Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GSK978744A

Inchikey : JVAPIYLPNKDKAQ-KGLIPLIRSA-N

ChemSpider : 26639424

Pubchem CID : 25263120

ChEMBL : CHEMBL1794067

	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 (0.21%)
TYK2	inactive (2.03%)
JAK2	inactive (0.06%)
JAK3	inactive (19.66%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (4.95%)
FES	inactive (0.05%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (11.7%)
ABL2	inactive (7.64%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (-0.52%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (0.31%)
BTK	inactive (-0.5%)
TXK	inactive (3.1%)
TEC	inactive (-0.09%)
ITK	inactive (0.81%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (-0.38%)
SRM	inactive (2.19%)
FRK	inactive (2.17%)
BLK	inactive (3.09%)
LCK	inactive (6.12%)
HCK	inactive (6.39%)
FGR	inactive (4.04%)
FYN	inactive (5.15%)
SRC	inactive (5.14%)
YES	inactive (4.27%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (-4.51%)
EphA4	inactive (-0.2%)
EphA3	inactive (1.69%)
EphB4	inactive (-0.4%)
EphB3	inactive (-0.83%)
EphB2	inactive (-2.42%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (-1.09%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (0.64%)
ZAP70	inactive (-0.42%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (3.54%)
ALK	inactive (4.65%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (11.63%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (0.26%)
IGF1R	inactive (-0.34%)
IRR	inactive (-2.11%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (0.79%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	active (51.41%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (3.73%)
TRKB	inactive (14.65%)
TRKC	inactive (29.36%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (6.85%)
MET	inactive (-4.35%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (3.2%)
MER	inactive (3.84%)
TYRO3	inactive (1.84%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (7.49%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (0.72%)
FGFR2	inactive (8.23%)
FGFR3	inactive (6.57%)
FGFR4	inactive (0.23%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (-1.26%)
KDR	inactive (22.16%)
FLT4	inactive (22.78%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (9.24%)
KIT	inactive (4.68%)
FLT3	inactive (5.21%)
PDGFRa	active (62.37%)
PDGFRb	active (54.56%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (14.57%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (2.04%)
TNK1	inactive (18.25%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (2.04%)
ErbB2	inactive (0.61%)
ErbB4	inactive (-1.55%)

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 (-0.05%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (-0.85%)

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 (16.41%)
MST1	inactive (34.09%)
MST2	inactive (25.66%)
MST4	inactive (1.05%)
HGK	inactive (4.28%)
MINK	inactive (2.89%)
LOK	active (85.74%)
PAK1	inactive (1.45%)
PAK3	inactive (-0.49%)
PAK2	inactive (-0.42%)
PAK5	inactive (-4.24%)
PAK6	inactive (-6.36%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (0.3%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (3.43%)
CK1g2	inactive (-0.43%)
CK1g1	inactive (2.39%)
CK1g3	inactive (1.34%)

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	active (93.53%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (1.36%)
AurC	inactive (-2.42%)
AurA	inactive (2.13%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	active (54.95%)
NEK2	inactive (19.71%)
NEK9	active (91.41%)
NEK7	inactive (0.36%)
NEK6	inactive (-3.82%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (-0.29%)
IKKe	inactive (-0.86%)
IKKb	inactive (-1.92%)
IKKa	inactive (-3.48%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (1.94%)

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 (3.37%)
GPRK6	inactive (4.23%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (1.13%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (-0.54%)
MSK2	inactive (1.7%)
RSK1	inactive (3.32%)
RSK2	inactive (5.89%)
RSK4	inactive (12.68%)
RSK3	inactive (3.27%)
p70S6K	inactive (1.5%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (-0.32%)
AKT1	inactive (-0.9%)
AKT3	inactive (-0.44%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (0.68%)
SGK3	inactive (0.55%)
SGK2	inactive (2.9%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (0.23%)
PKCg	inactive (-0.26%)
PKCa	inactive (3.02%)
PKCt	inactive (0.85%)
PKCi	inactive (1.09%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (-0.19%)
PKG1	inactive (-0.2%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (-8.23%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (1.42%)
ROCK2	inactive (0.84%)
MRCKb	inactive (3.59%)
MRCKa	inactive (4.31%)

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 (-1.71%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (-6.84%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (1.44%)
CaMK1d	inactive (0.92%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (4.08%)
PHKg2	inactive (-1.44%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (7.31%)
CaMK2a	inactive (2.24%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (-0.59%)
MAPKAPK2	inactive (-0.94%)
MAPKAPK3	inactive (-0.73%)
MNK2	inactive (2.94%)
MNK1	inactive (2.69%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (0.06%)
PKD1	inactive (0.36%)
PKD2	inactive (1.51%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (5.24%)
MARK3	inactive (5.81%)
MARK1	inactive (5.71%)
QIK	inactive (10.59%)
SIK	inactive (6.54%)
NuaK1	inactive (39.15%)
BRSK1	active (55.76%)
BRSK2	active (68.34%)
MELK	inactive (3.21%)
CHK1	inactive (-1.83%)
PASK	inactive (1.99%)
AMPKa1	inactive (5.73%)
AMPKa2	inactive (2.08%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (0.82%)
TSSK1	inactive (1.14%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (-5.26%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (1.97%)
PIM3	inactive (22.23%)
PIM1	inactive (19.08%)

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 (-0.96%)
p38a	inactive (3.54%)
p38b	inactive (1.86%)
p38d	inactive (-2.7%)
Erk2	inactive (-1.64%)
Erk1	inactive (-2.21%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (3.84%)
GSK3B	inactive (4.23%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-1.3%)
MSSK1	inactive (0.27%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (1.12%)
CLK2	inactive (7.52%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (4.78%)
HIPK4	inactive (9.28%)
DYRK1B	inactive (2.69%)
DYRK1A	inactive (3.71%)
DYRK2	inactive (1.61%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (10.15%)