Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW779439X

Inchikey : ZOTNSCLLJKXGSD-UHFFFAOYSA-N

ChemSpider : 8349301

Pubchem CID : 10173796

ChEMBL : CHEMBL468963

	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 (17.57%)
TYK2	inactive (8.28%)
JAK2	inactive (30.27%)
JAK3	inactive (49.24%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (37.32%)
FES	inactive (40.23%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	active (63.34%)
ABL2	active (57.29%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (7.32%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (13.74%)
BTK	inactive (5.93%)
TXK	inactive (21.32%)
TEC	inactive (22.94%)
ITK	inactive (13.52%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (28.47%)
SRM	inactive (3.44%)
FRK	inactive (15.43%)
BLK	inactive (15.74%)
LCK	inactive (34.35%)
HCK	inactive (32.57%)
FGR	inactive (47.52%)
FYN	inactive (32.2%)
SRC	active (62.62%)
YES	active (50.21%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (-0.78%)
EphA4	inactive (14.66%)
EphA3	inactive (6.24%)
EphB4	inactive (26.79%)
EphB3	inactive (0.09%)
EphB2	active (57.9%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	active (72.39%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (47.48%)
ZAP70	inactive (11.75%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (28.47%)
ALK	active (62.85%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	active (91.83%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	active (93.61%)
IGF1R	active (84.04%)
IRR	inactive (24.85%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (18.12%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	active (60.32%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (17.31%)
TRKB	inactive (12.69%)
TRKC	inactive (18.42%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (28%)
MET	inactive (27.11%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	active (58.84%)
MER	inactive (29.6%)
TYRO3	inactive (22.92%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (35.72%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (5.49%)
FGFR2	inactive (19.08%)
FGFR3	inactive (14.99%)
FGFR4	inactive (1.16%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (28.38%)
KDR	active (58.72%)
FLT4	inactive (25.51%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	active (92.15%)
KIT	active (107.78%)
FLT3	active (86.35%)
PDGFRa	active (78.69%)
PDGFRb	active (90.85%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (31.09%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (9.11%)
TNK1	active (64.37%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (6.43%)
ErbB2	inactive (2.62%)
ErbB4	inactive (14.77%)

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 (32.39%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (22.4%)

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 (55.74%)
MST1	inactive (22.92%)
MST2	inactive (10.05%)
MST4	inactive (0.67%)
HGK	active (64.78%)
MINK	active (54.8%)
LOK	inactive (47.04%)
PAK1	inactive (39.85%)
PAK3	inactive (17.16%)
PAK2	inactive (37.84%)
PAK5	inactive (43.21%)
PAK6	inactive (7.31%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (17.84%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	active (91.58%)
CK1g2	active (76.8%)
CK1g1	active (61.12%)
CK1g3	active (79.91%)

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 (5.67%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	active (56.46%)
AurC	active (88.27%)
AurA	active (74.19%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (11.41%)
NEK2	inactive (11.7%)
NEK9	inactive (45.37%)
NEK7	inactive (1.08%)
NEK6	inactive (-1.49%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	active (57.28%)
IKKe	inactive (48.53%)
IKKb	inactive (18.16%)
IKKa	inactive (39.48%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (32.34%)

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 (8.59%)
GPRK6	inactive (3.87%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (8.42%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (22.41%)
MSK2	inactive (7.3%)
RSK1	inactive (18.54%)
RSK2	inactive (23.82%)
RSK4	inactive (27.89%)
RSK3	inactive (20.48%)
p70S6K	inactive (7.77%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (1.56%)
AKT1	inactive (0.16%)
AKT3	inactive (3.07%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (18.12%)
SGK3	inactive (0.08%)
SGK2	inactive (3.07%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	active (61.51%)
PKCg	inactive (37.09%)
PKCa	active (77.34%)
PKCt	active (57.16%)
PKCi	inactive (2.12%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	active (60.53%)
PKG1	inactive (24.8%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (-0.22%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (25.97%)
ROCK2	inactive (38.8%)
MRCKb	inactive (21.59%)
MRCKa	inactive (21.55%)

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 (10.15%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (38.87%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (7.85%)
CaMK1d	inactive (18.51%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	active (69.44%)
PHKg2	inactive (25.72%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	active (56.74%)
CaMK2a	inactive (22.62%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (0.45%)
MAPKAPK2	inactive (0.62%)
MAPKAPK3	inactive (2.23%)
MNK2	inactive (24.54%)
MNK1	inactive (17.51%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	active (83.97%)
PKD1	active (79.43%)
PKD2	active (81.04%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (26.76%)
MARK3	inactive (45.99%)
MARK1	inactive (35.38%)
QIK	inactive (47.08%)
SIK	inactive (39.09%)
NuaK1	active (91.9%)
BRSK1	inactive (6.62%)
BRSK2	inactive (8.68%)
MELK	active (76.76%)
CHK1	inactive (11.47%)
PASK	inactive (18.65%)
AMPKa1	inactive (26.86%)
AMPKa2	inactive (34.75%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (2.56%)
TSSK1	inactive (45.28%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (1.71%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	active (51.76%)
PIM3	active (71.31%)
PIM1	active (68.43%)

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 (36.85%)
p38a	inactive (14.27%)
p38b	inactive (9.37%)
p38d	inactive (20.97%)
Erk2	inactive (14.19%)
Erk1	inactive (5.15%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	active (94.53%)
GSK3B	active (93.33%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-3.07%)
MSSK1	inactive (-2.9%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (42.45%)
CLK2	active (100.15%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	active (93.77%)
HIPK4	active (90.76%)
DYRK1B	active (92.87%)
DYRK1A	active (92.58%)
DYRK2	inactive (44.97%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (47.13%)