Compound in Profiling

Compound Information

Test on : Millipore

Compound Name : PDK1/Akt/Flt Dual Pathway Inhibitor

Inchikey : DPANHMGWPXVBQI-UHFFFAOYSA-N

ChemSpider : 4288420

Pubchem CID : 5113385

ChEMBL : CHEMBL599894

	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	Millipore
Abl	2	2
Ack	2	1
ALK	2	1
Axl	3	3
Src	11	10
Tec	5	4
PDGFR	5	5
Csk	2	1
DDR	2	1
EGFR	4	2
Eph	14	11
FAK	2	2
Fer	2	2
FGFR	4	4
VEGFR	3	3
InsR	3	3
JakA	4	2
Met	2	2
Musk	1	1
Ret	1	1
Sev	1	1
Syk	2	2
Tie	2	1
Trk	3	2

TK - Abl

Bioactivity
Kinase	Millipore
ABL1	inactive (107%)
ABL2	inactive (110%)

TK - Ack

Bioactivity
Kinase	Millipore
ACK	inactive (109%)

TK - ALK

Bioactivity
Kinase	Millipore
ALK	inactive (96%)

TK - Axl

Bioactivity
Kinase	Millipore
AXL	inactive (81%)
MER	inactive (124%)
TYRO3	inactive (106%)

TK - Src

Bioactivity
Kinase	Millipore
BLK	inactive (79%)
BRK	inactive (107%)
SRC	inactive (85%)
FGR	inactive (104%)
FYN	inactive (94%)
HCK	inactive (89%)
LCK	inactive (134%)
LYN	inactive (84%)
FRK	inactive (95%)
YES	inactive (108%)

TK - Tec

Bioactivity
Kinase	Millipore
BMX	inactive (96%)
BTK	inactive (86%)
ITK	inactive (105%)
TXK	inactive (103%)

TK - PDGFR

Bioactivity
Kinase	Millipore
KIT	inactive (114%)
FLT3	inactive (103%)
FMS	inactive (78%)
PDGFRa	inactive (128%)
PDGFRb	inactive (120%)

TK - Csk

Bioactivity
Kinase	Millipore
CSK	inactive (123%)

TK - DDR

Bioactivity
Kinase	Millipore
DDR2	inactive (115%)

TK - EGFR

Bioactivity
Kinase	Millipore
EGFR	inactive (126%)
ErbB4	inactive (106%)

TK - Eph

Bioactivity
Kinase	Millipore
EphA1	inactive (100%)
EphA2	inactive (107%)
EphA3	inactive (113%)
EphA4	inactive (115%)
EphA5	inactive (115%)
EphA7	inactive (103%)
EphA8	inactive (108%)
EphB1	inactive (96%)
EphB2	inactive (126%)
EphB3	inactive (108%)
EphB4	inactive (118%)

TK - FAK

Bioactivity
Kinase	Millipore
FAK	inactive (87%)
PYK2	inactive (146%)

TK - Fer

Bioactivity
Kinase	Millipore
FER	inactive (112%)
FES	inactive (139%)

TK - FGFR

Bioactivity
Kinase	Millipore
FGFR1	inactive (113%)
FGFR2	inactive (118%)
FGFR3	inactive (125%)
FGFR4	inactive (118%)

TK - VEGFR

Bioactivity
Kinase	Millipore
FLT1	inactive (115%)
FLT4	inactive (98%)
KDR	inactive (109%)

TK - InsR

Bioactivity
Kinase	Millipore
IGF1R	inactive (129%)
INSR	inactive (121%)
IRR	inactive (148%)

TK - JakA

Bioactivity
Kinase	Millipore
JAK2	inactive (111%)
JAK3	inactive (103%)

TK - Met

Bioactivity
Kinase	Millipore
MET	inactive (127%)
RON	inactive (95%)

TK - Musk

Bioactivity
Kinase	Millipore
MUSK	inactive (131%)

TK - Ret

Bioactivity
Kinase	Millipore
RET	inactive (105%)

TK - Sev

Bioactivity
Kinase	Millipore
ROS	inactive (103%)

TK - Syk

Bioactivity
Kinase	Millipore
SYK	inactive (135%)
ZAP70	inactive (111%)

TK - Tie

Bioactivity
Kinase	Millipore
TIE2	inactive (75%)

TK - Trk

Bioactivity
Kinase	Millipore
TRKA	inactive (96%)
TRKB	inactive (123%)

TKL

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

TKL - STKR

Bioactivity
Kinase	Millipore
ALK4	inactive (148%)
TGFbR1	inactive (91%)

TKL - RAF

Bioactivity
Kinase	Millipore
RAF1	inactive (87%)

TKL - IRAK

Bioactivity
Kinase	Millipore
IRAK1	inactive (109%)
IRAK4	inactive (129%)

TKL - LISK

Bioactivity
Kinase	Millipore
LIMK1	inactive (113%)

TKL - MLK

Bioactivity
Kinase	Millipore
MLK1	inactive (103%)
TAK1	inactive (99%)

TKL - RIPK

Bioactivity
Kinase	Millipore
RIPK2	inactive (101%)

CAMK

Test Member No. in Family
Family	no. Member on 518kinase	Millipore
CAMKL	20	12
CAMK1	5	3
CAMK2	4	3
RAD53	1	1
DAPK	5	4
DCAMKL	3	1
MAPKAPK	5	4
MLCK	5	1
PHK	2	1
PIM	3	3
PKD	3	2
STK33	1	-
TSSK	5	2

CAMK - CAMKL

Bioactivity
Kinase	Millipore
AMPKa1	inactive (114%)
AMPKa2	inactive (122%)
NuaK1	inactive (118%)
BRSK1	inactive (81%)
BRSK2	inactive (121%)
CHK1	inactive (95%)
LKB1	inactive (108%)
MARK1	inactive (107%)
MELK	inactive (67%)
MARK2	inactive (96%)
PASK	inactive (95%)
SIK	inactive (98%)

CAMK - CAMK1

Bioactivity
Kinase	Millipore
CaMK1a	inactive (107%)
CaMK4	inactive (122%)
CaMK1d	inactive (107%)

CAMK - CAMK2

Bioactivity
Kinase	Millipore
CaMK2b	inactive (105%)
CaMK2g	inactive (120%)
CaMK2d	inactive (104%)

CAMK - RAD53

Bioactivity
Kinase	Millipore
CHK2	inactive (85%)

CAMK - DAPK

Bioactivity
Kinase	Millipore
DAPK1	inactive (95%)
DAPK2	inactive (101%)
DRAK1	inactive (108%)
DAPK3	inactive (85%)

CAMK - DCAMKL

Bioactivity
Kinase	Millipore
DCLK2	inactive (75%)

CAMK - MAPKAPK

Bioactivity
Kinase	Millipore
MAPKAPK2	inactive (117%)
MAPKAPK3	inactive (105%)
MNK2	inactive (100%)
MAPKAPK5	inactive (93%)

CAMK - MLCK

Bioactivity
Kinase	Millipore
smMLCK	inactive (79%)

CAMK - PHK

Bioactivity
Kinase	Millipore
PHKg2	inactive (103%)

CAMK - PIM

Bioactivity
Kinase	Millipore
PIM1	inactive (85%)
PIM2	inactive (104%)
PIM3	inactive (107%)

CAMK - PKD

Bioactivity
Kinase	Millipore
PKD1	inactive (104%)
PKD2	inactive (96%)

CAMK - STK33

Bioactivity
Kinase	Millipore
STK33	inactive (103%)

CAMK - TSSK

Bioactivity
Kinase	Millipore
TSSK1	inactive (107%)
TSSK2	inactive (97%)

STE

Test Member No. in Family
Family	no. Member on 518kinase	Millipore
STE11	8	1
STE20	31	14
STE7	7	3

STE - STE11

Bioactivity
Kinase	Millipore
MAP3K5	inactive (107%)

STE - STE20

Bioactivity
Kinase	Millipore
GCK	inactive (107%)
LOK	inactive (98%)
MINK	inactive (105%)
MST1	inactive (108%)
MST2	inactive (117%)
MST3	inactive (81%)
PAK2	inactive (101%)
PAK3	inactive (92%)
PAK4	inactive (92%)
PAK5	inactive (80%)
PAK6	inactive (112%)
TAO1	inactive (107%)
TAO2	inactive (111%)
TAO3	inactive (98%)

STE - STE7

Bioactivity
Kinase	Millipore
MAP2K1	inactive (99%)
MAP2K6	inactive (85%)
MAP2K7	inactive (66%)

Other

Test Member No. in Family
Family	no. Member on 518kinase	Millipore
Aur	3	3
Haspin	1	1
IKK	4	3
NEK	11	5
PLK	4	3
TLK	2	1
ULK	5	2
WNK	4	2

Other - Aur

Bioactivity
Kinase	Millipore
AurA	inactive (71%)
AurB	inactive (89%)
AurC	inactive (96%)

Other - Haspin

Bioactivity
Kinase	Millipore
Haspin	inactive (86%)

Other - IKK

Bioactivity
Kinase	Millipore
IKKa	inactive (90%)
IKKb	inactive (111%)
TBK1	inactive (97%)

Other - NEK

Bioactivity
Kinase	Millipore
NEK11	inactive (97%)
NEK2	inactive (84%)
NEK3	inactive (116%)
NEK6	inactive (100%)
NEK7	inactive (116%)

Other - PLK

Bioactivity
Kinase	Millipore
PLK1	inactive (103%)
PLK3	inactive (76%)
PLK2	inactive (73%)

Other - TLK

Bioactivity
Kinase	Millipore
TLK2	inactive (110%)

Other - ULK

Bioactivity
Kinase	Millipore
ULK2	inactive (110%)
ULK3	inactive (116%)

Other - WNK

Bioactivity
Kinase	Millipore
Wnk2	inactive (121%)
Wnk3	inactive (115%)

CK1

Test Member No. in Family
Family	no. Member on 518kinase	Millipore
CK1	7	4
VRK	3	1

CK1 - CK1

Bioactivity
Kinase	Millipore
CK1g1	inactive (91%)
CK1g2	inactive (99%)
CK1g3	inactive (113%)
CK1d	inactive (84%)

CK1 - VRK

Bioactivity
Kinase	Millipore
VRK2	inactive (116%)

CMGC

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

CMGC - CK2

Bioactivity
Kinase	Millipore
CK2a1	inactive (97%)
CK2a2	inactive (129%)

CMGC - CLK

Bioactivity
Kinase	Millipore
CLK2	inactive (115%)
CLK3	inactive (83%)

CMGC - DYRK

Bioactivity
Kinase	Millipore
DYRK2	inactive (101%)
HIPK1	inactive (96%)
HIPK2	inactive (99%)
HIPK3	inactive (96%)

CMGC - GSK

Bioactivity
Kinase	Millipore
GSK3A	inactive (101%)
GSK3B	inactive (115%)

CMGC - MAPK

Bioactivity
Kinase	Millipore
JNK1	inactive (114%)
JNK2	inactive (109%)
JNK3	inactive (112%)
Erk1	inactive (103%)
Erk2	inactive (116%)
NLK	inactive (112%)
p38a	inactive (111%)
p38b	inactive (102%)
p38g	inactive (130%)
p38d	inactive (119%)

CMGC - SRPK

Bioactivity
Kinase	Millipore
MSSK1	inactive (107%)
SRPK1	inactive (107%)
SRPK2	inactive (101%)

AGC

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

AGC - DMPK

Bioactivity
Kinase	Millipore
DMPK1	inactive (127%)
MRCKa	inactive (107%)
MRCKb	inactive (116%)
ROCK1	inactive (112%)
ROCK2	inactive (114%)

AGC - GRK

Bioactivity
Kinase	Millipore
GPRK5	inactive (107%)
GPRK6	inactive (104%)
GPRK7	inactive (103%)

AGC - RSK

Bioactivity
Kinase	Millipore
MSK1	inactive (145%)
MSK2	inactive (108%)
p70S6K	inactive (83%)
RSK3	inactive (109%)
RSK2	inactive (67%)
RSK1	inactive (120%)
RSK4	inactive (96%)

AGC - PDK1

Bioactivity
Kinase	Millipore
PDK1	inactive (121%)

AGC - PKA

Bioactivity
Kinase	Millipore
PKACa	inactive (95%)
PRKX	inactive (126%)

AGC - Akt

Bioactivity
Kinase	Millipore
AKT1	inactive (103%)
AKT2	inactive (133%)
AKT3	inactive (117%)

AGC - PKC

Bioactivity
Kinase	Millipore
PKCa	inactive (113%)
PKCg	inactive (113%)
PKCd	inactive (91%)
PKCe	inactive (88%)
PKCz	inactive (113%)
PKCh	inactive (117%)
PKCt	inactive (109%)
PKCi	inactive (99%)

AGC - PKN

Bioactivity
Kinase	Millipore
PKN2	inactive (94%)

AGC - SGK

Bioactivity
Kinase	Millipore
SGK1	inactive (146%)
SGK2	inactive (94%)
SGK3	inactive (97%)

Atypical

Test Member No. in Family
Family	no. Member on 518kinase	Millipore
Alpha	6	1
PIKK	6	1

Atypical - Alpha

Bioactivity
Kinase	Millipore
eEF2K	inactive (95%)

Atypical - PIKK

Bioactivity
Kinase	Millipore
FRAP	inactive (93%)