Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : -

Inchikey : LTYGAJVXAFJKSY-UHFFFAOYSA-N

ChemSpider : 26639372

Pubchem CID : 53239967

	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 (26.78%)
TYK2	inactive (40.98%)
JAK2	inactive (11.09%)
JAK3	active (54.36%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (13.06%)
FES	inactive (7.01%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (32.91%)
ABL2	inactive (21.77%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (3.86%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (6.44%)
BTK	inactive (0.29%)
TXK	inactive (10.81%)
TEC	inactive (10.64%)
ITK	inactive (8.24%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (4.82%)
SRM	inactive (-1.72%)
FRK	inactive (3.93%)
BLK	inactive (36.72%)
LCK	inactive (13.21%)
HCK	inactive (28.91%)
FGR	inactive (21.55%)
FYN	inactive (9.66%)
SRC	inactive (42.86%)
YES	inactive (26.68%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (1.66%)
EphA4	inactive (22.41%)
EphA3	inactive (6.86%)
EphB4	inactive (8.11%)
EphB3	inactive (4.36%)
EphB2	inactive (18.14%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (43.63%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-8.48%)
ZAP70	inactive (5.97%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (10.43%)
ALK	inactive (15.06%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (17.01%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (11.72%)
IGF1R	inactive (19.44%)
IRR	inactive (4.17%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (3.5%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	active (51.18%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	active (51.33%)
TRKB	active (65.89%)
TRKC	active (66.93%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (39.25%)
MET	inactive (43.33%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (24.67%)
MER	inactive (7.72%)
TYRO3	inactive (24.08%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	active (71.26%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (32.78%)
FGFR2	active (53.31%)
FGFR3	active (56.67%)
FGFR4	inactive (5.81%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	active (50.58%)
KDR	active (75.26%)
FLT4	active (93.12%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	active (58.61%)
KIT	active (90.03%)
FLT3	active (79.51%)
PDGFRa	active (86.87%)
PDGFRb	active (86.76%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (10.44%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (1.83%)
TNK1	inactive (37.81%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (5.22%)
ErbB2	inactive (5.6%)
ErbB4	inactive (10.82%)

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 (2.58%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (40.97%)

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 (52.08%)
MST1	active (75.19%)
MST2	active (73.72%)
MST4	active (74.47%)
HGK	active (76.91%)
MINK	active (76.86%)
LOK	inactive (16.23%)
PAK1	inactive (7.33%)
PAK3	inactive (5.62%)
PAK2	inactive (2.66%)
PAK5	inactive (4.51%)
PAK6	inactive (-3.07%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (42.86%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (14.65%)
CK1g2	inactive (11.06%)
CK1g1	inactive (9.59%)
CK1g3	inactive (14.4%)

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 (4.96%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	active (55.23%)
AurC	active (79.21%)
AurA	active (80.23%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (3.28%)
NEK2	inactive (8.52%)
NEK9	inactive (22.37%)
NEK7	inactive (7.53%)
NEK6	inactive (4.37%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (46.7%)
IKKe	inactive (41.92%)
IKKb	inactive (13.07%)
IKKa	inactive (14.29%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	active (62.37%)

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 (6.58%)
GPRK6	inactive (18.69%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	active (65.2%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (12.16%)
MSK2	active (50.85%)
RSK1	inactive (31.34%)
RSK2	inactive (36.03%)
RSK4	active (59.88%)
RSK3	active (66.09%)
p70S6K	inactive (13.53%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (2.38%)
AKT1	inactive (0.61%)
AKT3	inactive (3.15%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (47.5%)
SGK3	inactive (10.2%)
SGK2	inactive (18.44%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (6.53%)
PKCg	inactive (5.52%)
PKCa	inactive (3.04%)
PKCt	inactive (6.57%)
PKCi	inactive (2.78%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (47.92%)
PKG1	inactive (16.68%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (6.55%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (32.98%)
ROCK2	inactive (47.46%)
MRCKb	inactive (5.66%)
MRCKa	inactive (10.53%)

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 (19.08%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (5.55%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-1.06%)
CaMK1d	inactive (0.92%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (47.56%)
PHKg2	inactive (19.81%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (16.32%)
CaMK2a	inactive (3.49%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (7.16%)
MAPKAPK2	inactive (2.48%)
MAPKAPK3	inactive (10.43%)
MNK2	inactive (10.53%)
MNK1	inactive (23.97%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	active (54.21%)
PKD1	active (67.28%)
PKD2	active (58.25%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (46.34%)
MARK3	inactive (42.94%)
MARK1	active (53.76%)
QIK	inactive (25.81%)
SIK	inactive (20.97%)
NuaK1	active (69.1%)
BRSK1	active (53.09%)
BRSK2	active (62.41%)
MELK	active (89.47%)
CHK1	inactive (33.02%)
PASK	inactive (0.4%)
AMPKa1	active (59.86%)
AMPKa2	inactive (42.78%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (2.94%)
TSSK1	inactive (19.35%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (9.33%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (1.21%)
PIM3	inactive (4.12%)
PIM1	inactive (4.82%)

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 (20.24%)
p38a	inactive (23.38%)
p38b	inactive (14.97%)
p38d	inactive (4.84%)
Erk2	inactive (31.15%)
Erk1	inactive (15.26%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	active (62.8%)
GSK3B	active (65.14%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-2.8%)
MSSK1	inactive (0.72%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (9.47%)
CLK2	active (64.14%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (34.68%)
HIPK4	inactive (11.79%)
DYRK1B	inactive (44.92%)
DYRK1A	active (74.43%)
DYRK2	inactive (29.04%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (27.99%)