Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW580509X

Inchikey : GOGIUMBXFRNDRK-UHFFFAOYSA-N

ChemSpider : 4487011

Pubchem CID : 5329860

ChEMBL : CHEMBL179311

	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 (-4.39%)
TYK2	inactive (-4.34%)
JAK2	inactive (1.58%)
JAK3	inactive (5.85%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (3.8%)
FES	inactive (2.42%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	active (77.65%)
ABL2	active (72.59%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (10.58%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (25.94%)
BTK	inactive (21.64%)
TXK	active (53.42%)
TEC	inactive (35.47%)
ITK	inactive (5.9%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (40.66%)
SRM	inactive (30.57%)
FRK	inactive (26.93%)
BLK	active (64.27%)
LCK	inactive (47.6%)
HCK	active (67.18%)
FGR	active (65.16%)
FYN	active (76.47%)
SRC	active (79.36%)
YES	active (80.24%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (3.85%)
EphA4	inactive (12%)
EphA3	inactive (8.5%)
EphB4	inactive (11.91%)
EphB3	inactive (2.36%)
EphB2	inactive (24.28%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (10.95%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-2.39%)
ZAP70	inactive (-2.95%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (3.16%)
ALK	inactive (8.1%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (43.27%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (5.78%)
IGF1R	inactive (4.95%)
IRR	inactive (3.36%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (20%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	-

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (30.87%)
TRKB	inactive (43.51%)
TRKC	inactive (49.3%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (3.42%)
MET	inactive (2.24%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-1.98%)
MER	inactive (7.73%)
TYRO3	inactive (40.57%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	active (68.53%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (40.23%)
FGFR2	active (68.17%)
FGFR3	active (70.02%)
FGFR4	inactive (7.65%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	active (55.85%)
KDR	active (73.18%)
FLT4	active (77.75%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	active (71.92%)
KIT	active (96.99%)
FLT3	active (68.05%)
PDGFRa	active (58.37%)
PDGFRb	active (74.76%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (16.09%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (15.3%)
TNK1	active (90.64%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (8.46%)
ErbB2	inactive (0.18%)
ErbB4	inactive (22.11%)

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 (2.08%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (5.54%)

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 (6.14%)
MST1	inactive (10.57%)
MST2	inactive (7.22%)
MST4	inactive (-4.12%)
HGK	inactive (25.87%)
MINK	inactive (16.75%)
LOK	inactive (8.64%)
PAK1	inactive (5.71%)
PAK3	inactive (2.36%)
PAK2	inactive (1.98%)
PAK5	inactive (-1.57%)
PAK6	inactive (2.64%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (3.57%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (6.31%)
CK1g2	inactive (3.73%)
CK1g1	inactive (6.2%)
CK1g3	inactive (5.62%)

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 (1.04%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (5.4%)
AurC	inactive (14.62%)
AurA	inactive (34.52%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (1.45%)
NEK2	inactive (2.94%)
NEK9	inactive (4.07%)
NEK7	inactive (2.42%)
NEK6	inactive (0.87%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (9.22%)
IKKe	inactive (4.13%)
IKKb	inactive (1.16%)
IKKa	inactive (-4.47%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (7.02%)

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 (-8.47%)
GPRK6	inactive (-5%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (2.17%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (7.32%)
MSK2	inactive (3.76%)
RSK1	inactive (4.04%)
RSK2	inactive (0.81%)
RSK4	inactive (3.54%)
RSK3	inactive (4.86%)
p70S6K	inactive (1.18%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (0.82%)
AKT1	inactive (0.85%)
AKT3	inactive (-0.57%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (2.05%)
SGK3	inactive (-0.11%)
SGK2	inactive (5.99%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (1.66%)
PKCg	inactive (3.87%)
PKCa	inactive (5.21%)
PKCt	inactive (0.3%)
PKCi	inactive (3.38%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (2.95%)
PKG1	inactive (2.34%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (-2.35%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (2.35%)
ROCK2	inactive (1.18%)
MRCKb	inactive (0.59%)
MRCKa	inactive (-0.94%)

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 (2.17%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (-0.14%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (1.2%)
CaMK1d	inactive (1.97%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (18.29%)
PHKg2	inactive (-0.05%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (9.35%)
CaMK2a	inactive (6.74%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (-0.22%)
MAPKAPK2	inactive (0.67%)
MAPKAPK3	inactive (3.53%)
MNK2	inactive (10.55%)
MNK1	inactive (16.98%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (3.64%)
PKD1	inactive (4.41%)
PKD2	inactive (3.71%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (1.64%)
MARK3	inactive (2.05%)
MARK1	inactive (2.37%)
QIK	inactive (31.24%)
SIK	inactive (28.56%)
NuaK1	inactive (13.38%)
BRSK1	inactive (-0.15%)
BRSK2	inactive (0.66%)
MELK	inactive (11.45%)
CHK1	inactive (3.19%)
PASK	inactive (-1.97%)
AMPKa1	inactive (1.33%)
AMPKa2	inactive (4.19%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (-3.49%)
TSSK1	inactive (-0.25%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (4.19%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (0.96%)
PIM3	inactive (-0.55%)
PIM1	inactive (2.93%)

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 (6.62%)
p38a	inactive (7.73%)
p38b	inactive (5.17%)
p38d	inactive (4.76%)
Erk2	inactive (1.18%)
Erk1	inactive (-2.17%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (9.4%)
GSK3B	inactive (11.15%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-1.28%)
MSSK1	inactive (0.2%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (13.23%)
CLK2	active (85.97%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (48.34%)
HIPK4	active (65.67%)
DYRK1B	inactive (37.7%)
DYRK1A	inactive (41.35%)
DYRK2	inactive (18.39%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (29.27%)