Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : SB-347804

Inchikey : ONINFKOEYCCERZ-UHFFFAOYSA-N

ChemSpider : 503651

Pubchem CID : 579429

ChEMBL : CHEMBL397570

	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 (6.11%)
TYK2	inactive (-1.49%)
JAK2	inactive (0.9%)
JAK3	inactive (2.52%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (0.95%)
FES	inactive (1.22%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (4.24%)
ABL2	inactive (2.41%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (0.65%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (0.33%)
BTK	inactive (-0.45%)
TXK	inactive (2.45%)
TEC	inactive (1.25%)
ITK	inactive (0.63%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (-2%)
SRM	inactive (-0.62%)
FRK	inactive (1.01%)
BLK	inactive (1.75%)
LCK	inactive (0.45%)
HCK	inactive (3.88%)
FGR	inactive (1.83%)
FYN	inactive (3.42%)
SRC	inactive (1.56%)
YES	inactive (4.07%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (-2.61%)
EphA4	inactive (2.26%)
EphA3	inactive (2.8%)
EphB4	inactive (0.04%)
EphB3	inactive (3.74%)
EphB2	inactive (5.96%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (1.23%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-0.64%)
ZAP70	inactive (2.47%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (0.33%)
ALK	inactive (1.01%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (4.13%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (2.79%)
IGF1R	inactive (-0.52%)
IRR	inactive (-0.16%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (-0.2%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (2.55%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (-0.28%)
TRKB	inactive (0.82%)
TRKC	inactive (1.15%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (2.12%)
MET	inactive (2.01%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-1.26%)
MER	inactive (0.78%)
TYRO3	inactive (2.87%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (-0.03%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (2.08%)
FGFR2	inactive (3.48%)
FGFR3	inactive (2.77%)
FGFR4	inactive (1.31%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (1.63%)
KDR	inactive (6.96%)
FLT4	inactive (-0.81%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (-0.85%)
KIT	inactive (5.86%)
FLT3	inactive (0.66%)
PDGFRa	inactive (7.32%)
PDGFRb	inactive (5.64%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (2.44%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (0.89%)
TNK1	inactive (2.53%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (1.78%)
ErbB2	inactive (-0.51%)
ErbB4	inactive (7.46%)

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 (0.51%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (3.03%)

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 (1.05%)
MST1	inactive (2.59%)
MST2	inactive (3.36%)
MST4	inactive (2.43%)
HGK	inactive (5.3%)
MINK	inactive (4.89%)
LOK	inactive (6.81%)
PAK1	inactive (3.8%)
PAK3	inactive (1.26%)
PAK2	inactive (0.15%)
PAK5	inactive (-0.51%)
PAK6	inactive (-6.51%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (1.68%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (1.93%)
CK1g2	inactive (0.5%)
CK1g1	inactive (0.78%)
CK1g3	inactive (-1.32%)

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 (2.6%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (1.27%)
AurC	inactive (-4.93%)
AurA	inactive (0.18%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (3.09%)
NEK2	inactive (1.31%)
NEK9	inactive (0.67%)
NEK7	inactive (2.46%)
NEK6	inactive (2.25%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (0.54%)
IKKe	inactive (3.72%)
IKKb	inactive (4.15%)
IKKa	inactive (4.51%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (2.26%)

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 (4.43%)
GPRK6	inactive (4.08%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (1.6%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (2.08%)
MSK2	inactive (2.25%)
RSK1	inactive (2.35%)
RSK2	inactive (2.51%)
RSK4	inactive (0.81%)
RSK3	inactive (1.7%)
p70S6K	inactive (0.86%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (0.77%)
AKT1	inactive (0.69%)
AKT3	inactive (0.2%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (2.65%)
SGK3	inactive (1.54%)
SGK2	inactive (0.76%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (2.09%)
PKCg	inactive (0.62%)
PKCa	inactive (-0.26%)
PKCt	inactive (-0.01%)
PKCi	inactive (-1.26%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (3.35%)
PKG1	inactive (1.54%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (1.79%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (1.82%)
ROCK2	inactive (2.62%)
MRCKb	inactive (1.57%)
MRCKa	inactive (-0.05%)

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 (0.73%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (5.74%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (2.49%)
CaMK1d	inactive (0.45%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (2.76%)
PHKg2	inactive (1.36%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (0.72%)
CaMK2a	inactive (-0.01%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (-0.3%)
MAPKAPK2	inactive (-0.56%)
MAPKAPK3	inactive (0.7%)
MNK2	inactive (1.1%)
MNK1	inactive (1.91%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (1.92%)
PKD1	inactive (2.87%)
PKD2	inactive (2.16%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (1.29%)
MARK3	inactive (1.66%)
MARK1	inactive (0.93%)
QIK	inactive (8.23%)
SIK	inactive (3.96%)
NuaK1	inactive (2.02%)
BRSK1	inactive (1.17%)
BRSK2	inactive (2.38%)
MELK	inactive (5.26%)
CHK1	inactive (0.56%)
PASK	inactive (0.96%)
AMPKa1	inactive (1.54%)
AMPKa2	inactive (2.24%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (0.33%)
TSSK1	inactive (0.89%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (0.36%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (-0.05%)
PIM3	inactive (1.6%)
PIM1	inactive (-0.95%)

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 (2.49%)
p38a	inactive (3.42%)
p38b	inactive (-0.91%)
p38d	inactive (0.84%)
Erk2	inactive (1.25%)
Erk1	inactive (-0.36%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (2.28%)
GSK3B	inactive (3.45%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-1.93%)
MSSK1	inactive (0.88%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (0.61%)
CLK2	inactive (1.4%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (-1.66%)
HIPK4	inactive (-0.61%)
DYRK1B	inactive (1.05%)
DYRK1A	inactive (3.62%)
DYRK2	inactive (0.26%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (1.89%)