Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GSK953913A

Inchikey : KKMQKOWAGAPQDL-UHFFFAOYSA-N

ChemSpider : 24701292

Pubchem CID : 42618164

ChEMBL : CHEMBL483748

	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 (10.02%)
TYK2	inactive (-0.94%)
JAK2	inactive (3.23%)
JAK3	inactive (-1.27%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (8.24%)
FES	inactive (4.62%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (7.38%)
ABL2	inactive (6.27%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (5.2%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (4.75%)
BTK	inactive (-0.08%)
TXK	inactive (1.28%)
TEC	inactive (4.44%)
ITK	inactive (0.35%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (5.54%)
SRM	inactive (1.62%)
FRK	inactive (1.07%)
BLK	inactive (3.91%)
LCK	inactive (3.87%)
HCK	inactive (6.46%)
FGR	inactive (4.64%)
FYN	inactive (3.52%)
SRC	inactive (6.83%)
YES	inactive (3.16%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (0.7%)
EphA4	inactive (10.44%)
EphA3	inactive (3.77%)
EphB4	inactive (2.91%)
EphB3	inactive (3.29%)
EphB2	inactive (12.56%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (13.43%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (0.64%)
ZAP70	inactive (-0.77%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (14.78%)
ALK	inactive (15.51%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (10.98%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (5.38%)
IGF1R	inactive (2.17%)
IRR	inactive (2.61%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (2.48%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (0.07%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (0.22%)
TRKB	inactive (2.46%)
TRKC	inactive (5.04%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (8.77%)
MET	inactive (5.85%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-1.13%)
MER	inactive (1.77%)
TYRO3	inactive (4.23%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (8.69%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (3.35%)
FGFR2	inactive (3.78%)
FGFR3	inactive (2.76%)
FGFR4	inactive (4.68%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (2.57%)
KDR	inactive (8.11%)
FLT4	inactive (1.58%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (1.76%)
KIT	inactive (8.06%)
FLT3	inactive (2.5%)
PDGFRa	inactive (13.22%)
PDGFRb	inactive (8.53%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (3.06%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (2.21%)
TNK1	inactive (16.02%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (2.78%)
ErbB2	inactive (3.62%)
ErbB4	inactive (8.97%)

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 (1.31%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (6.35%)

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 (2.03%)
MST1	inactive (7.76%)
MST2	inactive (5.97%)
MST4	inactive (0.38%)
HGK	inactive (6.71%)
MINK	inactive (5.92%)
LOK	inactive (9.35%)
PAK1	inactive (6.13%)
PAK3	inactive (4.21%)
PAK2	inactive (0.46%)
PAK5	inactive (-3.7%)
PAK6	inactive (4.76%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (3.72%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (3.35%)
CK1g2	inactive (3.43%)
CK1g1	inactive (3.44%)
CK1g3	inactive (4.76%)

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 (1.7%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (4.42%)
AurC	inactive (-6.92%)
AurA	inactive (7.25%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (2.44%)
NEK2	inactive (3.04%)
NEK9	inactive (7.84%)
NEK7	inactive (4.88%)
NEK6	inactive (3.3%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (2.74%)
IKKe	inactive (2.21%)
IKKb	inactive (21.89%)
IKKa	inactive (8.71%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (9.25%)

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 (6.27%)
GPRK6	inactive (8.2%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (2.39%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (0.96%)
MSK2	inactive (2.64%)
RSK1	inactive (3.06%)
RSK2	inactive (0.92%)
RSK4	inactive (0.34%)
RSK3	inactive (2.19%)
p70S6K	inactive (2.04%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (1.66%)
AKT1	inactive (0.83%)
AKT3	inactive (2.2%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (2.69%)
SGK3	inactive (2.72%)
SGK2	inactive (-1.22%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (3.62%)
PKCg	inactive (4.49%)
PKCa	inactive (1.77%)
PKCt	inactive (2.98%)
PKCi	inactive (0.28%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (3.35%)
PKG1	inactive (4.78%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (1.52%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (4.04%)
ROCK2	inactive (6.37%)
MRCKb	inactive (-2.27%)
MRCKa	inactive (-1.1%)

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 (4.7%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (3.41%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (2.15%)
CaMK1d	inactive (0.65%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (8.39%)
PHKg2	inactive (5.11%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (4.59%)
CaMK2a	inactive (2.94%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (1.86%)
MAPKAPK2	inactive (1.1%)
MAPKAPK3	inactive (6.72%)
MNK2	inactive (26.43%)
MNK1	inactive (17.67%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (2.51%)
PKD1	inactive (2.75%)
PKD2	inactive (4.54%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (1.99%)
MARK3	inactive (0.1%)
MARK1	inactive (3.63%)
QIK	inactive (4.1%)
SIK	inactive (10.31%)
NuaK1	inactive (-0.08%)
BRSK1	inactive (0.47%)
BRSK2	inactive (2.69%)
MELK	inactive (3.87%)
CHK1	inactive (0.12%)
PASK	inactive (0.09%)
AMPKa1	inactive (3.15%)
AMPKa2	inactive (2.32%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (2.52%)
TSSK1	inactive (3.97%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (1.02%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (-1.33%)
PIM3	inactive (1.38%)
PIM1	inactive (0.86%)

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 (6.21%)
p38a	inactive (8.35%)
p38b	inactive (6.57%)
p38d	inactive (3.8%)
Erk2	inactive (3.37%)
Erk1	inactive (3.1%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (4.95%)
GSK3B	inactive (3.98%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (0.04%)
MSSK1	inactive (3.53%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (3.69%)
CLK2	inactive (2.04%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (4.62%)
HIPK4	inactive (6.62%)
DYRK1B	inactive (2.12%)
DYRK1A	inactive (4.84%)
DYRK2	inactive (3.11%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (12.58%)