Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : GSK180736A

Inchikey : HEAIGWIZTYAQTC-UHFFFAOYSA-N

ChemSpider : 9408921

Pubchem CID : 11233873

ChEMBL : CHEMBL384073

	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	active (70.26%)
TYK2	inactive (26.3%)
JAK2	inactive (35.12%)
JAK3	inactive (30.77%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (2.17%)
FES	inactive (0.3%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (8.74%)
ABL2	inactive (19.73%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (1.35%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (1.24%)
BTK	inactive (-1.83%)
TXK	inactive (3.78%)
TEC	inactive (2.37%)
ITK	inactive (1.33%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (5.55%)
SRM	inactive (2.69%)
FRK	inactive (1.47%)
BLK	inactive (3.91%)
LCK	inactive (3.1%)
HCK	inactive (2.81%)
FGR	inactive (0.7%)
FYN	inactive (4.69%)
SRC	inactive (4.28%)
YES	inactive (3.94%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (-2.18%)
EphA4	inactive (4.52%)
EphA3	inactive (2.14%)
EphB4	inactive (0.92%)
EphB3	inactive (1.2%)
EphB2	inactive (5.02%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (8.37%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (1.72%)
ZAP70	inactive (1.91%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (1.52%)
ALK	inactive (3.89%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (29.2%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (4.22%)
IGF1R	inactive (8.59%)
IRR	inactive (0.72%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (0.08%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (5.88%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (3.3%)
TRKB	inactive (4.06%)
TRKC	inactive (5.04%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (21.42%)
MET	inactive (14.91%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-2.9%)
MER	inactive (0.93%)
TYRO3	inactive (2.1%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (34.95%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (6.58%)
FGFR2	inactive (18.4%)
FGFR3	inactive (14.71%)
FGFR4	inactive (7.73%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (2.35%)
KDR	inactive (12.26%)
FLT4	inactive (15.37%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (0.9%)
KIT	inactive (3.87%)
FLT3	inactive (0.62%)
PDGFRa	inactive (10.74%)
PDGFRb	inactive (6.86%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (3.1%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (3.68%)
TNK1	inactive (31.18%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (1.27%)
ErbB2	inactive (-0.74%)
ErbB4	inactive (5.19%)

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 (0.77%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (5.71%)

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 (3.21%)
MST1	inactive (5.91%)
MST2	inactive (6.58%)
MST4	inactive (-0.49%)
HGK	inactive (11.11%)
MINK	inactive (13.01%)
LOK	inactive (5.18%)
PAK1	inactive (9.83%)
PAK3	inactive (1.55%)
PAK2	inactive (-0.03%)
PAK5	inactive (5.58%)
PAK6	inactive (-1.9%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (5.95%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (1.43%)
CK1g2	inactive (1.77%)
CK1g1	inactive (2.31%)
CK1g3	inactive (0.47%)

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 (1.91%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (18.48%)
AurC	inactive (26.95%)
AurA	active (62.71%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (4.56%)
NEK2	inactive (2.73%)
NEK9	inactive (3.09%)
NEK7	inactive (2.72%)
NEK6	inactive (0.71%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (3.11%)
IKKe	inactive (4.43%)
IKKb	inactive (1.73%)
IKKa	inactive (7.79%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (1.11%)

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 (6.49%)
GPRK6	inactive (7.3%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (0.89%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (34.23%)
MSK2	inactive (16.68%)
RSK1	inactive (15.73%)
RSK2	inactive (11.24%)
RSK4	inactive (2.82%)
RSK3	inactive (7.93%)
p70S6K	inactive (13.79%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (1.45%)
AKT1	inactive (0.8%)
AKT3	inactive (2.79%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (7.18%)
SGK3	inactive (6.8%)
SGK2	inactive (4.13%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (10.84%)
PKCg	inactive (2.9%)
PKCa	inactive (0.39%)
PKCt	inactive (3.15%)
PKCi	inactive (1.22%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (12.59%)
PKG1	inactive (20.1%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	active (53.38%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	active (74.33%)
ROCK2	active (74.54%)
MRCKb	inactive (29.95%)
MRCKa	inactive (12.4%)

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 (2.29%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (-0.03%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-0.21%)
CaMK1d	inactive (-0.14%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (4.43%)
PHKg2	inactive (2.08%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (1.35%)
CaMK2a	inactive (0.1%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (0.76%)
MAPKAPK2	inactive (1.87%)
MAPKAPK3	inactive (1.05%)
MNK2	active (65.29%)
MNK1	inactive (46.24%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (7.95%)
PKD1	inactive (8.16%)
PKD2	inactive (8.48%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (4.62%)
MARK3	inactive (8.67%)
MARK1	inactive (9.5%)
QIK	inactive (1.13%)
SIK	inactive (3.8%)
NuaK1	inactive (11.27%)
BRSK1	inactive (8.31%)
BRSK2	inactive (15.5%)
MELK	inactive (6.05%)
CHK1	inactive (4.3%)
PASK	inactive (-0.21%)
AMPKa1	inactive (20.41%)
AMPKa2	inactive (5.96%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (1.4%)
TSSK1	inactive (1.21%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (1.59%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (-0.13%)
PIM3	inactive (-0.69%)
PIM1	inactive (-0.04%)

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 (0.78%)
p38a	inactive (6.99%)
p38b	inactive (3.88%)
p38d	inactive (2.31%)
Erk2	inactive (4.83%)
Erk1	inactive (3.56%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (-0.33%)
GSK3B	inactive (1.6%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-1.24%)
MSSK1	inactive (-0.84%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (1.47%)
CLK2	inactive (0.68%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (-0.69%)
HIPK4	inactive (-0.66%)
DYRK1B	inactive (3.29%)
DYRK1A	inactive (1.58%)
DYRK2	inactive (2.08%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (0.86%)