Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GSK625137A

Inchikey : KDDJEKWJEFRYAO-UHFFFAOYSA-N

ChemSpider : 13176822

Pubchem CID : 16048415

ChEMBL : CHEMBL230911

	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 (4.31%)
TYK2	inactive (-2.55%)
JAK2	inactive (1.86%)
JAK3	inactive (-1.1%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (4.57%)
FES	inactive (3.92%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (40.16%)
ABL2	active (54.19%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (16.1%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (49.65%)
BTK	inactive (11.79%)
TXK	active (76.11%)
TEC	active (58.7%)
ITK	inactive (1.74%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (36.91%)
SRM	inactive (5.81%)
FRK	inactive (7.89%)
BLK	inactive (17.49%)
LCK	inactive (41.61%)
HCK	inactive (43.71%)
FGR	inactive (26.96%)
FYN	inactive (37.62%)
SRC	active (59.78%)
YES	inactive (36.05%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	active (56.26%)
EphA4	active (62.84%)
EphA3	inactive (8.77%)
EphB4	inactive (36.05%)
EphB3	inactive (21.09%)
EphB2	active (57.73%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (13.45%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (1.64%)
ZAP70	inactive (28.99%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (6.16%)
ALK	inactive (5.19%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (14.74%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (6.25%)
IGF1R	inactive (5.9%)
IRR	inactive (1.56%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (27.57%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (3.55%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (1.84%)
TRKB	inactive (3.86%)
TRKC	inactive (4.68%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (2.14%)
MET	inactive (3.43%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-6.8%)
MER	inactive (3.16%)
TYRO3	inactive (3.61%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (27.01%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (6.54%)
FGFR2	inactive (8.42%)
FGFR3	inactive (6.17%)
FGFR4	inactive (1.49%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (5.65%)
KDR	inactive (10.73%)
FLT4	inactive (6.17%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	active (64.83%)
KIT	active (75.49%)
FLT3	inactive (4.55%)
PDGFRa	inactive (36.18%)
PDGFRb	inactive (26.04%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (6.28%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (7.25%)
TNK1	inactive (6.5%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (18.01%)
ErbB2	inactive (8.53%)
ErbB4	inactive (33.78%)

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 (2.52%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (8.98%)

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 (0.97%)
MST1	inactive (6.8%)
MST2	inactive (3.58%)
MST4	inactive (-1.56%)
HGK	inactive (32.34%)
MINK	inactive (26.11%)
LOK	inactive (9.99%)
PAK1	inactive (6.44%)
PAK3	inactive (6.71%)
PAK2	inactive (2.41%)
PAK5	inactive (2.18%)
PAK6	inactive (-5.82%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (5.89%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (7.76%)
CK1g2	inactive (4.95%)
CK1g1	inactive (5.37%)
CK1g3	inactive (4.47%)

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 (5.13%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (4.94%)
AurC	inactive (5.08%)
AurA	inactive (6.63%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (3.27%)
NEK2	inactive (6.13%)
NEK9	inactive (3.74%)
NEK7	inactive (3.98%)
NEK6	inactive (-0.35%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (9.27%)
IKKe	inactive (14.92%)
IKKb	inactive (27.46%)
IKKa	inactive (31.73%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (10.82%)

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 (9.17%)
GPRK6	inactive (3.56%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (1.99%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (0.93%)
MSK2	inactive (3.43%)
RSK1	inactive (-1.21%)
RSK2	inactive (1.47%)
RSK4	inactive (2.63%)
RSK3	inactive (2.57%)
p70S6K	inactive (2.1%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (2.56%)
AKT1	inactive (0.01%)
AKT3	inactive (3.46%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (2.48%)
SGK3	inactive (5.81%)
SGK2	inactive (3.52%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (7.89%)
PKCg	inactive (4.29%)
PKCa	inactive (4.38%)
PKCt	inactive (4.49%)
PKCi	inactive (4.85%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (5.42%)
PKG1	inactive (8.21%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (2.61%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (6.72%)
ROCK2	inactive (9.1%)
MRCKb	inactive (2.4%)
MRCKa	inactive (-0.04%)

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 (-0.01%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (1.19%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-0.82%)
CaMK1d	inactive (1.27%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (4.23%)
PHKg2	inactive (5.48%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (4.63%)
CaMK2a	inactive (3.97%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (2.24%)
MAPKAPK2	inactive (-0.33%)
MAPKAPK3	inactive (-0.36%)
MNK2	inactive (6.55%)
MNK1	inactive (9.56%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (6.16%)
PKD1	inactive (6.39%)
PKD2	inactive (5.63%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (1.61%)
MARK3	inactive (11.93%)
MARK1	inactive (8.02%)
QIK	inactive (14.21%)
SIK	inactive (23.96%)
NuaK1	inactive (1.68%)
BRSK1	inactive (4.23%)
BRSK2	inactive (2.72%)
MELK	inactive (7.85%)
CHK1	inactive (-2.65%)
PASK	inactive (-1.32%)
AMPKa1	inactive (2.86%)
AMPKa2	inactive (4.03%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (1.64%)
TSSK1	inactive (5.71%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (-2.35%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (0.75%)
PIM3	inactive (-1.81%)
PIM1	inactive (1.24%)

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 (6.49%)
p38a	inactive (14.95%)
p38b	inactive (14.78%)
p38d	inactive (5.81%)
Erk2	inactive (6.15%)
Erk1	inactive (5.5%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (12.7%)
GSK3B	inactive (9.17%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-0.84%)
MSSK1	inactive (-0.93%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (2.34%)
CLK2	inactive (1.33%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (-0.02%)
HIPK4	inactive (4.34%)
DYRK1B	inactive (17.88%)
DYRK1A	inactive (29.2%)
DYRK2	inactive (4.25%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (2.75%)