactive (3.95%)
HGK	inactive (46.22%)
MINK	inactive (31.35%)
LOK	inactive (18.35%)
PAK1	inactive (-1.25%)
PAK3	inactive (-2.19%)
PAK2	inactive (-1.54%)
PAK5	inactive (-4.63%)
PAK6	inactive (-4.16%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (7.67%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (-0.02%)
CK1g2	inactive (0.45%)
CK1g1	inactive (-0.45%)
CK1g3	inactive (1.85%)

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 (-0.5%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (7.52%)
AurC	inactive (5.22%)
AurA	inactive (5.79%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (0.56%)
NEK2	inactive (-7.26%)
NEK9	inactive (-2.86%)
NEK7	inactive (-0.97%)
NEK6	inactive (-0.88%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (24.77%)
IKKe	inactive (16.19%)
IKKb	inactive (-5.78%)
IKKa	inactive (-2.66%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (4.51%)

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 (2.63%)
GPRK6	inactive (2.07%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (5.36%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	active (85.16%)
MSK2	active (82.97%)
RSK1	active (86.39%)
RSK2	active (81.43%)
RSK4	inactive (30.95%)
RSK3	active (92.64%)
p70S6K	active (91.2%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (22.41%)
AKT1	inactive (37.35%)
AKT3	inactive (32.28%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (13.15%)
SGK3	inactive (41.73%)
SGK2	inactive (40.52%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	active (88.46%)
PKCg	inactive (49.01%)
PKCa	inactive (38.38%)
PKCt	active (55.2%)
PKCi	inactive (4.76%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	active (80.92%)
PKG1	active (61.23%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (21.69%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	active (78.44%)
ROCK2	active (83.39%)
MRCKb	active (72.04%)
MRCKa	active (65.92%)

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 (-1.47%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (1.52%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (1.19%)
CaMK1d	inactive (1.22%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (8.25%)
PHKg2	inactive (-2.24%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (4.05%)
CaMK2a	inactive (0.68%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (-1.13%)
MAPKAPK2	inactive (-1.08%)
MAPKAPK3	inactive (-2.76%)
MNK2	inactive (8.42%)
MNK1	inactive (4.63%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (2.27%)
PKD1	inactive (2.75%)
PKD2	inactive (4.59%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (10.83%)
MARK3	inactive (24.22%)
MARK1	inactive (16.53%)
QIK	inactive (9.23%)
SIK	inactive (-3.76%)
NuaK1	inactive (6.7%)
BRSK1	inactive (4.25%)
BRSK2	inactive (6.14%)
MELK	active (74.62%)
CHK1	inactive (1.88%)
PASK	inactive (12.89%)
AMPKa1	inactive (5.36%)
AMPKa2	inactive (3.46%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (-2.07%)
TSSK1	inactive (6.12%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (-1.97%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (37.5%)
PIM3	active (56.9%)
PIM1	active (79.15%)

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 (-0.67%)
p38a	inactive (-3.77%)
p38b	inactive (0.28%)
p38d	inactive (1.87%)
Erk2	inactive (1.38%)
Erk1	inactive (2.55%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	active (90.76%)
GSK3B	active (90.05%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-0.52%)
MSSK1	inactive (-1.01%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (2.98%)
CLK2	inactive (39.17%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (16.06%)
HIPK4	inactive (10.28%)
DYRK1B	active (71.24%)
DYRK1A	active (78.01%)
DYRK2	inactive (-0.12%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (4.16%)