Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GSK1007102B

Inchikey : YESZPTXRITXXAP-LMOVPXPDSA-N

ChemSpider : 28484241

Pubchem CID : 56604034

ChEMBL : CHEMBL1909349

	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 (4.4%)
TYK2	inactive (1.49%)
JAK2	inactive (0.78%)
JAK3	inactive (3.54%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (11.59%)
FES	inactive (5.21%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (5.55%)
ABL2	inactive (6.91%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (-5.08%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (-1.16%)
BTK	inactive (-0.15%)
TXK	inactive (2.31%)
TEC	inactive (5.82%)
ITK	inactive (0.91%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (-2.85%)
SRM	inactive (0.15%)
FRK	inactive (0.63%)
BLK	inactive (10.05%)
LCK	inactive (4.58%)
HCK	inactive (14.14%)
FGR	inactive (28.63%)
FYN	inactive (25%)
SRC	inactive (20.9%)
YES	inactive (23.82%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (-4.53%)
EphA4	inactive (-4.76%)
EphA3	inactive (-0.7%)
EphB4	inactive (1.16%)
EphB3	inactive (-3.07%)
EphB2	inactive (-10.4%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	active (80.14%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (0.56%)
ZAP70	inactive (1.24%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	active (76.58%)
ALK	inactive (19.62%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (11.08%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (1.91%)
IGF1R	inactive (-0.35%)
IRR	inactive (-2.16%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (0.1%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (1.93%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (0.16%)
TRKB	inactive (1.16%)
TRKC	inactive (0.7%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (3.42%)
MET	inactive (-0.12%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (8.92%)
MER	inactive (0.57%)
TYRO3	inactive (6.97%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	active (90.03%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (6.16%)
FGFR2	inactive (1.12%)
FGFR3	inactive (-0.33%)
FGFR4	inactive (1.13%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	active (79.76%)
KDR	active (75.36%)
FLT4	active (93.81%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (1.9%)
KIT	inactive (2.69%)
FLT3	inactive (-0.29%)
PDGFRa	active (70.5%)
PDGFRb	active (79.55%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (11.39%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (-1.74%)
TNK1	inactive (-3.26%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (7.41%)
ErbB2	inactive (-2.4%)
ErbB4	inactive (3.97%)

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 (-0.97%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (5.48%)

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 (24.78%)
MST1	inactive (15.95%)
MST2	inactive (-24.5%)
MST4	inactive (10.8%)
HGK	inactive (20.4%)
MINK	inactive (11%)
LOK	inactive (19.75%)
PAK1	inactive (13.97%)
PAK3	inactive (15.6%)
PAK2	inactive (48.93%)
PAK5	active (62.23%)
PAK6	active (67.59%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (6.28%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (4.15%)
CK1g2	inactive (4.43%)
CK1g1	inactive (7.01%)
CK1g3	inactive (9.88%)

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 (0.24%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (6.56%)
AurC	inactive (1.38%)
AurA	inactive (5.65%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (17.23%)
NEK2	inactive (33.49%)
NEK9	inactive (-1.03%)
NEK7	inactive (0.58%)
NEK6	inactive (-0.92%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	active (67.96%)
IKKe	active (98.87%)
IKKb	inactive (-3.23%)
IKKa	inactive (-2.27%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (8.72%)

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	active (113.79%)
GPRK6	inactive (1.51%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (27.81%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	active (51.31%)
MSK2	active (61.31%)
RSK1	active (71.6%)
RSK2	active (69.47%)
RSK4	inactive (23.4%)
RSK3	active (69.86%)
p70S6K	active (58.4%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	active (96.15%)
AKT1	active (96.39%)
AKT3	active (94.95%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (34.16%)
SGK3	active (94.21%)
SGK2	inactive (3.43%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	active (99.03%)
PKCg	active (81.14%)
PKCa	active (69.69%)
PKCt	active (84.79%)
PKCi	inactive (26.39%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	active (84.42%)
PKG1	active (81.14%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	active (88.15%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	active (51.72%)
ROCK2	active (59.44%)
MRCKb	active (66.16%)
MRCKa	active (72.78%)

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 (26.73%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (18.51%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (4.51%)
CaMK1d	inactive (29.44%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (12.34%)
PHKg2	inactive (-0.93%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (14.33%)
CaMK2a	inactive (1.68%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (-1.11%)
MAPKAPK2	inactive (-1%)
MAPKAPK3	inactive (-0.47%)
MNK2	inactive (33.12%)
MNK1	inactive (6.37%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	active (64.35%)
PKD1	active (61.64%)
PKD2	active (66.28%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	active (90.73%)
MARK3	active (101.34%)
MARK1	active (93.14%)
QIK	inactive (14.82%)
SIK	inactive (8.3%)
NuaK1	active (69.58%)
BRSK1	inactive (38.4%)
BRSK2	active (58.84%)
MELK	active (90.41%)
CHK1	inactive (31.05%)
PASK	inactive (15.87%)
AMPKa1	active (88.09%)
AMPKa2	active (68.09%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (14.79%)
TSSK1	active (95.61%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (2.31%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (20.65%)
PIM3	inactive (39%)
PIM1	inactive (35.22%)

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 (1.01%)
p38a	inactive (1.33%)
p38b	inactive (2.96%)
p38d	inactive (0.11%)
Erk2	inactive (5.15%)
Erk1	inactive (0.99%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	active (86.12%)
GSK3B	active (84.6%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-3.25%)
MSSK1	inactive (-2.07%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (1.71%)
CLK2	active (56.31%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	active (55.3%)
HIPK4	inactive (36.28%)
DYRK1B	inactive (9.96%)
DYRK1A	inactive (7.95%)
DYRK2	inactive (0.08%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (3.9%)