Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : CHEMBL232601

Inchikey : KTBZRPANEUUZDW-UHFFFAOYSA-N

ChemSpider : 17597910

Pubchem CID : 16664858

ChEMBL : CHEMBL232601

	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 (16.11%)
TYK2	inactive (-5.1%)
JAK2	inactive (0.95%)
JAK3	inactive (-1.26%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (8.05%)
FES	inactive (3.74%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (4.12%)
ABL2	inactive (-0.56%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (8.34%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (4.07%)
BTK	inactive (-0.86%)
TXK	inactive (2.43%)
TEC	inactive (4.6%)
ITK	inactive (0.96%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (3.25%)
SRM	inactive (-2.85%)
FRK	inactive (0.68%)
BLK	inactive (3.38%)
LCK	inactive (3.44%)
HCK	inactive (4.14%)
FGR	inactive (-0.28%)
FYN	inactive (4.09%)
SRC	inactive (8.09%)
YES	inactive (6.86%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (1.34%)
EphA4	inactive (13.1%)
EphA3	inactive (3.68%)
EphB4	inactive (1.48%)
EphB3	inactive (4.98%)
EphB2	inactive (10.24%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (10.04%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (-1.27%)
ZAP70	inactive (6.58%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (4.13%)
ALK	inactive (8.17%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (10.49%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (3.55%)
IGF1R	inactive (11.26%)
IRR	inactive (3.44%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (3.01%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (4.4%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (2.43%)
TRKB	inactive (7.68%)
TRKC	inactive (5.7%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (7.21%)
MET	inactive (4.48%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-9.25%)
MER	inactive (2.51%)
TYRO3	inactive (4.86%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (5.21%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (5.7%)
FGFR2	inactive (5.8%)
FGFR3	inactive (5.57%)
FGFR4	inactive (2.01%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (0.98%)
KDR	inactive (5.2%)
FLT4	inactive (18.63%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (2.49%)
KIT	inactive (9.61%)
FLT3	inactive (-0.34%)
PDGFRa	inactive (10.65%)
PDGFRb	inactive (5.33%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (3.83%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (2.46%)
TNK1	inactive (8.89%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (9.92%)
ErbB2	inactive (12.24%)
ErbB4	inactive (15.87%)

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 (2.28%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (6.32%)

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 (1.18%)
MST1	inactive (7.53%)
MST2	inactive (8.14%)
MST4	inactive (-0.29%)
HGK	inactive (7.77%)
MINK	inactive (8.88%)
LOK	inactive (12.04%)
PAK1	inactive (8.31%)
PAK3	inactive (6.13%)
PAK2	inactive (1.96%)
PAK5	inactive (-0.7%)
PAK6	inactive (1.74%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (5.16%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (2.23%)
CK1g2	inactive (5.09%)
CK1g1	inactive (6.2%)
CK1g3	inactive (5.46%)

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 (3.25%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (5.23%)
AurC	inactive (-6.13%)
AurA	inactive (3.45%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (4.61%)
NEK2	inactive (6.43%)
NEK9	inactive (10.07%)
NEK7	inactive (3.65%)
NEK6	inactive (3.58%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (5.06%)
IKKe	inactive (9.83%)
IKKb	inactive (9.09%)
IKKa	inactive (10.61%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (13.62%)

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 (11.26%)
GPRK6	inactive (11.12%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (-1.14%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (6.5%)
MSK2	inactive (2.3%)
RSK1	inactive (5.31%)
RSK2	inactive (1.98%)
RSK4	inactive (1.61%)
RSK3	inactive (2.17%)
p70S6K	inactive (1.93%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (2.46%)
AKT1	inactive (0.38%)
AKT3	inactive (1.48%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (7.28%)
SGK3	inactive (5.12%)
SGK2	inactive (5.78%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (6.37%)
PKCg	inactive (7.29%)
PKCa	inactive (0.67%)
PKCt	inactive (4.93%)
PKCi	inactive (1.46%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (3.03%)
PKG1	inactive (6.4%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (4.96%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (0.58%)
ROCK2	inactive (5.99%)
MRCKb	inactive (-1.24%)
MRCKa	inactive (2.68%)

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 (7.74%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (1.25%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-4.58%)
CaMK1d	inactive (-0.72%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (9.29%)
PHKg2	inactive (10.29%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (2.98%)
CaMK2a	inactive (2.77%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (3.73%)
MAPKAPK2	inactive (3.91%)
MAPKAPK3	inactive (4.91%)
MNK2	inactive (4.47%)
MNK1	inactive (7.18%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (7.33%)
PKD1	inactive (6.2%)
PKD2	inactive (5.88%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (2.14%)
MARK3	inactive (6.18%)
MARK1	inactive (6.78%)
QIK	inactive (9.59%)
SIK	inactive (5.66%)
NuaK1	inactive (-1.33%)
BRSK1	inactive (1.42%)
BRSK2	inactive (2.15%)
MELK	inactive (2.88%)
CHK1	inactive (7.12%)
PASK	inactive (1.32%)
AMPKa1	inactive (5.81%)
AMPKa2	inactive (4.32%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (5.4%)
TSSK1	inactive (6.62%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (10.75%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (1.37%)
PIM3	inactive (1.23%)
PIM1	inactive (0.05%)

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 (33.6%)
p38a	inactive (8.41%)
p38b	inactive (5.81%)
p38d	inactive (4.94%)
Erk2	inactive (5.52%)
Erk1	inactive (6.36%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (1.54%)
GSK3B	inactive (1.14%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (2.96%)
MSSK1	inactive (-1.29%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (2.19%)
CLK2	inactive (2.24%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (3.2%)
HIPK4	inactive (5.48%)
DYRK1B	inactive (0.51%)
DYRK1A	inactive (4.26%)
DYRK2	inactive (4.05%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (8.12%)