Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : -

Inchikey : XHBOHQMIFHBKMM-GDNBJRDFSA-N

ChemSpider : 5021543

Pubchem CID : 6539075

	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 (14.2%)
TYK2	inactive (17.16%)
JAK2	inactive (2.09%)
JAK3	inactive (20.42%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (8.18%)
FES	inactive (0.4%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (21.33%)
ABL2	inactive (4.52%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (0.76%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (1.7%)
BTK	inactive (-0.24%)
TXK	inactive (4.14%)
TEC	inactive (2.35%)
ITK	inactive (3.68%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (2.14%)
SRM	inactive (3.48%)
FRK	inactive (2.09%)
BLK	inactive (33.16%)
LCK	inactive (12.72%)
HCK	inactive (20.49%)
FGR	inactive (16.69%)
FYN	inactive (13.05%)
SRC	inactive (27.38%)
YES	inactive (14.31%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (-2.52%)
EphA4	inactive (1.13%)
EphA3	inactive (3.13%)
EphB4	inactive (3.08%)
EphB3	inactive (1.83%)
EphB2	inactive (5.77%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (31.68%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (0.31%)
ZAP70	inactive (5.7%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (2.8%)
ALK	inactive (8.32%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (8.86%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (6.31%)
IGF1R	inactive (11.87%)
IRR	inactive (3.14%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (2.54%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (46.81%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (46.22%)
TRKB	active (65.2%)
TRKC	active (73.06%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (7.23%)
MET	inactive (4.48%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (14.82%)
MER	inactive (10.83%)
TYRO3	inactive (7.48%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	active (51.54%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (15.35%)
FGFR2	inactive (31.56%)
FGFR3	inactive (29.56%)
FGFR4	inactive (3.82%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (12.59%)
KDR	active (53.59%)
FLT4	active (55.05%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (18.81%)
KIT	inactive (28.38%)
FLT3	inactive (17.72%)
PDGFRa	active (66.91%)
PDGFRb	active (71.29%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (5.59%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (1.79%)
TNK1	inactive (5.7%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (11.92%)
ErbB2	inactive (3.44%)
ErbB4	inactive (7.65%)

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 (0.86%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (4.91%)

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 (29.85%)
MST1	active (71.66%)
MST2	active (67.98%)
MST4	inactive (20.2%)
HGK	active (69.98%)
MINK	active (63.63%)
LOK	inactive (18.11%)
PAK1	inactive (2.53%)
PAK3	inactive (2.05%)
PAK2	inactive (0.6%)
PAK5	inactive (-4.48%)
PAK6	inactive (-1.53%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (6.25%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (2.88%)
CK1g2	inactive (1.27%)
CK1g1	inactive (1.57%)
CK1g3	inactive (0.92%)

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 (2.41%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (30.35%)
AurC	inactive (47.98%)
AurA	active (50.73%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (2.38%)
NEK2	inactive (3.05%)
NEK9	inactive (4.93%)
NEK7	inactive (3.01%)
NEK6	inactive (2.13%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (49.74%)
IKKe	inactive (23.1%)
IKKb	inactive (1.1%)
IKKa	inactive (6.64%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (12.54%)

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 (8.73%)
GPRK6	inactive (5.15%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (23.79%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (4.05%)
MSK2	inactive (3.55%)
RSK1	inactive (11.64%)
RSK2	inactive (14.73%)
RSK4	inactive (20.92%)
RSK3	inactive (25.92%)
p70S6K	inactive (3.09%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (1.06%)
AKT1	inactive (-0.46%)
AKT3	inactive (1.85%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (5.38%)
SGK3	inactive (-1.85%)
SGK2	inactive (-1.11%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (2.17%)
PKCg	inactive (2.72%)
PKCa	inactive (1.56%)
PKCt	inactive (0.84%)
PKCi	inactive (1.5%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (8.65%)
PKG1	inactive (1.76%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (2.58%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (5.77%)
ROCK2	inactive (13.31%)
MRCKb	inactive (2.85%)
MRCKa	inactive (4.01%)

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 (10.61%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (5.58%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (0.42%)
CaMK1d	inactive (4.29%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (49.29%)
PHKg2	inactive (13.82%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (14.98%)
CaMK2a	inactive (3.56%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (0.46%)
MAPKAPK2	inactive (1.33%)
MAPKAPK3	inactive (-0.05%)
MNK2	inactive (3.67%)
MNK1	inactive (9.3%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (4.44%)
PKD1	inactive (7.78%)
PKD2	inactive (5.28%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (32.45%)
MARK3	inactive (32.72%)
MARK1	inactive (36.35%)
QIK	inactive (18.18%)
SIK	inactive (14.72%)
NuaK1	active (55.6%)
BRSK1	inactive (42.71%)
BRSK2	active (54.24%)
MELK	inactive (20.35%)
CHK1	inactive (34.87%)
PASK	inactive (-0.69%)
AMPKa1	inactive (44.51%)
AMPKa2	inactive (26.8%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (1.25%)
TSSK1	inactive (9.92%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (1.27%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (1.18%)
PIM3	inactive (0.56%)
PIM1	inactive (1.23%)

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 (2.71%)
p38a	inactive (2.39%)
p38b	inactive (0.72%)
p38d	inactive (1.98%)
Erk2	inactive (2.53%)
Erk1	inactive (2.21%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (21.64%)
GSK3B	inactive (24.17%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-2.04%)
MSSK1	inactive (-1.04%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (3.39%)
CLK2	inactive (10.98%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (12.02%)
HIPK4	inactive (6.94%)
DYRK1B	inactive (24.48%)
DYRK1A	inactive (33.44%)
DYRK2	inactive (4.74%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (18.01%)