Compound Information



Test on : DRx, Metz

Compound Name
DRx : 5-indazolyl pyridine 24
Metz : Kinome_836

Inchikey
Same : BPNUQXPIQBZCMR-N
DRx : BPNUQXPIQBZCMR-LJQANCHMSA-N
Metz : BPNUQXPIQBZCMR-UHFFFAOYSA-N

ChemSpider
DRx : 23271831
Metz : 19576321

Pubchem CID
DRx : 23647015
Metz : 20744853

ChEMBL
DRx : CHEMBL212157
Metz : CHEMBL2002726




DRxMetz

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

Other


Test Member No. in Family
Familyno. Member on 518kinaseDRxMetz
44-
332
221
42-
21-
444
1192
331
443
11-
32-
21-
54-
22-
11-
1-1
1-1
Other - NAK

Bioactivity
KinaseDRxMetz
AAK1active (43nM)-
BIKEactive (120nM)-
GAKactive (180nM)-
MPSK1inactive (10001nM)-
Other - Aur

Bioactivity
KinaseDRxMetz
AurAinactive (10001nM)inactive (5011.87nM)
AurBinactive (10001nM)active (501.19nM)
AurCinactive (8400nM)-
Other - CAMKK

Bioactivity
KinaseDRxMetz
CaMKK1active (810nM)-
CaMKK2active (740nM)-
Other - PEK

Bioactivity
KinaseDRxMetz
HRIinactive (10001nM)-
PKRactive (2800nM)-
Other - IRE

Bioactivity
KinaseDRxMetz
IRE1inactive (10001nM)-
Other - IKK

Bioactivity
KinaseDRxMetz
IKKainactive (10001nM)inactive (2511.89nM)
IKKbinactive (10001nM)inactive (>3162.28nM)
IKKeinactive (10001nM)-
TBK1inactive (10001nM)-
Other - NEK

Bioactivity
KinaseDRxMetz
NEK1inactive (10001nM)-
NEK11inactive (10001nM)-
NEK2inactive (10001nM)inactive (>10000nM)
NEK3inactive (10001nM)-
NEK4inactive (10001nM)inactive (1584.89nM)
NEK5inactive (10001nM)-
NEK6inactive (10001nM)-
NEK7inactive (10001nM)-
NEK9inactive (10001nM)-
Other - WEE

Bioactivity
KinaseDRxMetz
MYT1inactive (10001nM)-
Wee1inactive (10001nM)-
Wee1Binactive (10001nM)-
Other - PLK

Bioactivity
KinaseDRxMetz
PLK1inactive (10001nM)inactive (>7943.28nM)
PLK2inactive (10001nM)-
PLK3inactive (10001nM)inactive (>7943.28nM)
PLK4inactive (10001nM)inactive (>3981.07nM)
Other - SgK496

Bioactivity
KinaseDRxMetz
SgK496inactive (10001nM)-
Other - NKF1

Bioactivity
KinaseDRxMetz
SBKinactive (10001nM)-
SgK110inactive (10001nM)-
Other - NKF4

Bioactivity
KinaseDRxMetz
CLIK1inactive (10001nM)-
Other - ULK

Bioactivity
KinaseDRxMetz
Fusedinactive (10001nM)-
ULK1inactive (8000nM)-
ULK2inactive (6000nM)-
ULK3inactive (10001nM)-
Other - TLK

Bioactivity
KinaseDRxMetz
TLK1inactive (10001nM)-
TLK2inactive (10001nM)-
Other - TTK

Bioactivity
KinaseDRxMetz
TTKinactive (10001nM)-
Other - CDC7

Bioactivity
KinaseDRxMetz
CDC7-active (12.59nM)
Other - TOPK

Bioactivity
KinaseDRxMetz
PBK-inactive (1258.93nM)

TK


Test Member No. in Family
Familyno. Member on 518kinaseDRxMetz
221
222
332
11119
553
555
221
22-
443
14131
222
222
442
333
332
443
222
11-
111
111
221
22-
221
333
TK - Abl

Bioactivity
KinaseDRxMetz
ABL1inactive (10001nM)inactive (>630.96nM)
ABL2inactive (10001nM)-
TK - ALK

Bioactivity
KinaseDRxMetz
ALKinactive (10001nM)inactive (>1258.93nM)
LTKinactive (10001nM)-
TK - Axl

Bioactivity
KinaseDRxMetz
AXLinactive (10001nM)inactive (>1995.26nM)
MERinactive (10001nM)-
TYRO3inactive (10001nM)inactive (>1995.26nM)
TK - Src

Bioactivity
KinaseDRxMetz
BLKinactive (10001nM)inactive (>1584.89nM)
BRKinactive (10001nM)inactive (>2511.89nM)
FGRinactive (10001nM)-
FRKinactive (10001nM)inactive (>2511.89nM)
FYNinactive (10001nM)inactive (>794.33nM)
HCKinactive (10001nM)-
LCKinactive (10001nM)inactive (>2511.89nM)
LYNinactive (10001nM)inactive (>1584.89nM)
SRCinactive (10001nM)inactive (>1995.26nM)
SRMinactive (10001nM)inactive (>1584.89nM)
YESinactive (10001nM)-
TK - Tec

Bioactivity
KinaseDRxMetz
BMXinactive (10001nM)-
BTKinactive (10001nM)inactive (>1258.93nM)
ITKinactive (10001nM)inactive (>1584.89nM)
TECinactive (10001nM)-
TXKinactive (10001nM)-
TK - PDGFR

Bioactivity
KinaseDRxMetz
FMSinactive (10001nM)inactive (>2511.89nM)
FLT3active (540nM)active (630.96nM)
KITinactive (10001nM)inactive (>1258.93nM)
PDGFRainactive (10001nM)-
PDGFRbinactive (10001nM)-
TK - Csk

Bioactivity
KinaseDRxMetz
CSKinactive (10001nM)-
CTKinactive (10001nM)inactive (>1995.26nM)
TK - DDR

Bioactivity
KinaseDRxMetz
DDR1inactive (10001nM)-
DDR2inactive (10001nM)-
TK - EGFR

Bioactivity
KinaseDRxMetz
EGFRinactive (10001nM)inactive (>1995.26nM)
ErbB2inactive (10001nM)inactive (>1584.89nM)
ErbB3inactive (10001nM)-
ErbB4inactive (10001nM)inactive (>3981.07nM)
TK - Eph

Bioactivity
KinaseDRxMetz
EphA1inactive (10001nM)-
EphA2inactive (10001nM)inactive (>3162.28nM)
EphA3inactive (10001nM)-
EphA4inactive (10001nM)-
EphA5inactive (10001nM)-
EphA6inactive (10001nM)-
EphA7inactive (10001nM)-
EphA8inactive (10001nM)-
EphB1inactive (10001nM)-
EphB2inactive (10001nM)-
EphB3inactive (10001nM)-
EphB4inactive (10001nM)-
EphB6inactive (10001nM)-
TK - FAK

Bioactivity
KinaseDRxMetz
FAKinactive (10001nM)inactive (>1584.89nM)
PYK2inactive (10001nM)active (1000nM)
TK - Fer

Bioactivity
KinaseDRxMetz
FERinactive (10001nM)active (1000nM)
FESinactive (10001nM)inactive (>1995.26nM)
TK - FGFR

Bioactivity
KinaseDRxMetz
FGFR1inactive (10001nM)inactive (>5011.87nM)
FGFR2inactive (10001nM)-
FGFR3inactive (10001nM)inactive (>1995.26nM)
FGFR4inactive (10001nM)-
TK - VEGFR

Bioactivity
KinaseDRxMetz
FLT1inactive (10001nM)inactive (>398.11nM)
FLT4inactive (10001nM)inactive (3981.07nM)
KDRinactive (10001nM)inactive (>7943.28nM)
TK - InsR

Bioactivity
KinaseDRxMetz
IGF1Rinactive (10001nM)inactive (>1995.26nM)
INSRinactive (10001nM)inactive (>5011.87nM)
IRRinactive (10001nM)-
TK - JakA

Bioactivity
KinaseDRxMetz
JAK1inactive (10001nM)-
JAK2inactive (10001nM)inactive (1258.93nM)
JAK3active (1500nM)inactive (>1584.89nM)
TYK2inactive (10001nM)inactive (>1995.26nM)
TK - Met

Bioactivity
KinaseDRxMetz
METinactive (10001nM)inactive (>3162.28nM)
RONinactive (10001nM)-
TK - Musk

Bioactivity
KinaseDRxMetz
MUSKinactive (10001nM)-
TK - Ret

Bioactivity
KinaseDRxMetz
RETinactive (10001nM)inactive (>1258.93nM)
TK - Sev

Bioactivity
KinaseDRxMetz
ROSinactive (10001nM)inactive (>1995.26nM)
TK - Syk

Bioactivity
KinaseDRxMetz
SYKinactive (10001nM)inactive (>1584.89nM)
ZAP70inactive (10001nM)-
TK - Tie

Bioactivity
KinaseDRxMetz
TIE1inactive (10001nM)-
TIE2inactive (10001nM)-
TK - Ack

Bioactivity
KinaseDRxMetz
TNK1inactive (10001nM)-
ACKinactive (10001nM)-
TK - Trk

Bioactivity
KinaseDRxMetz
TRKAinactive (10001nM)inactive (>2511.89nM)
TRKBinactive (10001nM)inactive (>5011.87nM)
TRKCinactive (10001nM)inactive (>1258.93nM)

TKL


Test Member No. in Family
Familyno. Member on 518kinaseDRxMetz
12101
54-
521
1082
432
431
211
TKL - STKR

Bioactivity
KinaseDRxMetz
ALK2inactive (10001nM)-
ALK4inactive (10001nM)-
ACTR2inactive (10001nM)-
ACTR2Binactive (10001nM)-
ALK1inactive (10001nM)-
BMPR1Ainactive (10001nM)-
BMPR1Binactive (10001nM)-
BMPR2inactive (10001nM)-
TGFbR1inactive (10001nM)-
TGFbR2inactive (10001nM)-
TKL - RIPK

Bioactivity
KinaseDRxMetz
SgK288inactive (10001nM)-
RIPK1inactive (10001nM)-
RIPK2inactive (10001nM)-
ANKRD3inactive (10001nM)-
TKL - RAF

Bioactivity
KinaseDRxMetz
BRAFinactive (10001nM)-
RAF1inactive (10001nM)-
TKL - MLK

Bioactivity
KinaseDRxMetz
DLKinactive (10001nM)-
LZKinactive (10001nM)-
MLK1inactive (10001nM)-
MLK2inactive (10001nM)-
MLK3inactive (10001nM)-
TAK1active (640nM)-
HH498inactive (10001nM)-
ZAKinactive (10001nM)inactive (>7943.28nM)
TKL - IRAK

Bioactivity
KinaseDRxMetz
IRAK1inactive (3100nM)active (1000nM)
IRAK3inactive (10001nM)-
IRAK4active (2500nM)active (1000nM)
TKL - LISK

Bioactivity
KinaseDRxMetz
LIMK1inactive (10001nM)active (1000nM)
LIMK2inactive (10001nM)-
TESK1inactive (10001nM)-
TKL - LRRK

Bioactivity
KinaseDRxMetz
LRRK2active (1900nM)-

Atypical


Test Member No. in Family
Familyno. Member on 518kinaseDRxMetz
52-
61-
33-
611
Atypical - ABC1

Bioactivity
KinaseDRxMetz
ADCK3inactive (10001nM)-
ADCK4inactive (10001nM)-
Atypical - PIKK

Bioactivity
KinaseDRxMetz
FRAPinactive (10001nM)-
Atypical - RIO

Bioactivity
KinaseDRxMetz
RIOK1active (620nM)-
RIOK2inactive (5300nM)-
RIOK3active (690nM)-
Atypical - Alpha

Bioactivity
KinaseDRxMetz
ChaK2inactive (10001nM)-
eEF2K-inactive (>3981.07nM)

AGC


Test Member No. in Family
Familyno. Member on 518kinaseDRxMetz
333
773
731
44-
51-
111
532
321
955
222
814
311
33-
AGC - Akt

Bioactivity
KinaseDRxMetz
AKT1active (76nM)active (39.81nM)
AKT2active (2900nM)active (501.19nM)
AKT3active (180nM)active (79.43nM)
AGC - DMPK

Bioactivity
KinaseDRxMetz
CRIKactive (13nM)-
DMPK1active (92nM)-
DMPK2active (460nM)-
MRCKaactive (380nM)active (79.43nM)
MRCKbactive (95nM)-
ROCK1active (37nM)active (19.95nM)
ROCK2inactive (10001nM)active (31.62nM)
AGC - GRK

Bioactivity
KinaseDRxMetz
RHOKinactive (10001nM)-
GPRK4active (1400nM)-
GPRK7active (1900nM)-
GPRK5--
AGC - NDR

Bioactivity
KinaseDRxMetz
LATS1active (1100nM)-
LATS2active (620nM)-
NDR1inactive (10001nM)-
NDR2inactive (10001nM)-
AGC - MAST

Bioactivity
KinaseDRxMetz
MAST1inactive (10001nM)-
AGC - PDK1

Bioactivity
KinaseDRxMetz
PDK1inactive (10001nM)inactive (>3981.07nM)
AGC - PKA

Bioactivity
KinaseDRxMetz
PKACaactive (56nM)active (19.95nM)
PKACbactive (90nM)-
PRKXactive (97nM)active (19.95nM)
AGC - PKN

Bioactivity
KinaseDRxMetz
PKN1active (210nM)-
PKN2active (590nM)active (100nM)
AGC - PKC

Bioactivity
KinaseDRxMetz
PKCdactive (27nM)active (7.94nM)
PKCeactive (11nM)-
PKChactive (9.5nM)-
PKCiinactive (10001nM)inactive (3981.07nM)
PKCtactive (12nM)-
PKCg-active (251.19nM)
PKCz-inactive (3162.28nM)
AGC - PKG

Bioactivity
KinaseDRxMetz
PKG1active (270nM)active (158.49nM)
PKG2active (19nM)active (398.11nM)
AGC - RSK

Bioactivity
KinaseDRxMetz
p70S6Kinactive (3600nM)active (63.1nM)
RSK2-active (1000nM)
MSK1-active (100nM)
MSK2-active (39.81nM)
AGC - SGK

Bioactivity
KinaseDRxMetz
SGK3inactive (5100nM)-
SGK1-active (794.33nM)
AGC - YANK

Bioactivity
KinaseDRxMetz
YANK1inactive (10001nM)-
YANK2inactive (10001nM)-
YANK3inactive (10001nM)-

CAMK


Test Member No. in Family
Familyno. Member on 518kinaseDRxMetz
20199
542
444
11-
111
552
331
544
54-
221
333
332
111
512
CAMK - CAMKL

Bioactivity
KinaseDRxMetz
AMPKa1inactive (10001nM)active (199.53nM)
AMPKa2inactive (10001nM)-
NuaK1inactive (10001nM)-
BRSK1inactive (10001nM)inactive (1258.93nM)
BRSK2inactive (10001nM)-
CHK1inactive (10001nM)inactive (>7943.28nM)
HUNKinactive (10001nM)-
LKB1inactive (10001nM)-
MARK1inactive (10001nM)-
MARK2inactive (10001nM)inactive (1995.26nM)
MARK3inactive (10001nM)inactive (1995.26nM)
MARK4inactive (10001nM)-
MELKactive (590nM)active (630.96nM)
NIM1inactive (10001nM)-
QSKinactive (10001nM)-
SIKinactive (10001nM)-
QIKinactive (10001nM)-
NuaK2inactive (4200nM)-
SNRKinactive (10001nM)-
PASK--
CAMK - CAMK1

Bioactivity
KinaseDRxMetz
CaMK1ainactive (10001nM)active (125.89nM)
CaMK1dactive (2400nM)-
CaMK1ginactive (10001nM)-
CaMK4active (710nM)-
CAMK - CAMK2

Bioactivity
KinaseDRxMetz
CaMK2aactive (320nM)-
CaMK2bactive (970nM)active (316.23nM)
CaMK2dactive (270nM)active (10nM)
CaMK2gactive (890nM)active (25.12nM)
CAMK - CASK

Bioactivity
KinaseDRxMetz
CASKinactive (10001nM)-
CAMK - RAD53

Bioactivity
KinaseDRxMetz
CHK2inactive (9800nM)inactive (1258.93nM)
CAMK - DAPK

Bioactivity
KinaseDRxMetz
DAPK1active (1600nM)-
DAPK2active (2500nM)-
DAPK3active (1200nM)active (199.53nM)
DRAK1inactive (5200nM)inactive (3162.28nM)
DRAK2inactive (5200nM)-
CAMK - DCAMKL

Bioactivity
KinaseDRxMetz
DCLK1inactive (10001nM)inactive (>10000nM)
DCLK2inactive (10001nM)-
DCLK3inactive (10001nM)-
CAMK - MAPKAPK

Bioactivity
KinaseDRxMetz
MAPKAPK2inactive (10001nM)inactive (1258.93nM)
MAPKAPK5inactive (10001nM)inactive (>1584.89nM)
MNK1inactive (10001nM)-
MNK2inactive (3400nM)inactive (1258.93nM)
MAPKAPK3-inactive (>10000nM)
CAMK - MLCK

Bioactivity
KinaseDRxMetz
caMLCKactive (400nM)-
smMLCKactive (870nM)-
skMLCKinactive (10001nM)-
SgK085active (1500nM)-
CAMK - PHK

Bioactivity
KinaseDRxMetz
PHKg1active (1200nM)-
PHKg2active (2600nM)active (1000nM)
CAMK - PIM

Bioactivity
KinaseDRxMetz
PIM1active (180nM)active (100nM)
PIM2active (220nM)active (79.43nM)
PIM3active (140nM)active (63.1nM)
CAMK - PKD

Bioactivity
KinaseDRxMetz
PKD1inactive (10001nM)-
PKD2inactive (10001nM)active (316.23nM)
PKD3active (1000nM)active (158.49nM)
CAMK - STK33

Bioactivity
KinaseDRxMetz
STK33active (220nM)-
CAMK - TSSK

Bioactivity
KinaseDRxMetz
TSSK1inactive (10001nM)active (630.96nM)
TSSK2-inactive (>1584.89nM)

STE


Test Member No. in Family
Familyno. Member on 518kinaseDRxMetz
88-
31279
772
STE - STE11

Bioactivity
KinaseDRxMetz
MAP3K5inactive (10001nM)-
MAP3K6inactive (10001nM)-
MAP3K1inactive (10001nM)-
MAP3K7inactive (10001nM)-
MAP3K2inactive (10001nM)-
MAP3K3inactive (10001nM)-
MAP3K4inactive (10001nM)-
MAP3K8active (230nM)-
STE - STE20

Bioactivity
KinaseDRxMetz
HPK1inactive (10001nM)-
LOKinactive (10001nM)-
GCKactive (1900nM)active (63.1nM)
KHS2inactive (10001nM)-
HGKactive (140nM)active (6.31nM)
KHS1inactive (10001nM)active (794.33nM)
MINKactive (100nM)active (50.12nM)
MST1inactive (10001nM)-
MST2inactive (5400nM)active (630.96nM)
MST3inactive (10001nM)-
MST4inactive (10001nM)-
MYO3Ainactive (10001nM)-
MYO3Binactive (10001nM)-
OSR1inactive (10001nM)-
PAK1active (1500nM)inactive (7943.28nM)
PAK2active (1500nM)-
PAK3inactive (10001nM)-
PAK4active (980nM)inactive (2511.89nM)
PAK6active (760nM)-
PAK5active (670nM)-
SLKinactive (10001nM)inactive (1584.89nM)
STLK3inactive (10001nM)-
TAO1active (470nM)active (1000nM)
TAO2inactive (4900nM)-
TAO3active (1100nM)-
TNIKactive (140nM)-
YSK1inactive (10001nM)-
STE - STE7

Bioactivity
KinaseDRxMetz
MAP2K1inactive (10001nM)-
MAP2K2inactive (10001nM)-
MAP2K3active (1200nM)-
MAP2K4inactive (10001nM)-
MAP2K5inactive (10001nM)-
MAP2K6inactive (10001nM)-
MAP2K7inactive (10001nM)-

CMGC


Test Member No. in Family
Familyno. Member on 518kinaseDRxMetz
2087
54-
442
321
1086
14148
222
32-
331
CMGC - CDK

Bioactivity
KinaseDRxMetz
PITSLREinactive (10001nM)-
CHEDinactive (3100nM)-
CDK11active (1300nM)-
PCTAIRE1active (1500nM)-
PCTAIRE2active (1900nM)-
PCTAIRE3inactive (7700nM)-
PFTAIRE2active (2100nM)-
PFTAIRE1active (790nM)-
CDC2-active (158.49nM)
CDK2-active (79.43nM)
CDK5-active (125.89nM)
CDK8--
CDK7--
CDK9--
CMGC - CDKL

Bioactivity
KinaseDRxMetz
CDKL1inactive (10001nM)-
CDKL2active (700nM)-
CDKL3active (1100nM)-
CDKL5active (200nM)-
CMGC - CLK

Bioactivity
KinaseDRxMetz
CLK1active (1.4nM)-
CLK2active (0.51nM)-
CLK3active (160nM)-
CLK4active (0.53nM)-
CMGC - CK2

Bioactivity
KinaseDRxMetz
CK2a1inactive (5500nM)active (316.23nM)
CK2a2inactive (3800nM)-
CMGC - DYRK

Bioactivity
KinaseDRxMetz
DYRK1Aactive (2.1nM)-
DYRK1Bactive (3.9nM)-
DYRK2active (63nM)-
HIPK1active (230nM)-
HIPK2active (220nM)active (251.19nM)
HIPK3active (110nM)-
HIPK4active (760nM)inactive (1258.93nM)
PRP4inactive (4600nM)-
DYRK3-active (251.19nM)
DYRK4-active (630.96nM)
CMGC - MAPK

Bioactivity
KinaseDRxMetz
Erk1inactive (10001nM)-
Erk2inactive (10001nM)active (398.11nM)
Erk3inactive (10001nM)-
Erk4inactive (10001nM)-
Erk5inactive (10001nM)-
Erk7active (89nM)-
JNK1inactive (10001nM)inactive (>3162.28nM)
JNK2inactive (10001nM)inactive (>3981.07nM)
JNK3inactive (10001nM)-
NLKinactive (10001nM)-
p38ainactive (10001nM)-
p38binactive (10001nM)-
p38dinactive (10001nM)inactive (5011.87nM)
p38ginactive (10001nM)inactive (3162.28nM)
CMGC - GSK

Bioactivity
KinaseDRxMetz
GSK3Ainactive (3900nM)active (316.23nM)
GSK3Bactive (350nM)active (63.1nM)
CMGC - RCK

Bioactivity
KinaseDRxMetz
ICKactive (550nM)-
MAKinactive (10001nM)-
CMGC - SRPK

Bioactivity
KinaseDRxMetz
SRPK1active (550nM)inactive (5011.87nM)
SRPK2active (1100nM)-
MSSK1active (1500nM)-

CK1


Test Member No. in Family
Familyno. Member on 518kinaseDRxMetz
775
31-
CK1 - CK1

Bioactivity
KinaseDRxMetz
CK1aactive (2100nM)inactive (1258.93nM)
CK1a2inactive (4600nM)-
CK1dactive (210nM)active (251.19nM)
CK1eactive (120nM)-
CK1g1active (530nM)active (398.11nM)
CK1g2active (380nM)active (316.23nM)
CK1g3active (910nM)active (501.19nM)
CK1 - VRK

Bioactivity
KinaseDRxMetz
VRK2inactive (4000nM)-