Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW806742X

Inchikey : SNRUTMWCDZHKKM-UHFFFAOYSA-N

ChemSpider : 4486980

Pubchem CID : 5329829

ChEMBL : CHEMBL188381

	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 (12.81%)
TYK2	inactive (-2.45%)
JAK2	inactive (1.31%)
JAK3	inactive (-1.69%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	active (60.42%)
FES	inactive (21.84%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	active (70.97%)
ABL2	active (71.91%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (29.38%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (26.05%)
BTK	inactive (5.19%)
TXK	inactive (8.63%)
TEC	inactive (7.04%)
ITK	active (67.32%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	active (77.12%)
SRM	inactive (14.34%)
FRK	inactive (40.91%)
BLK	active (86.33%)
LCK	active (80.13%)
HCK	active (77.32%)
FGR	active (57.18%)
FYN	active (53.45%)
SRC	active (86.55%)
YES	active (65.22%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (35.39%)
EphA4	active (59.75%)
EphA3	inactive (18.28%)
EphB4	inactive (30.67%)
EphB3	inactive (8.25%)
EphB2	active (54.79%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	active (59.02%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-15.2%)
ZAP70	inactive (3.87%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (6.43%)
ALK	inactive (4.22%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	active (66.9%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (2.39%)
IGF1R	inactive (0.46%)
IRR	inactive (3.26%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	active (88.61%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	active (58.5%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	active (90.54%)
TRKB	active (82.57%)
TRKC	active (87.1%)

TK - Met

Bioactivity
Kinase	GPCR
RON	active (90.45%)
MET	active (64.92%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (16.19%)
MER	inactive (49.2%)
TYRO3	inactive (27.24%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	active (71.96%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (20.28%)
FGFR2	active (53.86%)
FGFR3	inactive (23.29%)
FGFR4	inactive (2.57%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	active (96.07%)
KDR	active (99.56%)
FLT4	active (90.09%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	active (86.12%)
KIT	active (95.27%)
FLT3	active (87.42%)
PDGFRa	active (86.7%)
PDGFRb	active (82.09%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	active (79.25%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (4.69%)
TNK1	active (82.2%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (3.21%)
ErbB2	inactive (4.23%)
ErbB4	inactive (14.49%)

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 (2.86%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (22.72%)

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 (69.45%)
MST1	inactive (9.45%)
MST2	inactive (6.49%)
MST4	inactive (-3.21%)
HGK	active (85.06%)
MINK	active (80.29%)
LOK	active (70.36%)
PAK1	inactive (-0.37%)
PAK3	inactive (0.7%)
PAK2	inactive (-1.63%)
PAK5	inactive (1.16%)
PAK6	inactive (-2%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (13.69%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (-0.75%)
CK1g2	inactive (2.66%)
CK1g1	inactive (3.06%)
CK1g3	inactive (2.37%)

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 (-0.02%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	active (78.98%)
AurC	active (96.53%)
AurA	active (76.84%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (2.63%)
NEK2	inactive (3.03%)
NEK9	inactive (17.05%)
NEK7	inactive (-1.48%)
NEK6	inactive (0.14%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (9.01%)
IKKe	inactive (7.75%)
IKKb	inactive (2.85%)
IKKa	inactive (3.54%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (6.4%)

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 (-1.66%)
GPRK6	inactive (-2.97%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (1.53%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (-1.11%)
MSK2	inactive (4.78%)
RSK1	inactive (0.25%)
RSK2	inactive (-0.29%)
RSK4	inactive (-0.89%)
RSK3	inactive (2.2%)
p70S6K	inactive (1.95%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (1.22%)
AKT1	inactive (0.88%)
AKT3	inactive (2.79%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (1.43%)
SGK3	inactive (2.44%)
SGK2	inactive (4.82%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (-0.51%)
PKCg	inactive (2.99%)
PKCa	inactive (0.85%)
PKCt	inactive (0.96%)
PKCi	inactive (-0.73%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (-0.82%)
PKG1	inactive (0.56%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	-

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (1.61%)
ROCK2	inactive (3.48%)
MRCKb	inactive (-2.72%)
MRCKa	inactive (-0.82%)

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 (25.95%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (0.7%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (0.59%)
CaMK1d	inactive (0.2%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (9.58%)
PHKg2	inactive (2.53%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (0.14%)
CaMK2a	inactive (-1.5%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (-0.8%)
MAPKAPK2	inactive (-0.37%)
MAPKAPK3	inactive (7.62%)
MNK2	active (67.35%)
MNK1	active (73.26%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (3.42%)
PKD1	inactive (4.48%)
PKD2	inactive (3.78%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (1.56%)
MARK3	inactive (-0.68%)
MARK1	inactive (2.36%)
QIK	inactive (-0.49%)
SIK	inactive (7.29%)
NuaK1	inactive (10.09%)
BRSK1	inactive (5.53%)
BRSK2	inactive (1.96%)
MELK	inactive (-2.07%)
CHK1	inactive (-0.01%)
PASK	inactive (0.28%)
AMPKa1	inactive (1.3%)
AMPKa2	inactive (2.41%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (1.3%)
TSSK1	inactive (2.44%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (2.02%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (0.39%)
PIM3	inactive (-1.83%)
PIM1	inactive (-0.84%)

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 (3.15%)
p38a	inactive (13.57%)
p38b	inactive (16.71%)
p38d	inactive (6.6%)
Erk2	inactive (3.93%)
Erk1	inactive (3.33%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (9.4%)
GSK3B	inactive (13.6%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (1.1%)
MSSK1	inactive (16.65%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (1.99%)
CLK2	inactive (-2.84%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (34.05%)
HIPK4	active (83.57%)
DYRK1B	inactive (-0.44%)
DYRK1A	inactive (1.5%)
DYRK2	inactive (3.14%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (1.68%)