Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GSK619487A

Inchikey : KKMDOYLDYOJWIA-UHFFFAOYSA-N

ChemSpider : 26639423

Pubchem CID : 56604013

ChEMBL : CHEMBL1794066

	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 (3.51%)
TYK2	inactive (-1.36%)
JAK2	inactive (2.39%)
JAK3	inactive (-1.24%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (3.91%)
FES	inactive (5.88%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (3.17%)
ABL2	inactive (3.67%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (1.26%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (7.52%)
BTK	inactive (0.56%)
TXK	inactive (3.86%)
TEC	inactive (3.33%)
ITK	inactive (2.09%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (1.62%)
SRM	inactive (1.37%)
FRK	inactive (2.25%)
BLK	inactive (3.31%)
LCK	inactive (4.05%)
HCK	inactive (7.03%)
FGR	inactive (4.57%)
FYN	inactive (5.91%)
SRC	inactive (11.44%)
YES	inactive (5.89%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (0.34%)
EphA4	inactive (6.59%)
EphA3	inactive (3.69%)
EphB4	inactive (1.63%)
EphB3	inactive (4.06%)
EphB2	inactive (4.11%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (45.29%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (1.12%)
ZAP70	inactive (1.77%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (3.06%)
ALK	inactive (4.92%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (6.9%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (3.32%)
IGF1R	inactive (2.36%)
IRR	inactive (2.07%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (1.03%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (5.05%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (3.24%)
TRKB	inactive (1.02%)
TRKC	inactive (-0.14%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (0.48%)
MET	inactive (-3.51%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-4.23%)
MER	inactive (2.19%)
TYRO3	inactive (2.44%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (10.34%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (-4.66%)
FGFR2	inactive (11.4%)
FGFR3	inactive (2.73%)
FGFR4	inactive (-1.22%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (16.38%)
KDR	active (76.06%)
FLT4	inactive (26.57%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (2.92%)
KIT	inactive (3.87%)
FLT3	inactive (3.82%)
PDGFRa	inactive (19.49%)
PDGFRb	inactive (41.1%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (7.95%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (1.17%)
TNK1	inactive (0.26%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (3.18%)
ErbB2	inactive (3.93%)
ErbB4	inactive (10.34%)

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 (1.93%)

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 (3.12%)
MST1	inactive (4.54%)
MST2	inactive (6.04%)
MST4	inactive (4.19%)
HGK	inactive (6.21%)
MINK	inactive (5.83%)
LOK	inactive (11.25%)
PAK1	inactive (8.91%)
PAK3	inactive (8.39%)
PAK2	inactive (13.47%)
PAK5	active (80.08%)
PAK6	active (76.03%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (3.44%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (8.85%)
CK1g2	inactive (3.98%)
CK1g1	inactive (4.65%)
CK1g3	inactive (3.15%)

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%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (1.85%)
AurC	inactive (3.1%)
AurA	inactive (0.96%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (2.37%)
NEK2	inactive (2.51%)
NEK9	inactive (5.22%)
NEK7	inactive (5.15%)
NEK6	inactive (1.86%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (45.91%)
IKKe	active (95.78%)
IKKb	inactive (5.45%)
IKKa	inactive (0.96%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (7.59%)

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 (17.03%)
GPRK6	inactive (7.13%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (7.71%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (11.82%)
MSK2	inactive (14.91%)
RSK1	inactive (12.27%)
RSK2	inactive (14.35%)
RSK4	inactive (5.51%)
RSK3	inactive (5.77%)
p70S6K	inactive (26.54%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	active (95.45%)
AKT1	active (92.77%)
AKT3	active (94.18%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (4.36%)
SGK3	active (53.44%)
SGK2	inactive (16.44%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	active (99.9%)
PKCg	active (89.55%)
PKCa	inactive (30.38%)
PKCt	active (81.46%)
PKCi	inactive (6.53%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	active (83.21%)
PKG1	active (77.36%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	active (89.04%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (24.31%)
ROCK2	inactive (22.58%)
MRCKb	inactive (22.46%)
MRCKa	inactive (33.76%)

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 (7.53%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (3.29%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (6.84%)
CaMK1d	inactive (8.97%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (3.09%)
PHKg2	inactive (3.58%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (8.15%)
CaMK2a	inactive (5.73%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (1.22%)
MAPKAPK2	inactive (3.78%)
MAPKAPK3	inactive (4.41%)
MNK2	inactive (2.87%)
MNK1	inactive (2.25%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (14.17%)
PKD1	inactive (13.38%)
PKD2	inactive (11.14%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	active (62.08%)
MARK3	active (77.68%)
MARK1	active (74.1%)
QIK	inactive (14.8%)
SIK	inactive (10.55%)
NuaK1	inactive (42.94%)
BRSK1	inactive (10.48%)
BRSK2	inactive (19.25%)
MELK	active (76.43%)
CHK1	inactive (4.29%)
PASK	inactive (13.11%)
AMPKa1	active (82.6%)
AMPKa2	inactive (43.27%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (2.99%)
TSSK1	active (71.44%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (5.68%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (11.7%)
PIM3	inactive (23.83%)
PIM1	inactive (24.05%)

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 (6.93%)
p38a	inactive (11.34%)
p38b	inactive (7.19%)
p38d	inactive (2.9%)
Erk2	inactive (7.43%)
Erk1	inactive (4.59%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (48.94%)
GSK3B	active (51.78%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-2.54%)
MSSK1	inactive (-1.64%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (0.2%)
CLK2	inactive (18.01%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (4.91%)
HIPK4	inactive (2.64%)
DYRK1B	inactive (1.34%)
DYRK1A	inactive (-0.11%)
DYRK2	inactive (3.89%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (2.13%)