Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : SB-725317

Inchikey : VNVKSDCWJDOWNE-UHFFFAOYSA-N

ChemSpider : 23317380

Pubchem CID : 135435011

ChEMBL : CHEMBL260417

	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	active (54.95%)
TYK2	inactive (17.63%)
JAK2	inactive (28.44%)
JAK3	active (62.18%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (7.42%)
FES	inactive (3.83%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	active (72.6%)
ABL2	inactive (25.73%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (10.89%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (13.41%)
BTK	inactive (0.5%)
TXK	inactive (9.15%)
TEC	inactive (14.43%)
ITK	inactive (3.5%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (11.05%)
SRM	inactive (17.01%)
FRK	inactive (2.41%)
BLK	inactive (15.37%)
LCK	inactive (22.24%)
HCK	inactive (28.45%)
FGR	inactive (21.28%)
FYN	inactive (14.52%)
SRC	inactive (20.27%)
YES	inactive (27.44%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (24.22%)
EphA4	inactive (39.2%)
EphA3	inactive (13.98%)
EphB4	inactive (28.76%)
EphB3	inactive (5.92%)
EphB2	inactive (37.78%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (18.51%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (0.18%)
ZAP70	inactive (4.28%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	active (91.56%)
ALK	active (72.32%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (11.1%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (6.22%)
IGF1R	inactive (5.83%)
IRR	inactive (1.59%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (4.12%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (14.01%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (12.31%)
TRKB	inactive (14.5%)
TRKC	inactive (16.37%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (6.19%)
MET	inactive (10.9%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-7.01%)
MER	inactive (8.16%)
TYRO3	inactive (41.4%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (28.09%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (21.36%)
FGFR2	inactive (17.92%)
FGFR3	inactive (12.52%)
FGFR4	inactive (3.05%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (17.73%)
KDR	active (71.59%)
FLT4	active (60.87%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (6.92%)
KIT	active (63.08%)
FLT3	inactive (25.72%)
PDGFRa	active (67.09%)
PDGFRb	inactive (41.31%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (26.21%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (3.9%)
TNK1	inactive (20.35%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (6.97%)
ErbB2	inactive (4.82%)
ErbB4	inactive (21.98%)

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 (3.24%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (12.57%)

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 (34.44%)
MST1	inactive (10.17%)
MST2	inactive (10.62%)
MST4	inactive (35.03%)
HGK	active (75.24%)
MINK	active (67.71%)
LOK	active (61.34%)
PAK1	inactive (8.21%)
PAK3	inactive (6.07%)
PAK2	inactive (3.87%)
PAK5	inactive (8.52%)
PAK6	inactive (8.5%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (8.1%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (5.83%)
CK1g2	inactive (7.38%)
CK1g1	inactive (5.67%)
CK1g3	inactive (4.72%)

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 (5.59%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (12.72%)
AurC	inactive (8.73%)
AurA	inactive (37.69%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (11.22%)
NEK2	inactive (9%)
NEK9	inactive (13.17%)
NEK7	inactive (46.3%)
NEK6	inactive (15.25%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (22.56%)
IKKe	inactive (12.16%)
IKKb	inactive (9.61%)
IKKa	inactive (12.44%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (15.3%)

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 (17.41%)
GPRK6	inactive (32.61%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (14.59%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (13.64%)
MSK2	inactive (6.3%)
RSK1	inactive (32.95%)
RSK2	inactive (44.75%)
RSK4	active (59.73%)
RSK3	active (70.56%)
p70S6K	inactive (6.85%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (3.12%)
AKT1	inactive (2.07%)
AKT3	inactive (12.54%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (12.14%)
SGK3	inactive (16.7%)
SGK2	inactive (24.79%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (12.91%)
PKCg	inactive (48.06%)
PKCa	inactive (36.94%)
PKCt	inactive (33.19%)
PKCi	inactive (19.23%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (27.79%)
PKG1	inactive (6.22%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (4.28%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (1.33%)
ROCK2	inactive (6.43%)
MRCKb	inactive (15.5%)
MRCKa	inactive (13.49%)

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 (4.23%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (3.55%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (2.12%)
CaMK1d	inactive (14.43%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (10.67%)
PHKg2	inactive (7.34%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (20.15%)
CaMK2a	inactive (8.39%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (3.04%)
MAPKAPK2	inactive (2.69%)
MAPKAPK3	inactive (5.6%)
MNK2	inactive (35.13%)
MNK1	active (76.07%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (6.49%)
PKD1	inactive (7.7%)
PKD2	inactive (5.92%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (4.75%)
MARK3	inactive (8.75%)
MARK1	inactive (9.58%)
QIK	inactive (19.91%)
SIK	inactive (17.05%)
NuaK1	inactive (30.24%)
BRSK1	active (66.76%)
BRSK2	active (70.19%)
MELK	inactive (13.11%)
CHK1	inactive (16.8%)
PASK	inactive (0.71%)
AMPKa1	inactive (20.07%)
AMPKa2	inactive (12.08%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (4.53%)
TSSK1	inactive (5.96%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (3.27%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	active (75.22%)
PIM3	active (73.86%)
PIM1	active (65.54%)

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 (19.39%)
p38a	inactive (16%)
p38b	inactive (38.76%)
p38d	inactive (32.59%)
Erk2	inactive (10.06%)
Erk1	inactive (5.57%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	active (85.68%)
GSK3B	active (83.12%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (0.36%)
MSSK1	inactive (7.81%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (8.39%)
CLK2	inactive (5.65%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	active (57.99%)
HIPK4	inactive (10.45%)
DYRK1B	active (71.74%)
DYRK1A	active (55.48%)
DYRK2	active (53.33%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (5.84%)