Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : SB-739452

Inchikey : GVYKLTFFLMMUEN-UHFFFAOYSA-N

ChemSpider : 5022077

Pubchem CID : 6539611

ChEMBL : CHEMBL408564

	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 (-1.14%)
TYK2	inactive (-1.51%)
JAK2	inactive (1.59%)
JAK3	inactive (1.18%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (0.63%)
FES	inactive (3.27%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (24.15%)
ABL2	inactive (18.39%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (4.14%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (4.58%)
BTK	inactive (4.11%)
TXK	inactive (5.55%)
TEC	inactive (9.1%)
ITK	inactive (23.67%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (3.67%)
SRM	inactive (-0.3%)
FRK	inactive (4.35%)
BLK	inactive (20.52%)
LCK	inactive (6.71%)
HCK	inactive (9.03%)
FGR	inactive (11.35%)
FYN	inactive (1.8%)
SRC	inactive (14.25%)
YES	inactive (13.75%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (1.29%)
EphA4	inactive (2.95%)
EphA3	inactive (4.24%)
EphB4	inactive (3.48%)
EphB3	inactive (3.95%)
EphB2	inactive (5.48%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (3.71%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-0.45%)
ZAP70	inactive (3.08%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (0.72%)
ALK	inactive (4.4%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (3.03%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (-14.07%)
IGF1R	inactive (3.89%)
IRR	inactive (1.49%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (2.85%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (6.32%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (3.72%)
TRKB	inactive (1.56%)
TRKC	inactive (4.33%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (4.05%)
MET	inactive (6.65%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-1.16%)
MER	inactive (4.5%)
TYRO3	inactive (4.49%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (4.7%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (5.28%)
FGFR2	inactive (7.9%)
FGFR3	inactive (7.26%)
FGFR4	inactive (2.76%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (4.22%)
KDR	inactive (15.46%)
FLT4	inactive (9.43%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (1.78%)
KIT	inactive (4.71%)
FLT3	inactive (2.62%)
PDGFRa	inactive (12.94%)
PDGFRb	inactive (6.81%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (13.68%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (0.24%)
TNK1	inactive (-0.4%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (5.12%)
ErbB2	inactive (-3.9%)
ErbB4	inactive (15.78%)

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 (1.08%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (5.7%)

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 (2.51%)
MST1	inactive (4%)
MST2	inactive (5.58%)
MST4	inactive (-2.34%)
HGK	inactive (8.55%)
MINK	inactive (8.29%)
LOK	inactive (11.31%)
PAK1	inactive (6.66%)
PAK3	inactive (3.54%)
PAK2	inactive (3.61%)
PAK5	inactive (-1.99%)
PAK6	inactive (0.72%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (3.63%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (3.16%)
CK1g2	inactive (2.51%)
CK1g1	inactive (2.78%)
CK1g3	inactive (0.87%)

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 (4.35%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (14.49%)
AurC	inactive (29.38%)
AurA	inactive (45.56%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (1.85%)
NEK2	inactive (3.85%)
NEK9	inactive (3.52%)
NEK7	inactive (3.03%)
NEK6	inactive (0.56%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (4.8%)
IKKe	inactive (3.64%)
IKKb	inactive (2.38%)
IKKa	inactive (-2.15%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (-3.66%)

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 (4.09%)
GPRK6	inactive (-0.55%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (2.43%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (1.89%)
MSK2	inactive (2.64%)
RSK1	inactive (-0.1%)
RSK2	inactive (-0.3%)
RSK4	inactive (2.56%)
RSK3	inactive (2.85%)
p70S6K	inactive (2.07%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (2.15%)
AKT1	inactive (0.53%)
AKT3	inactive (1.46%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (3.09%)
SGK3	inactive (3.45%)
SGK2	inactive (-4.73%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (2.72%)
PKCg	inactive (3.32%)
PKCa	inactive (0.28%)
PKCt	inactive (0.79%)
PKCi	inactive (2.37%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (1.85%)
PKG1	inactive (3.36%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (-0.27%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (0.97%)
ROCK2	inactive (-0.88%)
MRCKb	inactive (0.57%)
MRCKa	inactive (-0.6%)

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 (2.71%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (1.73%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (2.02%)
CaMK1d	inactive (1.36%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (2.36%)
PHKg2	inactive (1.34%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (4.6%)
CaMK2a	inactive (2.92%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (0.07%)
MAPKAPK2	inactive (1.26%)
MAPKAPK3	inactive (3.6%)
MNK2	inactive (1.34%)
MNK1	inactive (13.86%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (4.81%)
PKD1	inactive (5.78%)
PKD2	inactive (5.03%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (2.43%)
MARK3	inactive (-5.02%)
MARK1	inactive (2.7%)
QIK	inactive (5%)
SIK	inactive (5.66%)
NuaK1	inactive (4.11%)
BRSK1	inactive (12.86%)
BRSK2	inactive (11.46%)
MELK	inactive (7.3%)
CHK1	inactive (4.35%)
PASK	inactive (-1.87%)
AMPKa1	inactive (3.4%)
AMPKa2	inactive (5.5%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (-1.08%)
TSSK1	inactive (1.5%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (4.49%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (0.42%)
PIM3	inactive (-2.95%)
PIM1	inactive (0.54%)

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 (3.7%)
p38a	inactive (6.49%)
p38b	inactive (3.71%)
p38d	inactive (2.57%)
Erk2	inactive (5.13%)
Erk1	inactive (2.64%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	active (80.64%)
GSK3B	active (65.65%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-5.19%)
MSSK1	inactive (-0.41%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (2.72%)
CLK2	inactive (2.79%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (3.67%)
HIPK4	inactive (2.1%)
DYRK1B	inactive (3.25%)
DYRK1A	inactive (4.33%)
DYRK2	inactive (4.31%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (-1.87%)