Compound in Profiling

Compound Information

Test on : RBC

Compound Name : CGP 57380

Inchikey : UQPMANVRZYYQMD-UHFFFAOYSA-N

ChemSpider : 9819164

Pubchem CID : 11644425

ChEMBL : CHEMBL1240885

	DRx	RBC	Metz	Millipore	GPCR
bioactivity	Kd (nM)	Remain Activity (%)	Ki (nM)	Remain Activity (%)	Inhibition (%)
active criteria	<3000nM	<50%	<1000nM	<50%	>50%

AGC

Test Member No. in Family
Family	no. Member on 518kinase	RBC
PDK1	1	1
Akt	3	3
DMPK	7	5
GRK	7	6
RSK	8	8
PKA	5	3
PKC	9	9
PKG	2	3
PKN	3	2
SGK	3	3
NDR	4	1

AGC - PDK1

Bioactivity
Kinase	RBC
PDK1	inactive (102.4%)

AGC - Akt

Bioactivity
Kinase	RBC
AKT1	inactive (93.3%)
AKT2	inactive (107.9%)
AKT3	inactive (104.45%)

AGC - DMPK

Bioactivity
Kinase	RBC
DMPK1	inactive (114.39%)
MRCKa	inactive (102.85%)
MRCKb	inactive (105.84%)
ROCK1	inactive (100.38%)
ROCK2	inactive (92.12%)

AGC - GRK

Bioactivity
Kinase	RBC
BARK1	inactive (98.62%)
BARK2	inactive (101.84%)
GPRK4	inactive (98.8%)
GPRK5	inactive (97.08%)
GPRK6	inactive (102.86%)
GPRK7	inactive (104.81%)

AGC - RSK

Bioactivity
Kinase	RBC
MSK1	inactive (96.67%)
MSK2	inactive (113.57%)
p70S6K	inactive (94.26%)
p70S6Kb	inactive (96.77%)
RSK2	inactive (89.82%)
RSK4	inactive (71.7%)
RSK1	inactive (82.17%)
RSK3	inactive (70.57%)

AGC - PKA

Bioactivity
Kinase	RBC
PKACg	inactive (96.24%)
PRKX	inactive (90.37%)
PKACa	inactive (96.76%)

AGC - PKC

Bioactivity
Kinase	RBC
PKCa	inactive (98.02%)
PKCd	inactive (111.69%)
PKCe	inactive (99.49%)
PKCh	inactive (84.67%)
PKCg	inactive (95.97%)
PKCi	inactive (91.28%)
PKCt	inactive (102.58%)
PKCz	inactive (108.6%)
PKCb	inactive (104.98%)

AGC - PKG

Bioactivity
Kinase	RBC
PKG2	inactive (97.03%)
PKG1	inactive (95.72%)

AGC - PKN

Bioactivity
Kinase	RBC
PKN1	inactive (102.13%)
PKN2	inactive (81.98%)

AGC - SGK

Bioactivity
Kinase	RBC
SGK1	inactive (91.51%)
SGK2	inactive (96.47%)
SGK3	inactive (102.11%)

AGC - NDR

Bioactivity
Kinase	RBC
NDR1	inactive (101.29%)

TK

Test Member No. in Family
Family	no. Member on 518kinase	RBC
Abl	2	2
Ack	2	1
ALK	2	2
Axl	3	3
Src	11	11
Tec	5	5
PDGFR	5	5
Csk	2	2
DDR	2	1
EGFR	4	3
Eph	14	12
FAK	2	2
Fer	2	2
FGFR	4	4
VEGFR	3	3
InsR	3	3
JakA	4	4
Musk	1	1
Ret	1	1
Met	2	2
Sev	1	1
Syk	2	2
Tie	2	1
Trk	3	3

TK - Abl

Bioactivity
Kinase	RBC
ABL1	inactive (88.09%)
ABL2	inactive (82.27%)

TK - Ack

Bioactivity
Kinase	RBC
ACK	inactive (61.53%)

TK - ALK

Bioactivity
Kinase	RBC
ALK	inactive (88.92%)
LTK	inactive (92.46%)

TK - Axl

Bioactivity
Kinase	RBC
AXL	active (45.4%)
MER	inactive (90.72%)
TYRO3	inactive (100.03%)

TK - Src

Bioactivity
Kinase	RBC
BLK	inactive (100.71%)
BRK	inactive (68.25%)
SRC	inactive (89.59%)
FGR	inactive (89.46%)
FRK	inactive (90.03%)
FYN	inactive (93.01%)
HCK	inactive (90.71%)
LCK	inactive (98.3%)
SRM	inactive (103.56%)
YES	inactive (92.87%)
LYN	inactive (89.73%)

TK - Tec

Bioactivity
Kinase	RBC
BMX	inactive (89.55%)
BTK	inactive (82.28%)
ITK	inactive (93.91%)
TEC	inactive (86.04%)
TXK	inactive (67.56%)

TK - PDGFR

Bioactivity
Kinase	RBC
KIT	inactive (93.54%)
FLT3	inactive (78.35%)
FMS	inactive (101.35%)
PDGFRb	inactive (97.98%)
PDGFRa	inactive (101.38%)

TK - Csk

Bioactivity
Kinase	RBC
CSK	inactive (80.21%)
CTK	inactive (95.63%)

TK - DDR

Bioactivity
Kinase	RBC
DDR2	inactive (94.2%)

TK - EGFR

Bioactivity
Kinase	RBC
EGFR	inactive (100.39%)
ErbB2	inactive (100.84%)
ErbB4	inactive (120.87%)

TK - Eph

Bioactivity
Kinase	RBC
EphA1	inactive (101.02%)
EphA2	inactive (89.86%)
EphA3	inactive (107.06%)
EphA4	inactive (90.1%)
EphA5	inactive (87.05%)
EphA6	active (49.32%)
EphA7	inactive (101.14%)
EphA8	inactive (94.03%)
EphB1	inactive (87.05%)
EphB2	inactive (91.56%)
EphB3	inactive (87.72%)
EphB4	inactive (87.78%)

TK - FAK

Bioactivity
Kinase	RBC
FAK	inactive (103.08%)
PYK2	inactive (101.44%)

TK - Fer

Bioactivity
Kinase	RBC
FER	inactive (100.11%)
FES	inactive (100.04%)

TK - FGFR

Bioactivity
Kinase	RBC
FGFR1	inactive (91.24%)
FGFR2	inactive (97.16%)
FGFR3	inactive (101.44%)
FGFR4	inactive (107.47%)

TK - VEGFR

Bioactivity
Kinase	RBC
FLT1	inactive (87.3%)
FLT4	inactive (92.91%)
KDR	inactive (104.41%)

TK - InsR

Bioactivity
Kinase	RBC
IGF1R	inactive (103.53%)
IRR	inactive (96.93%)
INSR	inactive (98.5%)

TK - JakA

Bioactivity
Kinase	RBC
JAK1	inactive (98.98%)
JAK2	inactive (105.03%)
JAK3	inactive (102.19%)
TYK2	inactive (92.28%)

TK - Musk

Bioactivity
Kinase	RBC
MUSK	inactive (93.86%)

TK - Ret

Bioactivity
Kinase	RBC
RET	inactive (78.13%)

TK - Met

Bioactivity
Kinase	RBC
RON	inactive (93.74%)
MET	inactive (124.12%)

TK - Sev

Bioactivity
Kinase	RBC
ROS	inactive (99.85%)

TK - Syk

Bioactivity
Kinase	RBC
SYK	inactive (97.4%)
ZAP70	inactive (95.2%)

TK - Tie

Bioactivity
Kinase	RBC
TIE2	inactive (94.92%)

TK - Trk

Bioactivity
Kinase	RBC
TRKA	inactive (108.72%)
TRKB	inactive (100.94%)
TRKC	inactive (81.54%)

TKL

Test Member No. in Family
Family	no. Member on 518kinase	RBC
STKR	12	5
RAF	5	3
IRAK	4	2
LISK	4	1
LRRK	2	1
MLK	10	5
RIPK	5	1

TKL - STKR

Bioactivity
Kinase	RBC
ALK1	inactive (107.87%)
ALK2	inactive (127.22%)
ALK4	inactive (104.25%)
TGFbR1	-
TGFbR2	inactive (100.63%)

TKL - RAF

Bioactivity
Kinase	RBC
ARAF	inactive (80.68%)
BRAF	inactive (91.69%)
RAF1	inactive (96.71%)

TKL - IRAK

Bioactivity
Kinase	RBC
IRAK1	inactive (91.83%)
IRAK4	inactive (88.25%)

TKL - LISK

Bioactivity
Kinase	RBC
LIMK1	inactive (95.25%)

TKL - LRRK

Bioactivity
Kinase	RBC
LRRK2	inactive (89.63%)

TKL - MLK

Bioactivity
Kinase	RBC
MLK1	inactive (99.99%)
MLK2	inactive (85.94%)
MLK3	inactive (93.86%)
TAK1	inactive (99.95%)
ZAK	inactive (88%)

TKL - RIPK

Bioactivity
Kinase	RBC
RIPK2	inactive (68.67%)

CAMK

Test Member No. in Family
Family	no. Member on 518kinase	RBC
CAMKL	20	13
CAMK1	5	5
CAMK2	4	4
RAD53	1	1
DAPK	5	4
DCAMKL	3	1
MAPKAPK	5	5
MLCK	5	2
PHK	2	2
PIM	3	3
PKD	3	3
TSSK	5	2
STK33	1	-

CAMK - CAMKL

Bioactivity
Kinase	RBC
NuaK1	inactive (95.47%)
BRSK1	inactive (63.05%)
BRSK2	inactive (60.58%)
CHK1	inactive (87.98%)
LKB1	inactive (97.07%)
MARK1	inactive (93.76%)
MARK3	inactive (92.52%)
MARK4	inactive (99.45%)
MELK	inactive (97.69%)
PASK	inactive (91.78%)
QIK	inactive (78.71%)
NuaK2	inactive (90.36%)
MARK2	inactive (87%)

CAMK - CAMK1

Bioactivity
Kinase	RBC
CaMK1a	inactive (103.34%)
CaMK1b	inactive (98.39%)
CaMK1d	inactive (130.27%)
CaMK1g	inactive (97.18%)
CaMK4	inactive (103.48%)

CAMK - CAMK2

Bioactivity
Kinase	RBC
CaMK2a	inactive (104.54%)
CaMK2b	inactive (97.68%)
CaMK2d	inactive (92.45%)
CaMK2g	inactive (119.1%)

CAMK - RAD53

Bioactivity
Kinase	RBC
CHK2	inactive (98.61%)

CAMK - DAPK

Bioactivity
Kinase	RBC
DAPK1	inactive (115.51%)
DAPK2	inactive (85.51%)
DRAK1	inactive (88.06%)
DAPK3	inactive (124.25%)

CAMK - DCAMKL

Bioactivity
Kinase	RBC
DCLK2	inactive (99.54%)

CAMK - MAPKAPK

Bioactivity
Kinase	RBC
MAPKAPK2	inactive (104.78%)
MAPKAPK3	inactive (94%)
MAPKAPK5	inactive (80.94%)
MNK1	inactive (75.23%)
MNK2	inactive (72.35%)

CAMK - MLCK

Bioactivity
Kinase	RBC
smMLCK	inactive (94.71%)
skMLCK	inactive (87.35%)

CAMK - PHK

Bioactivity
Kinase	RBC
PHKg1	inactive (87.47%)
PHKg2	inactive (101.44%)

CAMK - PIM

Bioactivity
Kinase	RBC
PIM1	inactive (95.51%)
PIM2	inactive (89.27%)
PIM3	inactive (95.01%)

CAMK - PKD

Bioactivity
Kinase	RBC
PKD1	inactive (98.89%)
PKD3	inactive (86.66%)
PKD2	inactive (81.3%)

CAMK - TSSK

Bioactivity
Kinase	RBC
TSSK1	inactive (96.35%)
TSSK2	inactive (90.75%)

CAMK - STK33

Bioactivity
Kinase	RBC
STK33	inactive (94.27%)

STE

Test Member No. in Family
Family	no. Member on 518kinase	RBC
STE11	8	3
STE-Unique	2	2
STE20	31	23
STE7	7	3

STE - STE11

Bioactivity
Kinase	RBC
MAP3K5	inactive (110.63%)
MAP3K2	inactive (95.55%)
MAP3K3	inactive (87.56%)

STE - STE-Unique

Bioactivity
Kinase	RBC
COT	inactive (99.73%)
NIK	inactive (111.14%)

STE - STE20

Bioactivity
Kinase	RBC
GCK	inactive (88.94%)
HGK	inactive (59.41%)
KHS1	inactive (51.98%)
LOK	inactive (70.51%)
MINK	inactive (88.93%)
MST1	inactive (90.35%)
MST2	inactive (90.8%)
MST3	inactive (81.6%)
MST4	inactive (91.02%)
OSR1	inactive (109.64%)
PAK1	inactive (95.17%)
PAK2	inactive (102.9%)
PAK3	inactive (103.88%)
PAK4	inactive (104.32%)
PAK5	inactive (116.43%)
PAK6	inactive (108.69%)
SLK	inactive (99.45%)
YSK1	inactive (112.28%)
STLK3	inactive (88.5%)
TAO1	inactive (91.95%)
TAO2	inactive (97.29%)
TAO3	inactive (92.41%)
MYO3B	inactive (87.91%)

STE - STE7

Bioactivity
Kinase	RBC
MAP2K1	inactive (101.22%)
MAP2K2	inactive (89.96%)
MAP2K6	inactive (87.61%)

Other

Test Member No. in Family
Family	no. Member on 518kinase	RBC
Aur	3	3
CAMKK	2	2
Haspin	1	1
IKK	4	4
NEK	11	8
TOPK	1	1
PLK	4	3
SgK496	1	1
NAK	4	1
TTK	1	1
ULK	5	3
WEE	3	1
WNK	4	2
TLK	2	1

Other - Aur

Bioactivity
Kinase	RBC
AurA	inactive (92.26%)
AurB	inactive (96.87%)
AurC	inactive (96.01%)

Other - CAMKK

Bioactivity
Kinase	RBC
CaMKK1	inactive (101.16%)
CaMKK2	inactive (83.62%)

Other - Haspin

Bioactivity
Kinase	RBC
Haspin	inactive (87.74%)

Other - IKK

Bioactivity
Kinase	RBC
IKKa	inactive (99.49%)
IKKb	inactive (104.61%)
IKKe	inactive (100.02%)
TBK1	inactive (99.64%)

Other - NEK

Bioactivity
Kinase	RBC
NEK1	inactive (93.97%)
NEK11	inactive (101.76%)
NEK2	inactive (89.29%)
NEK4	inactive (92.81%)
NEK6	inactive (101.55%)
NEK7	inactive (97.02%)
NEK9	inactive (97.92%)
NEK3	inactive (102.24%)

Other - TOPK

Bioactivity
Kinase	RBC
PBK	inactive (87.57%)

Other - PLK

Bioactivity
Kinase	RBC
PLK1	inactive (99.94%)
PLK2	inactive (101.18%)
PLK3	inactive (98.02%)

Other - SgK496

Bioactivity
Kinase	RBC
SgK496	inactive (109.01%)

Other - NAK

Bioactivity
Kinase	RBC
MPSK1	inactive (107.68%)

Other - TTK

Bioactivity
Kinase	RBC
TTK	inactive (96.12%)

Other - ULK

Bioactivity
Kinase	RBC
ULK1	inactive (95.6%)
ULK2	inactive (110.27%)
ULK3	inactive (92.83%)

Other - WEE

Bioactivity
Kinase	RBC
Wee1	inactive (93.93%)

Other - WNK

Bioactivity
Kinase	RBC
Wnk2	inactive (109.85%)
Wnk3	inactive (103.38%)

Other - TLK

Bioactivity
Kinase	RBC
TLK2	inactive (79.03%)

CK1

Test Member No. in Family
Family	no. Member on 518kinase	RBC
CK1	7	6
VRK	3	1

CK1 - CK1

Bioactivity
Kinase	RBC
CK1d	inactive (67.67%)
CK1g1	inactive (83.27%)
CK1g2	inactive (95.74%)
CK1g3	inactive (97.85%)
CK1a	inactive (90.25%)
CK1e	inactive (80.45%)

CK1 - VRK

Bioactivity
Kinase	RBC
VRK1	inactive (82.92%)

CMGC

Test Member No. in Family
Family	no. Member on 518kinase	RBC
CK2	3	2
CLK	4	4
DYRK	10	9
MAPK	14	10
GSK	2	2
SRPK	3	3

CMGC - CK2

Bioactivity
Kinase	RBC
CK2a1	inactive (89.91%)
CK2a2	-

CMGC - CLK

Bioactivity
Kinase	RBC
CLK1	inactive (102.19%)
CLK2	inactive (92.42%)
CLK3	inactive (111.81%)
CLK4	inactive (88.72%)

CMGC - DYRK

Bioactivity
Kinase	RBC
DYRK1A	inactive (86.43%)
DYRK1B	inactive (99.24%)
DYRK2	inactive (90.55%)
DYRK3	inactive (89.02%)
DYRK4	inactive (104.15%)
HIPK1	inactive (106.41%)
HIPK2	inactive (105.91%)
HIPK3	inactive (100.5%)
HIPK4	inactive (98.55%)

CMGC - MAPK

Bioactivity
Kinase	RBC
Erk1	inactive (105.01%)
Erk2	inactive (80.83%)
JNK3	inactive (100.5%)
NLK	inactive (95.4%)
p38a	inactive (79.51%)
p38b	inactive (108.19%)
p38d	inactive (104.44%)
p38g	inactive (94.18%)
JNK1	inactive (111.23%)
JNK2	inactive (102.92%)

CMGC - GSK

Bioactivity
Kinase	RBC
GSK3A	inactive (88.65%)
GSK3B	inactive (101%)

CMGC - SRPK

Bioactivity
Kinase	RBC
MSSK1	inactive (91.46%)
SRPK1	inactive (104.43%)
SRPK2	inactive (97.1%)

Atypical

Test Member No. in Family
Family	no. Member on 518kinase	RBC
PDHK	5	1

Atypical - PDHK

Bioactivity
Kinase	RBC
PDHK1	inactive (102.4%)