Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GW778894X

Inchikey : CWRTWFWDDAJOMG-UHFFFAOYSA-N

ChemSpider : 8483988

Pubchem CID : 10308522

ChEMBL : CHEMBL495696

	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 (14.89%)
TYK2	inactive (11%)
JAK2	inactive (22.14%)
JAK3	inactive (36.18%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (48.9%)
FES	inactive (34.26%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (47.52%)
ABL2	inactive (44.32%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (13.39%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (39.71%)
BTK	inactive (5.13%)
TXK	inactive (24.39%)
TEC	inactive (39.33%)
ITK	inactive (21.08%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (23.53%)
SRM	inactive (14.72%)
FRK	inactive (15.98%)
BLK	inactive (26.48%)
LCK	inactive (18.29%)
HCK	inactive (35.91%)
FGR	inactive (41.73%)
FYN	inactive (39.23%)
SRC	active (65.96%)
YES	inactive (36.97%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (15.02%)
EphA4	inactive (43.79%)
EphA3	inactive (19.24%)
EphB4	inactive (22.48%)
EphB3	inactive (3.9%)
EphB2	inactive (46.23%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	active (71.04%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	active (53.19%)
ZAP70	inactive (13.28%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (12.73%)
ALK	inactive (18.74%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	active (74.2%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (40.89%)
IGF1R	inactive (38.2%)
IRR	inactive (10.82%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (7.43%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (24.59%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	active (65.74%)
TRKB	active (75.34%)
TRKC	active (87.55%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (15.57%)
MET	inactive (17.31%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (33.8%)
MER	inactive (46.05%)
TYRO3	inactive (47.82%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (37.35%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (8.94%)
FGFR2	inactive (23.43%)
FGFR3	inactive (17.21%)
FGFR4	inactive (5.22%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (28.26%)
KDR	inactive (43.88%)
FLT4	inactive (22.26%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	active (79.4%)
KIT	active (100.33%)
FLT3	active (67.97%)
PDGFRa	active (52.51%)
PDGFRb	active (65.09%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (18.65%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (11.74%)
TNK1	active (52.28%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (6.11%)
ErbB2	inactive (5.3%)
ErbB4	inactive (19.09%)

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 (15.07%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	active (65.16%)

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 (45.77%)
MST1	inactive (27.62%)
MST2	inactive (24.35%)
MST4	inactive (3.34%)
HGK	active (64.35%)
MINK	active (53.38%)
LOK	inactive (15.76%)
PAK1	inactive (7.42%)
PAK3	inactive (5.22%)
PAK2	inactive (3.52%)
PAK5	inactive (12.68%)
PAK6	inactive (-4.67%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	active (63.04%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	active (69.82%)
CK1g2	inactive (41.38%)
CK1g1	inactive (28.25%)
CK1g3	inactive (43.05%)

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 (9.23%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	active (64.02%)
AurC	active (96.67%)
AurA	active (74.47%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (10.94%)
NEK2	inactive (6.24%)
NEK9	inactive (15.55%)
NEK7	inactive (4.18%)
NEK6	inactive (5.8%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (22.05%)
IKKe	inactive (27.9%)
IKKb	inactive (20.48%)
IKKa	inactive (30.99%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (34.99%)

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 (21.59%)
GPRK6	inactive (8.01%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (6.25%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (8.54%)
MSK2	inactive (8.46%)
RSK1	inactive (7.07%)
RSK2	inactive (4.03%)
RSK4	inactive (8.8%)
RSK3	inactive (4.16%)
p70S6K	inactive (3.59%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (1.66%)
AKT1	inactive (1.36%)
AKT3	inactive (5.1%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (10.4%)
SGK3	inactive (7.33%)
SGK2	inactive (5.14%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (31.91%)
PKCg	inactive (31.17%)
PKCa	active (72.84%)
PKCt	inactive (14.17%)
PKCi	inactive (1.84%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (25.9%)
PKG1	active (50.22%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (2.66%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (5.33%)
ROCK2	inactive (12.38%)
MRCKb	inactive (1.01%)
MRCKa	inactive (2.93%)

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 (10.63%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (0.56%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-0.33%)
CaMK1d	inactive (3.54%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	active (58.31%)
PHKg2	inactive (22.19%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	active (63.35%)
CaMK2a	inactive (35.37%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (4.15%)
MAPKAPK2	inactive (1.6%)
MAPKAPK3	inactive (5%)
MNK2	inactive (33.05%)
MNK1	inactive (22.51%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	active (54.86%)
PKD1	inactive (49.46%)
PKD2	inactive (46.76%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (9.89%)
MARK3	inactive (13.11%)
MARK1	inactive (15.19%)
QIK	inactive (11.94%)
SIK	inactive (15.14%)
NuaK1	active (73.41%)
BRSK1	inactive (7.19%)
BRSK2	inactive (12.06%)
MELK	active (55.85%)
CHK1	inactive (3.73%)
PASK	inactive (0.01%)
AMPKa1	inactive (10.4%)
AMPKa2	inactive (12.52%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (2.95%)
TSSK1	inactive (10.64%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (3.93%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (7.85%)
PIM3	inactive (34.05%)
PIM1	inactive (12.44%)

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 (44.31%)
p38a	inactive (14.63%)
p38b	inactive (13.97%)
p38d	inactive (47.1%)
Erk2	active (59.37%)
Erk1	inactive (35.84%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	active (89.47%)
GSK3B	active (88.08%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (23.01%)
MSSK1	inactive (3.11%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	active (78.39%)
CLK2	active (96.94%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	active (89.32%)
HIPK4	active (88.13%)
DYRK1B	active (86.55%)
DYRK1A	active (86.37%)
DYRK2	active (71.52%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	active (63.93%)