Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW410563A

Inchikey : RDHBGCDZTMPHGL-UHFFFAOYSA-N

ChemSpider : 13556254

Pubchem CID : 21701565

ChEMBL : CHEMBL1909357

	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 (12.6%)
TYK2	inactive (-3.35%)
JAK2	inactive (0.53%)
JAK3	inactive (2.14%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (7.9%)
FES	inactive (3.54%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	active (78.49%)
ABL2	active (65.15%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (16.83%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (13.02%)
BTK	inactive (15.88%)
TXK	inactive (29.51%)
TEC	inactive (36.6%)
ITK	inactive (1.28%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	active (65.49%)
SRM	inactive (18.72%)
FRK	inactive (19.92%)
BLK	inactive (48.95%)
LCK	active (72.24%)
HCK	active (75.14%)
FGR	inactive (46.22%)
FYN	active (56.25%)
SRC	active (70.55%)
YES	inactive (41.95%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (10.61%)
EphA4	inactive (49.93%)
EphA3	inactive (16.73%)
EphB4	inactive (36.9%)
EphB3	inactive (2.9%)
EphB2	inactive (41.35%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (18.9%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (0.27%)
ZAP70	inactive (1.79%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (24.81%)
ALK	inactive (13.84%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (10.18%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (6.96%)
IGF1R	inactive (10.98%)
IRR	inactive (3.05%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (9.45%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (7.42%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (2.17%)
TRKB	inactive (6.25%)
TRKC	inactive (7.05%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (2.44%)
MET	inactive (9.16%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-10.38%)
MER	inactive (4.97%)
TYRO3	inactive (34.45%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	active (89.43%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (17.22%)
FGFR2	inactive (15.85%)
FGFR3	inactive (10.2%)
FGFR4	inactive (4.07%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	active (93.16%)
KDR	active (71.95%)
FLT4	active (106.9%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (6.14%)
KIT	inactive (40.52%)
FLT3	inactive (3.03%)
PDGFRa	active (93.87%)
PDGFRb	active (76.63%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (17.68%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (5.7%)
TNK1	inactive (23.77%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	active (80.9%)
ErbB2	inactive (26.32%)
ErbB4	active (68.67%)

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 (2.62%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (10.02%)

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 (5.63%)
MST1	inactive (9.47%)
MST2	inactive (8.26%)
MST4	inactive (-1.08%)
HGK	inactive (21.39%)
MINK	inactive (18.01%)
LOK	active (70.08%)
PAK1	inactive (7.41%)
PAK3	inactive (5.36%)
PAK2	inactive (2.35%)
PAK5	inactive (7.08%)
PAK6	inactive (0.34%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (5.54%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (5.91%)
CK1g2	inactive (4.75%)
CK1g1	inactive (4.87%)
CK1g3	inactive (4.02%)

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 (2.77%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (8.54%)
AurC	inactive (4.32%)
AurA	inactive (7.23%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (5.46%)
NEK2	inactive (7.02%)
NEK9	inactive (11.57%)
NEK7	inactive (4.92%)
NEK6	inactive (4.18%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (5.95%)
IKKe	inactive (6.95%)
IKKb	inactive (6.01%)
IKKa	inactive (11.61%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (7.27%)

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 (7.5%)
GPRK6	inactive (5.91%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (1.01%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (4.76%)
MSK2	inactive (2.32%)
RSK1	inactive (6.05%)
RSK2	inactive (3.02%)
RSK4	inactive (3.03%)
RSK3	inactive (3.51%)
p70S6K	inactive (2.36%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (1.77%)
AKT1	inactive (0.96%)
AKT3	inactive (1.76%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (5.46%)
SGK3	inactive (4.55%)
SGK2	inactive (2.34%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (0.65%)
PKCg	inactive (7.37%)
PKCa	inactive (3.24%)
PKCt	inactive (5.28%)
PKCi	inactive (1.78%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (3.65%)
PKG1	inactive (3.61%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (2.06%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (0.99%)
ROCK2	inactive (3.9%)
MRCKb	inactive (0.25%)
MRCKa	inactive (0.79%)

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 (25.46%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (0.34%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-3.77%)
CaMK1d	inactive (0.02%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (23.48%)
PHKg2	inactive (7.74%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (3.68%)
CaMK2a	inactive (2.74%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (2.36%)
MAPKAPK2	inactive (3.42%)
MAPKAPK3	inactive (7.13%)
MNK2	inactive (15.84%)
MNK1	inactive (30.88%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (8.58%)
PKD1	inactive (9.92%)
PKD2	inactive (10.51%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (4.13%)
MARK3	inactive (6.46%)
MARK1	inactive (7.86%)
QIK	inactive (18.93%)
SIK	inactive (33.21%)
NuaK1	inactive (1.93%)
BRSK1	inactive (3.78%)
BRSK2	inactive (6.2%)
MELK	inactive (8.15%)
CHK1	inactive (4%)
PASK	inactive (0.97%)
AMPKa1	inactive (5.7%)
AMPKa2	inactive (5.2%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (2.03%)
TSSK1	inactive (3.21%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (6.25%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (2.78%)
PIM3	inactive (4.22%)
PIM1	inactive (1.44%)

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 (5.02%)
p38a	inactive (22.07%)
p38b	inactive (17.35%)
p38d	inactive (6.31%)
Erk2	inactive (7.98%)
Erk1	inactive (7.04%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (8.57%)
GSK3B	inactive (11.18%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-0.28%)
MSSK1	inactive (0.42%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (2.38%)
CLK2	inactive (0.29%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (2.79%)
HIPK4	inactive (9.35%)
DYRK1B	inactive (4.18%)
DYRK1A	inactive (7.48%)
DYRK2	inactive (4.5%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (6.37%)