Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GSK614526A

Inchikey : QQQGLCMEJYJOMK-YDALLXLXSA-N

ChemSpider : 28484519

Pubchem CID : 56603966

ChEMBL : CHEMBL1909375

	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 (2.18%)
TYK2	inactive (-1.89%)
JAK2	inactive (-2.12%)
JAK3	inactive (0.33%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (0.7%)
FES	inactive (4.12%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (-0.45%)
ABL2	inactive (2.28%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (-0.82%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (-0.7%)
BTK	inactive (1.17%)
TXK	inactive (1.67%)
TEC	inactive (1.67%)
ITK	inactive (0.41%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (2.47%)
SRM	inactive (0.87%)
FRK	inactive (0.68%)
BLK	inactive (1.76%)
LCK	inactive (3.66%)
HCK	inactive (1%)
FGR	inactive (2.16%)
FYN	inactive (1.07%)
SRC	inactive (-2.58%)
YES	inactive (2.07%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (0.02%)
EphA4	inactive (2.58%)
EphA3	inactive (-1.12%)
EphB4	inactive (1.1%)
EphB3	inactive (0.62%)
EphB2	inactive (-3.01%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (22.98%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-4.11%)
ZAP70	inactive (-0.24%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (2.22%)
ALK	inactive (1.45%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (0.45%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (-1.35%)
IGF1R	inactive (0.19%)
IRR	inactive (-0.44%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (2.67%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (-3.74%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (-3.52%)
TRKB	inactive (0.79%)
TRKC	inactive (-0.37%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (-2.78%)
MET	inactive (5.81%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (0.17%)
MER	inactive (-0.43%)
TYRO3	inactive (1.75%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (25.17%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (0.08%)
FGFR2	inactive (0.8%)
FGFR3	inactive (0.67%)
FGFR4	inactive (2.23%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (17.37%)
KDR	active (81.33%)
FLT4	inactive (33.92%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (1.4%)
KIT	inactive (-2.57%)
FLT3	inactive (-0.61%)
PDGFRa	inactive (24.37%)
PDGFRb	inactive (47.2%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (4.39%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (-0.46%)
TNK1	inactive (1.67%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (1.8%)
ErbB2	inactive (3.51%)
ErbB4	inactive (7.9%)

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 (0.53%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (0.01%)

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 (3.31%)
MST1	inactive (2.14%)
MST2	inactive (2.41%)
MST4	inactive (-0.64%)
HGK	inactive (2.54%)
MINK	inactive (0.93%)
LOK	inactive (5.64%)
PAK1	inactive (7.58%)
PAK3	inactive (4.06%)
PAK2	inactive (16.59%)
PAK5	inactive (49.77%)
PAK6	active (58.43%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (0.19%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (-2.58%)
CK1g2	inactive (2.18%)
CK1g1	inactive (2.69%)
CK1g3	inactive (3.35%)

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 (-3.86%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (0.87%)
AurC	inactive (1.45%)
AurA	inactive (1.08%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (0.55%)
NEK2	inactive (0.91%)
NEK9	inactive (0.02%)
NEK7	inactive (-0.58%)
NEK6	inactive (0.79%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (41.18%)
IKKe	active (98.7%)
IKKb	inactive (4.4%)
IKKa	inactive (-0.05%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (4.1%)

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 (14.01%)
GPRK6	inactive (0.91%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (4.72%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (7.89%)
MSK2	inactive (17.49%)
RSK1	inactive (23.27%)
RSK2	inactive (24.88%)
RSK4	inactive (8.09%)
RSK3	inactive (13.28%)
p70S6K	inactive (25.38%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	-
AKT1	active (91.12%)
AKT3	active (90.43%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (2.09%)
SGK3	inactive (47.44%)
SGK2	inactive (2.29%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	active (96.35%)
PKCg	inactive (44.59%)
PKCa	inactive (18.35%)
PKCt	active (72.29%)
PKCi	inactive (11.39%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	active (76.49%)
PKG1	active (76.38%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	active (85.38%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (12.39%)
ROCK2	inactive (10.04%)
MRCKb	inactive (19.53%)
MRCKa	inactive (23.52%)

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 (1.08%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (2.93%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-0.65%)
CaMK1d	inactive (0.84%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (2.21%)
PHKg2	inactive (1.65%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (0.35%)
CaMK2a	inactive (-2.05%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (0.32%)
MAPKAPK2	inactive (-0.71%)
MAPKAPK3	inactive (-0.82%)
MNK2	inactive (-0.07%)
MNK1	inactive (1.82%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (15.88%)
PKD1	inactive (19.2%)
PKD2	inactive (12.62%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	active (55.16%)
MARK3	active (67.86%)
MARK1	active (61.09%)
QIK	inactive (6.59%)
SIK	inactive (4.19%)
NuaK1	inactive (34.39%)
BRSK1	inactive (1.83%)
BRSK2	inactive (1.11%)
MELK	inactive (18.39%)
CHK1	inactive (2.95%)
PASK	inactive (7.61%)
AMPKa1	inactive (39.34%)
AMPKa2	inactive (4.25%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (2.67%)
TSSK1	active (70.38%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (0.89%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (7.09%)
PIM3	inactive (10.11%)
PIM1	inactive (7.63%)

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 (0.92%)
p38a	inactive (0.75%)
p38b	inactive (1.41%)
p38d	inactive (-1.56%)
Erk2	inactive (1.3%)
Erk1	inactive (2.32%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (44.41%)
GSK3B	inactive (46.85%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-2.53%)
MSSK1	inactive (-4.41%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (-0.53%)
CLK2	inactive (9.59%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (6.03%)
HIPK4	inactive (0.31%)
DYRK1B	inactive (-1.07%)
DYRK1A	inactive (-0.73%)
DYRK2	inactive (-2.07%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (-1.67%)