Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GSK204925A

Inchikey : WJXHPWZUPIMHJP-UHFFFAOYSA-N

ChemSpider : 24695666

Pubchem CID : 25263099

ChEMBL : CHEMBL473629

	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 (-5.52%)
TYK2	inactive (-2.99%)
JAK2	inactive (0.41%)
JAK3	inactive (-0.4%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (1.49%)
FES	inactive (1.71%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (13.7%)
ABL2	inactive (8.26%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (2.94%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (3.43%)
BTK	inactive (0.02%)
TXK	inactive (3.1%)
TEC	inactive (4.4%)
ITK	inactive (2.27%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (4.33%)
SRM	inactive (-2.68%)
FRK	inactive (1.86%)
BLK	inactive (6.17%)
LCK	inactive (5.88%)
HCK	inactive (11.19%)
FGR	inactive (7.7%)
FYN	inactive (2.86%)
SRC	inactive (12.89%)
YES	inactive (4.7%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (0.66%)
EphA4	inactive (3.61%)
EphA3	inactive (4.07%)
EphB4	inactive (2.56%)
EphB3	inactive (2.11%)
EphB2	inactive (6.52%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (4.2%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-0.89%)
ZAP70	inactive (0.59%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (1.98%)
ALK	inactive (5.89%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (6.98%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (0.56%)
IGF1R	inactive (2.07%)
IRR	inactive (2.64%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (2.48%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (3.75%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (3.49%)
TRKB	inactive (8.57%)
TRKC	inactive (14.67%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (6.81%)
MET	inactive (5.5%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-2.35%)
MER	inactive (6.75%)
TYRO3	inactive (0.83%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (23.21%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (2.62%)
FGFR2	inactive (3.63%)
FGFR3	inactive (2.85%)
FGFR4	inactive (2%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (4.71%)
KDR	inactive (16.99%)
FLT4	inactive (21.03%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (4.7%)
KIT	inactive (5.42%)
FLT3	inactive (7.46%)
PDGFRa	active (51.41%)
PDGFRb	inactive (49.91%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (14.92%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (2.21%)
TNK1	inactive (13.48%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (7.65%)
ErbB2	inactive (2.47%)
ErbB4	inactive (13.11%)

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 (0.72%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (3.36%)

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 (7.11%)
MST1	inactive (13.55%)
MST2	inactive (11.02%)
MST4	inactive (-2.27%)
HGK	inactive (26.22%)
MINK	inactive (18.83%)
LOK	active (66.74%)
PAK1	inactive (5.32%)
PAK3	inactive (2.82%)
PAK2	inactive (-0.01%)
PAK5	inactive (-5.75%)
PAK6	inactive (-0.86%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (2.39%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (3.77%)
CK1g2	inactive (7.82%)
CK1g1	inactive (5.65%)
CK1g3	inactive (6.34%)

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 (80.22%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (7.8%)
AurC	inactive (8.14%)
AurA	inactive (8.4%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (1.3%)
NEK2	inactive (4.49%)
NEK9	inactive (6.63%)
NEK7	inactive (2.45%)
NEK6	inactive (1.69%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (22.3%)
IKKe	inactive (2.69%)
IKKb	inactive (0.18%)
IKKa	inactive (1.12%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (6.73%)

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 (2.5%)
GPRK6	inactive (-0.33%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (2.44%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (0.4%)
MSK2	inactive (0.9%)
RSK1	inactive (-0.89%)
RSK2	inactive (0.32%)
RSK4	inactive (2.25%)
RSK3	inactive (1.86%)
p70S6K	inactive (0.05%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (0.89%)
AKT1	inactive (0.01%)
AKT3	inactive (-0.88%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (3.41%)
SGK3	inactive (2.59%)
SGK2	inactive (-1.95%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (0.58%)
PKCg	inactive (1.47%)
PKCa	inactive (1.14%)
PKCt	inactive (-0.63%)
PKCi	inactive (1.71%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (2.13%)
PKG1	inactive (4.13%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (-4.15%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (0.3%)
ROCK2	inactive (-1.5%)
MRCKb	inactive (1.01%)
MRCKa	inactive (2.94%)

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 (4.01%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (0.05%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (0.6%)
CaMK1d	inactive (1.85%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (2.4%)
PHKg2	inactive (0.33%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (3.66%)
CaMK2a	inactive (2.38%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (-0.58%)
MAPKAPK2	inactive (1.03%)
MAPKAPK3	inactive (4.28%)
MNK2	inactive (12.82%)
MNK1	inactive (6.3%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (4.36%)
PKD1	inactive (5.06%)
PKD2	inactive (4.84%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (0.86%)
MARK3	inactive (1.74%)
MARK1	inactive (3.45%)
QIK	inactive (3.75%)
SIK	inactive (9.48%)
NuaK1	inactive (9.13%)
BRSK1	active (76.88%)
BRSK2	active (80.33%)
MELK	inactive (1.31%)
CHK1	inactive (7.39%)
PASK	inactive (-0.56%)
AMPKa1	inactive (4.42%)
AMPKa2	inactive (1.32%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (-0.8%)
TSSK1	inactive (2.26%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (1.51%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (0.47%)
PIM3	inactive (-2.48%)
PIM1	inactive (-0.29%)

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 (3.52%)
p38a	inactive (13.14%)
p38b	inactive (2.87%)
p38d	inactive (1.8%)
Erk2	inactive (3.64%)
Erk1	inactive (0.82%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (3.18%)
GSK3B	inactive (0.1%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-4.19%)
MSSK1	inactive (0.18%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (3.27%)
CLK2	inactive (2.64%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (3.92%)
HIPK4	inactive (19.09%)
DYRK1B	inactive (1.81%)
DYRK1A	inactive (3.09%)
DYRK2	inactive (4.14%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (-0.04%)