Compound Information
Test on : DRx
Compound Name : [4-[2-(1H-indazol-3-yl)ethenyl]phenyl]-(1-piperazinyl)methanone
Inchikey : YYLKKYCXAOBSRM-UHFFFAOYSA-N
ChemSpider : 34233115
Pubchem CID : 67089852
ChEMBL : CHEMBL3184303
|
DRx |
RBC |
Metz |
Millipore |
GPCR |
bioactivity |
Kd (nM) |
Remain Activity (%) |
Ki (nM) |
Remain Activity (%) |
Inhibition (%) |
active criteria |
<3000nM |
<50% |
<1000nM |
<50% |
>50% |
Other
Other - NAK
Bioactivity |
---|
Kinase | DRx |
---|
AAK1 | active (48nM) |
BIKE | active (9.6nM) |
GAK | active (260nM) |
MPSK1 | active (29nM) |
Other - Aur
Bioactivity |
---|
Kinase | DRx |
---|
AurA | active (650nM) |
AurB | active (88nM) |
AurC | active (59nM) |
Other - CAMKK
Bioactivity |
---|
Kinase | DRx |
---|
CaMKK1 | active (210nM) |
CaMKK2 | active (470nM) |
Other - PEK
Bioactivity |
---|
Kinase | DRx |
---|
HRI | inactive (10001nM) |
PKR | inactive (3600nM) |
Other - IRE
Bioactivity |
---|
Kinase | DRx |
---|
IRE1 | inactive (3500nM) |
Other - IKK
Bioactivity |
---|
Kinase | DRx |
---|
IKKa | active (180nM) |
IKKb | active (430nM) |
IKKe | active (340nM) |
TBK1 | active (130nM) |
Other - NEK
Bioactivity |
---|
Kinase | DRx |
---|
NEK1 | inactive (3100nM) |
NEK11 | inactive (10001nM) |
NEK2 | inactive (5300nM) |
NEK3 | active (1000nM) |
NEK4 | active (1100nM) |
NEK5 | active (2300nM) |
NEK6 | active (120nM) |
NEK7 | active (210nM) |
NEK9 | active (520nM) |
Other - WEE
Bioactivity |
---|
Kinase | DRx |
---|
MYT1 | inactive (10001nM) |
Wee1 | active (2800nM) |
Wee1B | inactive (4700nM) |
Other - PLK
Bioactivity |
---|
Kinase | DRx |
---|
PLK1 | inactive (10001nM) |
PLK2 | inactive (10001nM) |
PLK3 | inactive (10001nM) |
PLK4 | active (21nM) |
Other - SgK496
Bioactivity |
---|
Kinase | DRx |
---|
SgK496 | active (660nM) |
Other - NKF1
Bioactivity |
---|
Kinase | DRx |
---|
SBK | active (580nM) |
SgK110 | active (230nM) |
Other - NKF4
Bioactivity |
---|
Kinase | DRx |
---|
CLIK1 | active (630nM) |
Other - ULK
Bioactivity |
---|
Kinase | DRx |
---|
Fused | inactive (10001nM) |
ULK1 | active (53nM) |
ULK2 | active (130nM) |
ULK3 | active (120nM) |
Other - TLK
Bioactivity |
---|
Kinase | DRx |
---|
TLK1 | active (2700nM) |
TLK2 | active (1800nM) |
Other - TTK
Bioactivity |
---|
Kinase | DRx |
---|
TTK | active (110nM) |
TK
TK - Abl
Bioactivity |
---|
Kinase | DRx |
---|
ABL1 | active (63nM) |
ABL2 | active (250nM) |
TK - ALK
Bioactivity |
---|
Kinase | DRx |
---|
ALK | active (660nM) |
LTK | active (920nM) |
TK - Axl
Bioactivity |
---|
Kinase | DRx |
---|
AXL | active (180nM) |
MER | active (750nM) |
TYRO3 | inactive (10001nM) |
TK - Src
Bioactivity |
---|
Kinase | DRx |
---|
BLK | inactive (3500nM) |
BRK | inactive (10001nM) |
FGR | active (440nM) |
FRK | active (2100nM) |
FYN | active (660nM) |
HCK | inactive (4300nM) |
LCK | active (1200nM) |
LYN | inactive (3100nM) |
SRC | active (2800nM) |
SRM | active (2700nM) |
YES | active (18nM) |
TK - Tec
Bioactivity |
---|
Kinase | DRx |
---|
BMX | active (1900nM) |
BTK | active (1000nM) |
ITK | active (240nM) |
TEC | inactive (10001nM) |
TXK | active (580nM) |
TK - PDGFR
Bioactivity |
---|
Kinase | DRx |
---|
FMS | active (120nM) |
FLT3 | active (15nM) |
KIT | active (53nM) |
PDGFRa | active (130nM) |
PDGFRb | active (30nM) |
TK - Csk
Bioactivity |
---|
Kinase | DRx |
---|
CSK | inactive (4400nM) |
CTK | active (3000nM) |
TK - DDR
Bioactivity |
---|
Kinase | DRx |
---|
DDR1 | inactive (3200nM) |
DDR2 | active (2100nM) |
TK - EGFR
Bioactivity |
---|
Kinase | DRx |
---|
EGFR | inactive (10001nM) |
ErbB2 | inactive (10001nM) |
ErbB3 | inactive (10001nM) |
ErbB4 | inactive (10001nM) |
TK - Eph
Bioactivity |
---|
Kinase | DRx |
---|
EphA1 | active (150nM) |
EphA2 | active (1500nM) |
EphA3 | active (810nM) |
EphA4 | inactive (10001nM) |
EphA5 | inactive (10001nM) |
EphA6 | active (1500nM) |
EphA7 | active (390nM) |
EphA8 | inactive (10001nM) |
EphB1 | active (2500nM) |
EphB2 | inactive (10001nM) |
EphB3 | inactive (10001nM) |
EphB4 | active (2900nM) |
EphB6 | active (130nM) |
TK - FAK
Bioactivity |
---|
Kinase | DRx |
---|
FAK | active (2100nM) |
PYK2 | active (760nM) |
TK - Fer
Bioactivity |
---|
Kinase | DRx |
---|
FER | active (1100nM) |
FES | active (750nM) |
TK - FGFR
Bioactivity |
---|
Kinase | DRx |
---|
FGFR1 | active (370nM) |
FGFR2 | active (850nM) |
FGFR3 | active (1200nM) |
FGFR4 | active (2300nM) |
TK - VEGFR
Bioactivity |
---|
Kinase | DRx |
---|
FLT1 | active (73nM) |
FLT4 | active (1300nM) |
KDR | active (120nM) |
TK - InsR
Bioactivity |
---|
Kinase | DRx |
---|
IGF1R | active (920nM) |
INSR | active (400nM) |
IRR | active (420nM) |
TK - JakA
Bioactivity |
---|
Kinase | DRx |
---|
JAK1 | active (1200nM) |
JAK2 | active (76nM) |
JAK3 | active (39nM) |
TYK2 | active (160nM) |
TK - Met
Bioactivity |
---|
Kinase | DRx |
---|
MET | active (170nM) |
RON | active (810nM) |
TK - Musk
Bioactivity |
---|
Kinase | DRx |
---|
MUSK | active (200nM) |
TK - Ret
Bioactivity |
---|
Kinase | DRx |
---|
RET | active (150nM) |
TK - Sev
Bioactivity |
---|
Kinase | DRx |
---|
ROS | inactive (10001nM) |
TK - Syk
Bioactivity |
---|
Kinase | DRx |
---|
SYK | active (670nM) |
ZAP70 | active (940nM) |
TK - Tie
Bioactivity |
---|
Kinase | DRx |
---|
TIE1 | active (300nM) |
TIE2 | active (1100nM) |
TK - Ack
Bioactivity |
---|
Kinase | DRx |
---|
TNK1 | active (580nM) |
ACK | active (1600nM) |
TK - Trk
Bioactivity |
---|
Kinase | DRx |
---|
TRKA | active (270nM) |
TRKB | active (140nM) |
TRKC | active (250nM) |
TKL
TKL - STKR
Bioactivity |
---|
Kinase | DRx |
---|
ALK2 | active (140nM) |
ALK4 | inactive (10001nM) |
ACTR2 | active (320nM) |
ACTR2B | active (370nM) |
ALK1 | inactive (10001nM) |
BMPR1A | active (1900nM) |
BMPR1B | active (120nM) |
BMPR2 | active (370nM) |
TGFbR1 | inactive (10001nM) |
TGFbR2 | inactive (10001nM) |
TKL - RIPK
Bioactivity |
---|
Kinase | DRx |
---|
SgK288 | active (82nM) |
RIPK1 | active (64nM) |
RIPK2 | inactive (3700nM) |
ANKRD3 | active (130nM) |
TKL - RAF
Bioactivity |
---|
Kinase | DRx |
---|
BRAF | inactive (10001nM) |
RAF1 | inactive (10001nM) |
TKL - MLK
Bioactivity |
---|
Kinase | DRx |
---|
DLK | active (67nM) |
LZK | active (500nM) |
MLK1 | active (650nM) |
MLK2 | active (1500nM) |
MLK3 | active (230nM) |
TAK1 | active (36nM) |
HH498 | inactive (10001nM) |
ZAK | active (580nM) |
TKL - IRAK
Bioactivity |
---|
Kinase | DRx |
---|
IRAK1 | active (48nM) |
IRAK3 | active (240nM) |
IRAK4 | active (680nM) |
TKL - LISK
Bioactivity |
---|
Kinase | DRx |
---|
LIMK1 | inactive (10001nM) |
LIMK2 | inactive (10001nM) |
TESK1 | inactive (10001nM) |
TKL - LRRK
Bioactivity |
---|
Kinase | DRx |
---|
LRRK2 | active (350nM) |
Atypical
Atypical
Test Member No. in Family |
---|
Family | no. Member on 518kinase | DRx |
---|
ABC1 | 5 | 2 |
PIKK | 6 | 1 |
RIO | 3 | 3 |
Alpha | 6 | 1 |
Atypical - ABC1
Bioactivity |
---|
Kinase | DRx |
---|
ADCK3 | inactive (10001nM) |
ADCK4 | inactive (10001nM) |
Atypical - PIKK
Bioactivity |
---|
Kinase | DRx |
---|
FRAP | inactive (10001nM) |
Atypical - RIO
Bioactivity |
---|
Kinase | DRx |
---|
RIOK1 | active (47nM) |
RIOK2 | inactive (5000nM) |
RIOK3 | active (61nM) |
Atypical - Alpha
Bioactivity |
---|
Kinase | DRx |
---|
ChaK2 | inactive (10001nM) |
AGC
AGC - Akt
Bioactivity |
---|
Kinase | DRx |
---|
AKT1 | inactive (10001nM) |
AKT2 | inactive (10001nM) |
AKT3 | inactive (10001nM) |
AGC - DMPK
Bioactivity |
---|
Kinase | DRx |
---|
CRIK | active (650nM) |
DMPK1 | inactive (3800nM) |
DMPK2 | active (2100nM) |
MRCKa | inactive (10001nM) |
MRCKb | inactive (10001nM) |
ROCK1 | active (300nM) |
ROCK2 | active (250nM) |
AGC - GRK
Bioactivity |
---|
Kinase | DRx |
---|
RHOK | inactive (10001nM) |
GPRK4 | active (71nM) |
GPRK7 | inactive (5000nM) |
AGC - NDR
Bioactivity |
---|
Kinase | DRx |
---|
LATS1 | inactive (5000nM) |
LATS2 | active (1500nM) |
NDR1 | active (390nM) |
NDR2 | active (1100nM) |
AGC - MAST
Bioactivity |
---|
Kinase | DRx |
---|
MAST1 | inactive (10001nM) |
AGC - PDK1
Bioactivity |
---|
Kinase | DRx |
---|
PDK1 | active (650nM) |
AGC - PKA
Bioactivity |
---|
Kinase | DRx |
---|
PKACa | inactive (10001nM) |
PKACb | inactive (10001nM) |
PRKX | active (1200nM) |
AGC - PKN
Bioactivity |
---|
Kinase | DRx |
---|
PKN1 | active (580nM) |
PKN2 | active (880nM) |
AGC - PKC
Bioactivity |
---|
Kinase | DRx |
---|
PKCd | inactive (10001nM) |
PKCe | inactive (10001nM) |
PKCh | inactive (10001nM) |
PKCi | inactive (10001nM) |
PKCt | inactive (10001nM) |
AGC - PKG
Bioactivity |
---|
Kinase | DRx |
---|
PKG1 | active (2500nM) |
PKG2 | active (800nM) |
AGC - RSK
Bioactivity |
---|
Kinase | DRx |
---|
p70S6K | active (310nM) |
AGC - SGK
Bioactivity |
---|
Kinase | DRx |
---|
SGK3 | active (96nM) |
AGC - YANK
Bioactivity |
---|
Kinase | DRx |
---|
YANK1 | inactive (4400nM) |
YANK2 | inactive (10001nM) |
YANK3 | inactive (10001nM) |
CAMK
CAMK - CAMKL
Bioactivity |
---|
Kinase | DRx |
---|
AMPKa1 | active (430nM) |
AMPKa2 | active (440nM) |
NuaK1 | inactive (10001nM) |
BRSK1 | active (1900nM) |
BRSK2 | active (1200nM) |
CHK1 | active (710nM) |
HUNK | active (460nM) |
LKB1 | active (240nM) |
MARK1 | active (310nM) |
MARK2 | active (440nM) |
MARK3 | active (1300nM) |
MARK4 | active (210nM) |
MELK | active (210nM) |
NIM1 | active (1100nM) |
QSK | active (2300nM) |
SIK | active (670nM) |
QIK | active (560nM) |
NuaK2 | active (54nM) |
SNRK | inactive (10001nM) |
CAMK - CAMK1
Bioactivity |
---|
Kinase | DRx |
---|
CaMK1a | active (1400nM) |
CaMK1d | active (530nM) |
CaMK1g | active (2100nM) |
CaMK4 | inactive (10001nM) |
CAMK - CAMK2
Bioactivity |
---|
Kinase | DRx |
---|
CaMK2a | inactive (4000nM) |
CaMK2b | inactive (10001nM) |
CaMK2d | inactive (10001nM) |
CaMK2g | inactive (10001nM) |
CAMK - CASK
Bioactivity |
---|
Kinase | DRx |
---|
CASK | inactive (10001nM) |
CAMK - RAD53
Bioactivity |
---|
Kinase | DRx |
---|
CHK2 | active (95nM) |
CAMK - DAPK
Bioactivity |
---|
Kinase | DRx |
---|
DAPK1 | active (360nM) |
DAPK2 | active (1800nM) |
DAPK3 | active (310nM) |
DRAK1 | active (2.9nM) |
DRAK2 | active (4.8nM) |
CAMK - DCAMKL
Bioactivity |
---|
Kinase | DRx |
---|
DCLK1 | active (2000nM) |
DCLK2 | inactive (10001nM) |
DCLK3 | active (86nM) |
CAMK - MAPKAPK
Bioactivity |
---|
Kinase | DRx |
---|
MAPKAPK2 | inactive (10001nM) |
MAPKAPK5 | active (1200nM) |
MNK1 | inactive (10001nM) |
MNK2 | active (1200nM) |
CAMK - MLCK
Bioactivity |
---|
Kinase | DRx |
---|
caMLCK | active (4.3nM) |
smMLCK | active (740nM) |
skMLCK | active (52nM) |
SgK085 | active (170nM) |
CAMK - PHK
Bioactivity |
---|
Kinase | DRx |
---|
PHKg1 | active (210nM) |
PHKg2 | active (140nM) |
CAMK - PIM
Bioactivity |
---|
Kinase | DRx |
---|
PIM1 | inactive (10001nM) |
PIM2 | inactive (10001nM) |
PIM3 | inactive (10001nM) |
CAMK - PKD
Bioactivity |
---|
Kinase | DRx |
---|
PKD1 | active (1200nM) |
PKD2 | active (1500nM) |
PKD3 | active (780nM) |
CAMK - STK33
Bioactivity |
---|
Kinase | DRx |
---|
STK33 | active (140nM) |
CAMK - TSSK
Bioactivity |
---|
Kinase | DRx |
---|
TSSK1 | active (2300nM) |
STE
STE
Test Member No. in Family |
---|
Family | no. Member on 518kinase | DRx |
---|
STE11 | 8 | 8 |
STE20 | 31 | 27 |
STE7 | 7 | 7 |
STE - STE11
Bioactivity |
---|
Kinase | DRx |
---|
MAP3K5 | inactive (10001nM) |
MAP3K6 | inactive (10001nM) |
MAP3K1 | inactive (10001nM) |
MAP3K7 | inactive (10001nM) |
MAP3K2 | active (72nM) |
MAP3K3 | active (120nM) |
MAP3K4 | active (1600nM) |
MAP3K8 | active (5.2nM) |
STE - STE20
Bioactivity |
---|
Kinase | DRx |
---|
HPK1 | active (63nM) |
LOK | active (13nM) |
GCK | active (11nM) |
KHS2 | active (150nM) |
HGK | active (33nM) |
KHS1 | active (260nM) |
MINK | active (25nM) |
MST1 | active (560nM) |
MST2 | inactive (10001nM) |
MST3 | active (1100nM) |
MST4 | active (1100nM) |
MYO3A | active (740nM) |
MYO3B | inactive (6000nM) |
OSR1 | active (1700nM) |
PAK1 | active (2100nM) |
PAK2 | active (2700nM) |
PAK3 | active (460nM) |
PAK4 | active (1500nM) |
PAK6 | active (1300nM) |
PAK5 | active (390nM) |
SLK | active (13nM) |
STLK3 | active (890nM) |
TAO1 | active (1800nM) |
TAO2 | inactive (10001nM) |
TAO3 | active (1000nM) |
TNIK | active (28nM) |
YSK1 | inactive (4300nM) |
STE - STE7
Bioactivity |
---|
Kinase | DRx |
---|
MAP2K1 | active (530nM) |
MAP2K2 | active (850nM) |
MAP2K3 | active (150nM) |
MAP2K4 | active (250nM) |
MAP2K5 | active (120nM) |
MAP2K6 | active (820nM) |
MAP2K7 | inactive (10001nM) |
CMGC
CMGC - CDK
Bioactivity |
---|
Kinase | DRx |
---|
PITSLRE | inactive (10001nM) |
CHED | inactive (10001nM) |
CDK11 | inactive (10001nM) |
PCTAIRE1 | active (830nM) |
PCTAIRE2 | active (1900nM) |
PCTAIRE3 | inactive (10001nM) |
PFTAIRE2 | active (2600nM) |
PFTAIRE1 | active (870nM) |
CMGC - CDKL
Bioactivity |
---|
Kinase | DRx |
---|
CDKL1 | inactive (10001nM) |
CDKL2 | active (1400nM) |
CDKL3 | inactive (10001nM) |
CDKL5 | inactive (10001nM) |
CMGC - CLK
Bioactivity |
---|
Kinase | DRx |
---|
CLK1 | active (64nM) |
CLK2 | active (93nM) |
CLK3 | inactive (6200nM) |
CLK4 | active (49nM) |
CMGC - CK2
Bioactivity |
---|
Kinase | DRx |
---|
CK2a1 | active (1200nM) |
CK2a2 | active (230nM) |
CMGC - DYRK
Bioactivity |
---|
Kinase | DRx |
---|
DYRK1A | active (180nM) |
DYRK1B | active (940nM) |
DYRK2 | active (390nM) |
HIPK1 | active (430nM) |
HIPK2 | active (300nM) |
HIPK3 | active (580nM) |
HIPK4 | active (1000nM) |
PRP4 | active (270nM) |
CMGC - MAPK
Bioactivity |
---|
Kinase | DRx |
---|
Erk1 | inactive (10001nM) |
Erk2 | inactive (10001nM) |
Erk3 | inactive (5500nM) |
Erk4 | inactive (10001nM) |
Erk5 | active (2700nM) |
Erk7 | active (1100nM) |
JNK1 | active (580nM) |
JNK2 | active (230nM) |
JNK3 | active (51nM) |
NLK | inactive (10001nM) |
p38a | inactive (10001nM) |
p38b | active (1400nM) |
p38d | inactive (10001nM) |
p38g | inactive (10001nM) |
CMGC - GSK
Bioactivity |
---|
Kinase | DRx |
---|
GSK3A | inactive (10001nM) |
GSK3B | inactive (10001nM) |
CMGC - RCK
Bioactivity |
---|
Kinase | DRx |
---|
ICK | active (2200nM) |
MAK | inactive (10001nM) |
CMGC - SRPK
Bioactivity |
---|
Kinase | DRx |
---|
SRPK1 | active (55nM) |
SRPK2 | active (15nM) |
MSSK1 | active (200nM) |
CK1
CK1
Test Member No. in Family |
---|
Family | no. Member on 518kinase | DRx |
---|
CK1 | 7 | 7 |
VRK | 3 | 1 |
CK1 - CK1
Bioactivity |
---|
Kinase | DRx |
---|
CK1a | active (1200nM) |
CK1a2 | inactive (10001nM) |
CK1d | active (2300nM) |
CK1e | active (630nM) |
CK1g1 | active (1200nM) |
CK1g2 | active (580nM) |
CK1g3 | active (1200nM) |
CK1 - VRK
Bioactivity |
---|
Kinase | DRx |
---|
VRK2 | inactive (10001nM) |