Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GSK1326255A

Inchikey : UKKOZAHWQFYYRW-UHFFFAOYSA-N

ChemSpider : 24696851

Pubchem CID : 25218601

ChEMBL : CHEMBL476259

	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 (20.84%)
TYK2	inactive (-2.78%)
JAK2	inactive (2.85%)
JAK3	inactive (0.07%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	active (82.38%)
FES	active (80.53%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (8.95%)
ABL2	inactive (5.54%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (6.03%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (6.36%)
BTK	inactive (-1.71%)
TXK	inactive (6.29%)
TEC	inactive (7.76%)
ITK	inactive (7.34%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	active (64.75%)
SRM	inactive (14.83%)
FRK	inactive (19.33%)
BLK	inactive (8.52%)
LCK	inactive (9.44%)
HCK	inactive (11.51%)
FGR	inactive (7.49%)
FYN	inactive (25.13%)
SRC	inactive (15.3%)
YES	inactive (19.32%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (-0.82%)
EphA4	inactive (12.93%)
EphA3	inactive (4.22%)
EphB4	inactive (2.91%)
EphB3	inactive (2.33%)
EphB2	inactive (8.57%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	active (96.81%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	active (73.39%)
ZAP70	inactive (29.31%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	active (94.99%)
ALK	active (86.58%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	active (81.27%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	active (97.29%)
IGF1R	active (93.64%)
IRR	active (97.24%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (3.39%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (15.04%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (3.87%)
TRKB	inactive (9.14%)
TRKC	inactive (7.22%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (8.86%)
MET	inactive (22.95%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	active (65.98%)
MER	inactive (20%)
TYRO3	inactive (18.36%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (28.12%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (2.41%)
FGFR2	inactive (6.48%)
FGFR3	inactive (1.74%)
FGFR4	inactive (12.36%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (0.37%)
KDR	inactive (18.55%)
FLT4	inactive (2.22%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	active (81.47%)
KIT	inactive (23.58%)
FLT3	inactive (20.26%)
PDGFRa	inactive (46.49%)
PDGFRb	active (54.51%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (4.59%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (44.27%)
TNK1	active (92.81%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (40.3%)
ErbB2	inactive (12.93%)
ErbB4	active (76.35%)

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 (3.69%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (37.57%)

STE

Test Member No. in Family
Family	no. Member on 518kinase	GPCR
STE20	31	12
STE7	7	1

STE - STE20

Bioactivity
Kinase	GPCR
GCK	active (51.58%)
MST1	inactive (43.94%)
MST2	inactive (13.84%)
MST4	inactive (0.06%)
HGK	active (78.89%)
MINK	active (70.19%)
LOK	inactive (29.22%)
PAK1	inactive (3.04%)
PAK3	inactive (5.21%)
PAK2	inactive (2.08%)
PAK5	inactive (22.59%)
PAK6	inactive (-7.38%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (37.68%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	active (67.47%)
CK1g2	active (72.66%)
CK1g1	active (72.1%)
CK1g3	active (79.75%)

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 (49.78%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (3.04%)
AurC	inactive (-4.81%)
AurA	inactive (10.4%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (21.61%)
NEK2	inactive (17.59%)
NEK9	inactive (32.55%)
NEK7	inactive (8.87%)
NEK6	inactive (8.4%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (10.22%)
IKKe	inactive (5.85%)
IKKb	inactive (7.11%)
IKKa	inactive (18.67%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	active (83.05%)

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 (44.95%)
GPRK6	active (58.79%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (2.45%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (8.65%)
MSK2	inactive (12.03%)
RSK1	active (69.66%)
RSK2	active (66.83%)
RSK4	active (63.37%)
RSK3	active (53.53%)
p70S6K	inactive (7.03%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (1.62%)
AKT1	inactive (0.33%)
AKT3	inactive (2.68%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (13.78%)
SGK3	inactive (4.03%)
SGK2	inactive (5.14%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (9.93%)
PKCg	inactive (29.82%)
PKCa	inactive (16.63%)
PKCt	inactive (8.87%)
PKCi	inactive (1.12%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (47.01%)
PKG1	inactive (46.53%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (4.23%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	active (64.64%)
ROCK2	active (69.83%)
MRCKb	inactive (23.34%)
MRCKa	inactive (30.45%)

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	active (80.92%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (8.21%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (37.94%)
CaMK1d	active (71.47%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	active (80.74%)
PHKg2	active (71.69%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	active (70.99%)
CaMK2a	inactive (43.62%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (40.9%)
MAPKAPK2	inactive (3.23%)
MAPKAPK3	inactive (11.91%)
MNK2	inactive (7.76%)
MNK1	inactive (10.67%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	active (65.92%)
PKD1	active (73.76%)
PKD2	active (75.72%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (42.59%)
MARK3	active (66.64%)
MARK1	active (50.14%)
QIK	inactive (11.69%)
SIK	inactive (14.68%)
NuaK1	active (62.84%)
BRSK1	inactive (2.49%)
BRSK2	inactive (6.88%)
MELK	active (78.7%)
CHK1	inactive (10.69%)
PASK	inactive (20.68%)
AMPKa1	inactive (26.87%)
AMPKa2	inactive (13.22%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	active (91.08%)
TSSK1	active (94.79%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (49.98%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (13.26%)
PIM3	inactive (49.35%)
PIM1	inactive (45.28%)

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	active (83.78%)
p38a	inactive (11.71%)
p38b	inactive (14.26%)
p38d	inactive (5.13%)
Erk2	inactive (30.25%)
Erk1	inactive (13.14%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (8.5%)
GSK3B	inactive (9.55%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (12.71%)
MSSK1	inactive (25.37%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (21.98%)
CLK2	active (93.81%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	active (81.52%)
HIPK4	active (84.59%)
DYRK1B	active (81.9%)
DYRK1A	active (81.88%)
DYRK2	inactive (49.04%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	active (70.33%)