Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : -

Inchikey : FOTACNUKABBYFV-YVLHZVERSA-N

ChemSpider : 5021549

Pubchem CID : 6539081

	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 (12.66%)
TYK2	inactive (4.42%)
JAK2	inactive (12.3%)
JAK3	inactive (45.55%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (11.13%)
FES	inactive (-0.27%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (36.29%)
ABL2	inactive (20.35%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (-1.85%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (-1.5%)
BTK	inactive (-1.1%)
TXK	inactive (4.75%)
TEC	inactive (6.56%)
ITK	inactive (5.29%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (-2.63%)
SRM	inactive (3.32%)
FRK	inactive (1.92%)
BLK	inactive (28.58%)
LCK	inactive (13.88%)
HCK	inactive (38.5%)
FGR	inactive (31.96%)
FYN	active (71.6%)
SRC	inactive (39.47%)
YES	inactive (22.14%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (-3.24%)
EphA4	inactive (1.79%)
EphA3	inactive (0.31%)
EphB4	inactive (1.51%)
EphB3	inactive (-4.87%)
EphB2	inactive (-4.93%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (16.46%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-2.67%)
ZAP70	inactive (1.21%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (4.2%)
ALK	inactive (4.93%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (15.31%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (2.17%)
IGF1R	inactive (1.72%)
IRR	inactive (0.22%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (2.05%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	active (51.3%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (30.37%)
TRKB	inactive (40.23%)
TRKC	inactive (48.45%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (16.74%)
MET	inactive (13.34%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (13.18%)
MER	inactive (4.37%)
TYRO3	inactive (17.03%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	active (77.99%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (4.86%)
FGFR2	inactive (17.31%)
FGFR3	inactive (10.81%)
FGFR4	inactive (2.26%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (39.39%)
KDR	active (71.49%)
FLT4	active (80.59%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (45.79%)
KIT	inactive (24.65%)
FLT3	active (55.99%)
PDGFRa	active (84.28%)
PDGFRb	active (85.96%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (7.91%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (0.01%)
TNK1	inactive (5.07%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (4.58%)
ErbB2	inactive (-0.17%)
ErbB4	inactive (-2.34%)

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 (0.81%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (32.78%)

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 (14.28%)
MST1	active (81.54%)
MST2	active (77.91%)
MST4	inactive (10.7%)
HGK	active (65.35%)
MINK	active (53.79%)
LOK	inactive (12.59%)
PAK1	inactive (1.52%)
PAK3	inactive (-0.22%)
PAK2	inactive (0.1%)
PAK5	inactive (5.79%)
PAK6	inactive (0.35%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (33.67%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (1.61%)
CK1g2	inactive (14.22%)
CK1g1	inactive (7.57%)
CK1g3	inactive (20.64%)

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 (2.98%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (47.99%)
AurC	active (82.92%)
AurA	active (61%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (2.33%)
NEK2	inactive (0.66%)
NEK9	inactive (0.18%)
NEK7	inactive (0.46%)
NEK6	inactive (9.49%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	active (82.9%)
IKKe	active (93.39%)
IKKb	inactive (6.93%)
IKKa	inactive (3.25%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	active (70.08%)

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 (9.41%)
GPRK6	inactive (10.09%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	active (68.92%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (11.61%)
MSK2	inactive (20.9%)
RSK1	inactive (32.42%)
RSK2	inactive (35.95%)
RSK4	inactive (39.31%)
RSK3	inactive (35.51%)
p70S6K	inactive (18.12%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (1.73%)
AKT1	inactive (2.22%)
AKT3	inactive (6.82%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (19.03%)
SGK3	inactive (3.19%)
SGK2	inactive (1.89%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (1.97%)
PKCg	inactive (9.06%)
PKCa	inactive (7.21%)
PKCt	inactive (7.78%)
PKCi	inactive (1.73%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	active (54.4%)
PKG1	inactive (14.34%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (13.51%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (30.24%)
ROCK2	inactive (43.85%)
MRCKb	inactive (12.66%)
MRCKa	inactive (6.98%)

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 (13.53%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (10.18%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (3.51%)
CaMK1d	inactive (7.89%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	active (50.55%)
PHKg2	inactive (16.43%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (36.69%)
CaMK2a	inactive (17.53%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (1.18%)
MAPKAPK2	inactive (-1.28%)
MAPKAPK3	inactive (-2.61%)
MNK2	inactive (13.9%)
MNK1	inactive (6.56%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (46.27%)
PKD1	active (56%)
PKD2	active (62.07%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	active (77.53%)
MARK3	active (88.65%)
MARK1	active (87.06%)
QIK	inactive (39.66%)
SIK	active (72.24%)
NuaK1	active (75.64%)
BRSK1	inactive (37.99%)
BRSK2	active (50.12%)
MELK	active (93.19%)
CHK1	inactive (18.12%)
PASK	inactive (2.64%)
AMPKa1	active (72.26%)
AMPKa2	inactive (36.3%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (0.83%)
TSSK1	active (50.24%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (3.08%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (5.85%)
PIM3	inactive (48.75%)
PIM1	inactive (27.81%)

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 (10.76%)
p38a	inactive (-2.21%)
p38b	inactive (7.86%)
p38d	inactive (1.38%)
Erk2	inactive (31.34%)
Erk1	inactive (13.5%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	active (80.56%)
GSK3B	active (82.73%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-1.99%)
MSSK1	inactive (-1.97%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (11.37%)
CLK2	active (72.17%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (16.84%)
HIPK4	inactive (16.95%)
DYRK1B	active (53.94%)
DYRK1A	active (57.05%)
DYRK2	inactive (22.35%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (47.22%)