Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW445015X

Inchikey : IDHOIXYTISLBFT-BQYQJAHWSA-N

ChemSpider : 23278145

Pubchem CID : 44418555

ChEMBL : CHEMBL218969

	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 (12.65%)
TYK2	inactive (-3.23%)
JAK2	inactive (1.45%)
JAK3	inactive (0.49%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (4.88%)
FES	inactive (1.6%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (25.93%)
ABL2	inactive (16.14%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (9.89%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (16.08%)
BTK	inactive (1.29%)
TXK	inactive (24.53%)
TEC	inactive (16.41%)
ITK	inactive (2.59%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (14.53%)
SRM	inactive (0.97%)
FRK	inactive (1.8%)
BLK	inactive (6.2%)
LCK	inactive (7.19%)
HCK	inactive (20.11%)
FGR	inactive (9.23%)
FYN	inactive (10.75%)
SRC	inactive (13.65%)
YES	inactive (9.93%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (3.92%)
EphA4	inactive (26.08%)
EphA3	inactive (6.47%)
EphB4	inactive (9.19%)
EphB3	inactive (4.91%)
EphB2	inactive (19.69%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (5.23%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-0.24%)
ZAP70	inactive (2.36%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (2.98%)
ALK	inactive (4.22%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (5.86%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (2.34%)
IGF1R	inactive (6.92%)
IRR	inactive (2.86%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (5.42%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (3.97%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (1.73%)
TRKB	inactive (4.3%)
TRKC	inactive (5.34%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (5.25%)
MET	inactive (5.5%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-5.59%)
MER	inactive (1.66%)
TYRO3	inactive (3.96%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (6.36%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (3.14%)
FGFR2	inactive (4.95%)
FGFR3	inactive (4.39%)
FGFR4	inactive (-0.62%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (0.49%)
KDR	inactive (7.71%)
FLT4	inactive (3.1%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (4.09%)
KIT	inactive (14.52%)
FLT3	inactive (1.3%)
PDGFRa	inactive (17.8%)
PDGFRb	inactive (20.13%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (-0.24%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (8.09%)
TNK1	inactive (20.73%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (3.62%)
ErbB2	inactive (6.67%)
ErbB4	inactive (14.85%)

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%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (7.91%)

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 (2.16%)
MST1	inactive (17.2%)
MST2	inactive (15.19%)
MST4	inactive (2.47%)
HGK	inactive (19.68%)
MINK	inactive (15.54%)
LOK	inactive (9.43%)
PAK1	inactive (7.54%)
PAK3	inactive (5.93%)
PAK2	inactive (2.02%)
PAK5	inactive (4.8%)
PAK6	inactive (11.97%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (5.22%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (5.05%)
CK1g2	inactive (2.72%)
CK1g1	inactive (3.62%)
CK1g3	inactive (3.55%)

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 (3.11%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (-0.01%)
AurC	inactive (-3.67%)
AurA	inactive (9.59%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (4.28%)
NEK2	inactive (5.88%)
NEK9	inactive (3.57%)
NEK7	inactive (4.03%)
NEK6	inactive (3.73%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (6.39%)
IKKe	inactive (5.71%)
IKKb	inactive (5.04%)
IKKa	inactive (2.32%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (11.72%)

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	inactive (0.44%)
GPRK6	inactive (8.41%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (2.37%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (6.01%)
MSK2	inactive (4.27%)
RSK1	inactive (4.99%)
RSK2	inactive (3.84%)
RSK4	inactive (0.63%)
RSK3	inactive (2.74%)
p70S6K	inactive (1.97%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (2.34%)
AKT1	inactive (1.08%)
AKT3	inactive (1.52%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (5.48%)
SGK3	inactive (4.02%)
SGK2	inactive (0.66%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (5.78%)
PKCg	inactive (4.82%)
PKCa	inactive (1.68%)
PKCt	inactive (5.04%)
PKCi	inactive (1.08%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (5.05%)
PKG1	inactive (5.68%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (6.15%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (1.27%)
ROCK2	inactive (8.78%)
MRCKb	inactive (0.83%)
MRCKa	inactive (2.94%)

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 (3.83%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (0.28%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-2.38%)
CaMK1d	inactive (-0.91%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (7.61%)
PHKg2	inactive (7.42%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (3.14%)
CaMK2a	inactive (3.24%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (3.16%)
MAPKAPK2	inactive (2.51%)
MAPKAPK3	inactive (3.22%)
MNK2	inactive (14.95%)
MNK1	inactive (29.39%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (4.34%)
PKD1	inactive (5.01%)
PKD2	inactive (3.79%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (3.49%)
MARK3	inactive (6.03%)
MARK1	inactive (7.06%)
QIK	inactive (18.47%)
SIK	inactive (39.53%)
NuaK1	inactive (9.32%)
BRSK1	inactive (14.96%)
BRSK2	inactive (17.41%)
MELK	inactive (4.29%)
CHK1	inactive (5.73%)
PASK	inactive (0.95%)
AMPKa1	inactive (7.91%)
AMPKa2	inactive (6.66%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (2.6%)
TSSK1	inactive (5.13%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (7.67%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (1.06%)
PIM3	inactive (5.04%)
PIM1	inactive (2.22%)

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 (5.08%)
p38a	inactive (6.09%)
p38b	inactive (7.21%)
p38d	inactive (3.77%)
Erk2	inactive (5.85%)
Erk1	inactive (4.66%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (12.28%)
GSK3B	inactive (10.8%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (2.3%)
MSSK1	inactive (3.21%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (2.09%)
CLK2	inactive (2.46%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (3.05%)
HIPK4	inactive (3.78%)
DYRK1B	inactive (0.92%)
DYRK1A	inactive (1.83%)
DYRK2	inactive (3.1%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (7.63%)