Compound in Profiling

Compound Information

Test on : GPCR

Compound Name : CHEMBL524901

Inchikey : ZRWNCIWVANTRGL-UHFFFAOYSA-N

ChemSpider : 8368982

Pubchem CID : 10193482

ChEMBL : CHEMBL524901

	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 (4.8%)
TYK2	inactive (-3.09%)
JAK2	inactive (1.4%)
JAK3	inactive (-2.75%)

TK - Fer

Bioactivity
Kinase	GPCR
FER	inactive (1.85%)
FES	inactive (5.72%)

TK - Abl

Bioactivity
Kinase	GPCR
ABL1	inactive (6.5%)
ABL2	inactive (1.19%)

TK - Csk

Bioactivity
Kinase	GPCR
CSK	inactive (1.9%)

TK - Tec

Bioactivity
Kinase	GPCR
BMX	inactive (2.01%)
BTK	inactive (-2.44%)
TXK	inactive (-0.63%)
TEC	inactive (3.12%)
ITK	inactive (0.08%)

TK - Src

Bioactivity
Kinase	GPCR
BRK	inactive (3.25%)
SRM	inactive (1.41%)
FRK	inactive (0.39%)
BLK	inactive (2.58%)
LCK	inactive (1.64%)
HCK	inactive (6.17%)
FGR	inactive (0.54%)
FYN	inactive (3.59%)
SRC	inactive (5.93%)
YES	inactive (0.1%)

TK - Eph

Bioactivity
Kinase	GPCR
EphA2	inactive (-1.53%)
EphA4	inactive (5.87%)
EphA3	inactive (6.16%)
EphB4	inactive (1.07%)
EphB3	inactive (3.37%)
EphB2	inactive (9.04%)

TK - FAK

Bioactivity
Kinase	GPCR
PYK2	inactive (6.44%)

TK - Syk

Bioactivity
Kinase	GPCR
SYK	inactive (0.5%)
ZAP70	inactive (2.9%)

TK - ALK

Bioactivity
Kinase	GPCR
LTK	inactive (2.33%)
ALK	inactive (3.78%)

TK - Sev

Bioactivity
Kinase	GPCR
ROS	inactive (8.64%)

TK - InsR

Bioactivity
Kinase	GPCR
INSR	inactive (4.01%)
IGF1R	inactive (1.61%)
IRR	inactive (0.25%)

TK - DDR

Bioactivity
Kinase	GPCR
DDR2	inactive (1.44%)

TK - Musk

Bioactivity
Kinase	GPCR
MUSK	inactive (0.6%)

TK - Trk

Bioactivity
Kinase	GPCR
TRKA	inactive (1.75%)
TRKB	inactive (1.35%)
TRKC	inactive (2.63%)

TK - Met

Bioactivity
Kinase	GPCR
RON	inactive (0.88%)
MET	inactive (0.15%)

TK - Axl

Bioactivity
Kinase	GPCR
AXL	inactive (-4.37%)
MER	inactive (-0.16%)
TYRO3	inactive (2.64%)

TK - Ret

Bioactivity
Kinase	GPCR
RET	inactive (0.87%)

TK - FGFR

Bioactivity
Kinase	GPCR
FGFR1	inactive (2.22%)
FGFR2	inactive (3.87%)
FGFR3	inactive (1.83%)
FGFR4	inactive (2.53%)

TK - VEGFR

Bioactivity
Kinase	GPCR
FLT1	inactive (0.94%)
KDR	inactive (6.83%)
FLT4	inactive (0.07%)

TK - PDGFR

Bioactivity
Kinase	GPCR
FMS	inactive (5.17%)
KIT	inactive (5.88%)
FLT3	inactive (1.48%)
PDGFRa	inactive (6.66%)
PDGFRb	inactive (4.61%)

TK - Tie

Bioactivity
Kinase	GPCR
TIE2	inactive (3.09%)

TK - Ack

Bioactivity
Kinase	GPCR
ACK	inactive (-0.49%)
TNK1	inactive (-1.51%)

TK - EGFR

Bioactivity
Kinase	GPCR
EGFR	inactive (0.23%)
ErbB2	inactive (-0.02%)
ErbB4	inactive (8.49%)

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 (1.39%)

TKL - RAF

Bioactivity
Kinase	GPCR
BRAF	inactive (7.07%)

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 (1.94%)
MST1	inactive (1.9%)
MST2	inactive (2.29%)
MST4	inactive (-2.39%)
HGK	inactive (8.87%)
MINK	inactive (12.13%)
LOK	inactive (1.98%)
PAK1	inactive (4.03%)
PAK3	inactive (3.78%)
PAK2	inactive (0.34%)
PAK5	inactive (1.01%)
PAK6	inactive (-5.92%)

STE - STE7

Bioactivity
Kinase	GPCR
MAP2K1	inactive (3.9%)

CK1

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

CK1 - CK1

Bioactivity
Kinase	GPCR
CK1a	inactive (16.38%)
CK1g2	inactive (5.14%)
CK1g1	inactive (4.83%)
CK1g3	inactive (4.33%)

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 (3.55%)

Other - Aur

Bioactivity
Kinase	GPCR
AurB	inactive (5.43%)
AurC	inactive (1.86%)
AurA	inactive (8.82%)

Other - NEK

Bioactivity
Kinase	GPCR
NEK1	inactive (0.27%)
NEK2	inactive (4.3%)
NEK9	inactive (9.51%)
NEK7	inactive (1.47%)
NEK6	inactive (2.66%)

Other - IKK

Bioactivity
Kinase	GPCR
TBK1	inactive (1.95%)
IKKe	inactive (13.44%)
IKKb	inactive (4.44%)
IKKa	inactive (9.01%)

Other - TTK

Bioactivity
Kinase	GPCR
TTK	inactive (8.22%)

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 (15.49%)
GPRK6	inactive (3.86%)

AGC - PDK1

Bioactivity
Kinase	GPCR
PDK1	inactive (1.47%)

AGC - RSK

Bioactivity
Kinase	GPCR
MSK1	inactive (6.41%)
MSK2	inactive (7.41%)
RSK1	inactive (4.45%)
RSK2	inactive (2.86%)
RSK4	inactive (0.49%)
RSK3	inactive (3.97%)
p70S6K	inactive (2.73%)

AGC - Akt

Bioactivity
Kinase	GPCR
AKT2	inactive (1.85%)
AKT1	inactive (0.29%)
AKT3	inactive (1.68%)

AGC - SGK

Bioactivity
Kinase	GPCR
SGK1	inactive (3.79%)
SGK3	inactive (8.34%)
SGK2	inactive (5.05%)

AGC - PKC

Bioactivity
Kinase	GPCR
PKCh	inactive (2.05%)
PKCg	inactive (4.8%)
PKCa	inactive (2.26%)
PKCt	inactive (2.41%)
PKCi	inactive (4.4%)

AGC - PKG

Bioactivity
Kinase	GPCR
PKG2	inactive (4.91%)
PKG1	inactive (8.93%)

AGC - PKA

Bioactivity
Kinase	GPCR
PRKX	inactive (3.97%)

AGC - DMPK

Bioactivity
Kinase	GPCR
ROCK1	inactive (4.7%)
ROCK2	inactive (4.16%)
MRCKb	inactive (3.84%)
MRCKa	inactive (-2.56%)

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 (3.47%)

CAMK - DCAMKL

Bioactivity
Kinase	GPCR
DCLK2	inactive (1.43%)

CAMK - CAMK1

Bioactivity
Kinase	GPCR
CaMK4	inactive (-0.41%)
CaMK1d	inactive (-0.17%)

CAMK - PHK

Bioactivity
Kinase	GPCR
PHKg1	inactive (4.16%)
PHKg2	inactive (2.46%)

CAMK - CAMK2

Bioactivity
Kinase	GPCR
CaMK2d	inactive (3.72%)
CaMK2a	inactive (6.81%)

CAMK - MAPKAPK

Bioactivity
Kinase	GPCR
MAPKAPK5	inactive (1.07%)
MAPKAPK2	inactive (2.19%)
MAPKAPK3	inactive (4.86%)
MNK2	inactive (7.83%)
MNK1	inactive (10.91%)

CAMK - PKD

Bioactivity
Kinase	GPCR
PKD3	inactive (5%)
PKD1	inactive (5.95%)
PKD2	inactive (5.4%)

CAMK - CAMKL

Bioactivity
Kinase	GPCR
MARK4	inactive (2.05%)
MARK3	inactive (-0.34%)
MARK1	inactive (5.05%)
QIK	inactive (2.87%)
SIK	inactive (6.56%)
NuaK1	inactive (0.6%)
BRSK1	inactive (1.97%)
BRSK2	inactive (1.28%)
MELK	inactive (11.89%)
CHK1	inactive (1.83%)
PASK	inactive (-2.98%)
AMPKa1	inactive (2.5%)
AMPKa2	inactive (2.36%)

CAMK - TSSK

Bioactivity
Kinase	GPCR
TSSK2	inactive (1.85%)
TSSK1	inactive (2.58%)

CAMK - DAPK

Bioactivity
Kinase	GPCR
DAPK1	inactive (-0.07%)

CAMK - PIM

Bioactivity
Kinase	GPCR
PIM2	inactive (-1.06%)
PIM3	inactive (-0.85%)
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 (5.01%)
p38a	inactive (8.35%)
p38b	inactive (4.06%)
p38d	inactive (4.03%)
Erk2	inactive (4.35%)
Erk1	inactive (0.61%)

CMGC - GSK

Bioactivity
Kinase	GPCR
GSK3A	inactive (13.09%)
GSK3B	inactive (13.01%)

CMGC - SRPK

Bioactivity
Kinase	GPCR
SRPK1	inactive (-3.38%)
MSSK1	inactive (-0.57%)

CMGC - CLK

Bioactivity
Kinase	GPCR
CLK3	inactive (0.72%)
CLK2	inactive (6.81%)

CMGC - DYRK

Bioactivity
Kinase	GPCR
HIPK1	inactive (6.02%)
HIPK4	inactive (3.35%)
DYRK1B	inactive (40.27%)
DYRK1A	inactive (33.91%)
DYRK2	inactive (5.39%)

CMGC - CK2

Bioactivity
Kinase	GPCR
CK2a1	inactive (4.66%)