Compound Information
Test on : RBC, Millipore
Compound Name
RBC : REL-(9R,12S)-9,10,11,12-TETRAHYDRO-9,12-EPOXY-1H-DIINDOLO[1,2,3-FG:3',2',1'-KL]PYRROLO[3,4-I][1,6]BENZODIAZOCINE-1,3(2H)-DIONE
Millipore : SB 218078
Inchikey
Same : OTPNDVKVEAIXTI-N
RBC : OTPNDVKVEAIXTI-IYBDPMFKSA-N
Millipore : OTPNDVKVEAIXTI-UHFFFAOYSA-N
ChemSpider
RBC : 394549
Millipore : 2632300
Pubchem CID
RBC : 447446
Millipore : 3387354
ChEMBL
RBC : CHEMBL289422
Millipore : CHEMBL304428
RBC | Millipore |
| |
|
DRx |
RBC |
Metz |
Millipore |
GPCR |
bioactivity |
Kd (nM) |
Remain Activity (%) |
Ki (nM) |
Remain Activity (%) |
Inhibition (%) |
active criteria |
<3000nM |
<50% |
<1000nM |
<50% |
>50% |
AGC
AGC - PDK1
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
PDK1 | active (10.62%) | active (27%) |
AGC - Akt
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
AKT1 | inactive (63.9%) | inactive (107%) |
AKT2 | active (48.52%) | inactive (101%) |
AKT3 | active (27.14%) | inactive (96%) |
AGC - DMPK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
DMPK1 | inactive (98.85%) | inactive (110%) |
MRCKa | inactive (84.03%) | inactive (116%) |
MRCKb | inactive (101.58%) | inactive (103%) |
ROCK1 | inactive (88.7%) | inactive (110%) |
ROCK2 | inactive (73.67%) | inactive (101%) |
AGC - GRK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
BARK1 | inactive (97.92%) | - |
BARK2 | inactive (101.24%) | - |
GPRK4 | inactive (77%) | - |
GPRK5 | inactive (88.73%) | inactive (105%) |
GPRK6 | inactive (55.58%) | inactive (104%) |
GPRK7 | inactive (53.41%) | inactive (109%) |
AGC - RSK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
MSK1 | active (9.88%) | active (41%) |
MSK2 | active (12.36%) | inactive (56%) |
p70S6K | active (2.38%) | inactive (51%) |
p70S6Kb | active (35.01%) | - |
RSK2 | active (2.35%) | active (11%) |
RSK4 | active (1.08%) | active (9%) |
RSK1 | active (1.58%) | active (8%) |
RSK3 | active (1.33%) | active (13%) |
AGC - PKA
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
PKACg | active (39.81%) | - |
PRKX | active (17.46%) | inactive (84%) |
PKACa | active (44.74%) | inactive (70%) |
AGC - PKC
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
PKCa | active (13.94%) | inactive (96%) |
PKCd | active (19.05%) | inactive (103%) |
PKCe | active (28.44%) | inactive (116%) |
PKCh | active (47.62%) | inactive (89%) |
PKCg | active (32.85%) | inactive (92%) |
PKCi | inactive (86.42%) | inactive (115%) |
PKCt | active (43.17%) | active (7%) |
PKCz | inactive (87.41%) | inactive (111%) |
PKCb | active (6.42%) | - |
AGC - PKG
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
PKG2 | active (6.01%) | - |
PKG1 | active (35.65%) | - |
AGC - PKN
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
PKN1 | active (2.68%) | - |
PKN2 | active (15.9%) | active (47%) |
AGC - SGK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
SGK1 | active (23.85%) | inactive (53%) |
SGK2 | active (18.57%) | inactive (77%) |
SGK3 | inactive (71.7%) | inactive (98%) |
AGC - NDR
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
NDR1 | active (46.19%) | - |
TK
TK - Abl
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
ABL1 | inactive (72.66%) | inactive (114%) |
ABL2 | inactive (68.05%) | inactive (103%) |
TK - Ack
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
ACK | active (2.39%) | active (8%) |
TK - ALK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
ALK | active (36.91%) | inactive (81%) |
LTK | active (21.81%) | - |
TK - Axl
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
AXL | active (38.13%) | inactive (91%) |
MER | active (13.63%) | active (34%) |
TYRO3 | inactive (55.28%) | inactive (70%) |
TK - Src
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
BLK | active (37.68%) | inactive (101%) |
BRK | inactive (83.92%) | inactive (100%) |
SRC | inactive (69.51%) | inactive (103%) |
FGR | active (30.86%) | inactive (102%) |
FRK | inactive (101.52%) | inactive (71%) |
FYN | inactive (59.91%) | inactive (81%) |
HCK | active (24.79%) | inactive (76%) |
LCK | active (36.21%) | active (50%) |
SRM | inactive (104.62%) | - |
YES | active (31.86%) | inactive (115%) |
LYN | active (35.38%) | active (10%) |
TK - Tec
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
BMX | active (27.48%) | active (14%) |
BTK | active (43.26%) | active (22%) |
ITK | active (8.29%) | inactive (88%) |
TEC | inactive (142.03%) | - |
TXK | active (22.69%) | inactive (71%) |
TK - PDGFR
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
KIT | inactive (60.84%) | inactive (101%) |
FLT3 | active (0.19%) | active (24%) |
FMS | active (29.34%) | active (30%) |
PDGFRb | active (19.08%) | inactive (90%) |
PDGFRa | active (32.83%) | inactive (93%) |
TK - Csk
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
CSK | inactive (79.7%) | inactive (111%) |
CTK | inactive (91.75%) | - |
TK - DDR
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
DDR2 | inactive (80.13%) | inactive (77%) |
TK - EGFR
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
EGFR | inactive (78.34%) | inactive (102%) |
ErbB2 | inactive (98.38%) | - |
ErbB4 | inactive (72.46%) | inactive (118%) |
TK - Eph
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
EphA1 | inactive (90.12%) | inactive (113%) |
EphA2 | inactive (91.26%) | inactive (94%) |
EphA3 | inactive (96.53%) | inactive (102%) |
EphA4 | inactive (91.44%) | inactive (112%) |
EphA5 | inactive (78.68%) | inactive (94%) |
EphA6 | inactive (63.93%) | - |
EphA7 | inactive (69.21%) | inactive (100%) |
EphA8 | inactive (89.87%) | inactive (96%) |
EphB1 | inactive (80.21%) | inactive (112%) |
EphB2 | inactive (98.38%) | inactive (104%) |
EphB3 | inactive (93.23%) | inactive (118%) |
EphB4 | inactive (75.42%) | inactive (107%) |
TK - FAK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
FAK | active (23.48%) | inactive (105%) |
PYK2 | active (41.51%) | inactive (90%) |
TK - Fer
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
FER | active (5.39%) | active (33%) |
FES | active (42.08%) | inactive (90%) |
TK - FGFR
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
FGFR1 | active (29.13%) | inactive (72%) |
FGFR2 | active (34.11%) | inactive (83%) |
FGFR3 | active (36.32%) | inactive (82%) |
FGFR4 | inactive (70.4%) | inactive (103%) |
TK - VEGFR
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
FLT1 | active (13.31%) | active (7%) |
FLT4 | active (4.97%) | active (0%) |
KDR | active (4.55%) | active (38%) |
TK - InsR
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
IGF1R | inactive (63.79%) | inactive (73%) |
IRR | active (7.16%) | inactive (74%) |
INSR | active (17.19%) | inactive (94%) |
TK - JakA
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
JAK1 | active (22.22%) | - |
JAK2 | active (14.19%) | inactive (86%) |
JAK3 | active (1.87%) | active (8%) |
TYK2 | active (4.32%) | - |
TK - Musk
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
MUSK | active (25.83%) | inactive (103%) |
TK - Ret
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
RET | active (3.21%) | active (37%) |
TK - Met
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
RON | inactive (87.75%) | inactive (92%) |
MET | inactive (76.89%) | inactive (130%) |
TK - Sev
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
ROS | active (1.6%) | inactive (94%) |
TK - Syk
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
SYK | active (15.79%) | inactive (90%) |
ZAP70 | inactive (88.44%) | inactive (132%) |
TK - Tie
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
TIE2 | inactive (94.13%) | inactive (97%) |
TK - Trk
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
TRKA | active (4.98%) | active (12%) |
TRKB | active (6.87%) | active (19%) |
TRKC | active (1.41%) | - |
TKL
TKL - STKR
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
ALK1 | inactive (78.58%) | - |
ALK2 | inactive (85.82%) | - |
ALK4 | inactive (113.16%) | inactive (90%) |
TGFbR1 | inactive (110.47%) | inactive (114%) |
TGFbR2 | inactive (70.34%) | - |
TKL - RAF
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
ARAF | inactive (126.66%) | - |
BRAF | inactive (105.05%) | - |
RAF1 | inactive (120.59%) | inactive (77%) |
TKL - IRAK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
IRAK1 | active (37.52%) | inactive (101%) |
IRAK4 | active (14.04%) | active (38%) |
TKL - LISK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
LIMK1 | active (49.34%) | inactive (106%) |
TKL - LRRK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
LRRK2 | active (1.91%) | - |
TKL - MLK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
MLK1 | active (8.72%) | active (1%) |
MLK2 | active (2.66%) | - |
MLK3 | active (1.37%) | - |
TAK1 | active (6.06%) | inactive (88%) |
ZAK | inactive (89.7%) | - |
TKL - RIPK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
RIPK2 | inactive (79.65%) | inactive (105%) |
CAMK
CAMK - CAMKL
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
NuaK1 | active (2.09%) | active (39%) |
BRSK1 | active (14.81%) | inactive (98%) |
BRSK2 | active (13.56%) | inactive (53%) |
CHK1 | active (3.63%) | active (25%) |
LKB1 | inactive (50.46%) | inactive (106%) |
MARK1 | active (10.43%) | active (38%) |
MARK3 | active (8.53%) | - |
MARK4 | active (5.31%) | - |
MELK | active (7.13%) | inactive (55%) |
PASK | active (43.27%) | inactive (117%) |
QIK | active (33.92%) | - |
NuaK2 | inactive (52%) | - |
MARK2 | active (4.88%) | inactive (63%) |
AMPKa1 | - | inactive (74%) |
AMPKa2 | - | inactive (55%) |
SIK | - | inactive (123%) |
CAMK - CAMK1
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
CaMK1a | inactive (69.74%) | inactive (63%) |
CaMK1b | inactive (50.49%) | - |
CaMK1d | active (33.57%) | inactive (89%) |
CaMK1g | inactive (56.53%) | - |
CaMK4 | inactive (98.71%) | inactive (90%) |
CAMK - CAMK2
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
CaMK2a | active (2.84%) | - |
CaMK2b | active (9.85%) | active (32%) |
CaMK2d | active (7.03%) | active (-1%) |
CaMK2g | active (8.36%) | active (0%) |
CAMK - RAD53
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
CHK2 | active (13%) | active (26%) |
CAMK - DAPK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
DAPK1 | active (32.66%) | active (49%) |
DAPK2 | active (39.35%) | inactive (54%) |
DRAK1 | active (8.65%) | active (16%) |
DAPK3 | active (24.58%) | inactive (80%) |
CAMK - DCAMKL
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
DCLK2 | inactive (89.62%) | inactive (77%) |
CAMK - MAPKAPK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
MAPKAPK2 | inactive (99.24%) | inactive (104%) |
MAPKAPK3 | inactive (93.06%) | inactive (95%) |
MAPKAPK5 | inactive (80.43%) | inactive (90%) |
MNK1 | active (48.64%) | - |
MNK2 | active (9.71%) | inactive (97%) |
CAMK - MLCK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
smMLCK | active (4.01%) | inactive (90%) |
skMLCK | active (7.76%) | - |
CAMK - PHK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
PHKg1 | active (2.75%) | - |
PHKg2 | inactive (75.57%) | inactive (112%) |
CAMK - PIM
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
PIM1 | active (0.44%) | active (-2%) |
PIM2 | active (1.86%) | active (6%) |
PIM3 | active (0.24%) | active (38%) |
CAMK - PKD
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
PKD1 | active (1.89%) | inactive (87%) |
PKD3 | active (-0.05%) | - |
PKD2 | active (2.02%) | inactive (92%) |
CAMK - TSSK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
TSSK1 | active (17.7%) | inactive (92%) |
TSSK2 | inactive (87.15%) | inactive (82%) |
CAMK - STK33
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
STK33 | active (12.73%) | inactive (106%) |
STE
STE - STE11
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
MAP3K5 | inactive (56.2%) | inactive (96%) |
MAP3K2 | active (13.97%) | - |
MAP3K3 | active (18.37%) | - |
STE - STE-Unique
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
COT | inactive (94.63%) | - |
NIK | inactive (134.48%) | - |
STE - STE20
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
GCK | active (3.75%) | active (20%) |
HGK | active (0.99%) | - |
KHS1 | active (2.69%) | - |
LOK | active (9.25%) | inactive (116%) |
MINK | active (0.9%) | inactive (86%) |
MST1 | active (3.56%) | active (19%) |
MST2 | active (3.22%) | active (10%) |
MST3 | active (14.25%) | inactive (80%) |
MST4 | active (20.52%) | - |
OSR1 | inactive (92.41%) | - |
PAK1 | active (23.61%) | - |
PAK2 | active (43.9%) | inactive (91%) |
PAK3 | active (41.67%) | inactive (79%) |
PAK4 | inactive (75.29%) | inactive (84%) |
PAK5 | inactive (64.66%) | inactive (120%) |
PAK6 | inactive (85.4%) | active (19%) |
SLK | active (25.97%) | - |
YSK1 | active (34.36%) | - |
STLK3 | inactive (88.33%) | - |
TAO1 | inactive (66.92%) | inactive (75%) |
TAO2 | inactive (57.41%) | inactive (113%) |
TAO3 | active (24.47%) | inactive (96%) |
MYO3B | active (19.07%) | - |
STE - STE7
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
MAP2K1 | active (29.48%) | active (40%) |
MAP2K2 | inactive (87.94%) | - |
MAP2K6 | active (19.27%) | active (27%) |
MAP2K7 | - | inactive (100%) |
Other
Other - Aur
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
AurA | active (22.28%) | inactive (95%) |
AurB | active (9.52%) | active (2%) |
AurC | active (36.48%) | inactive (104%) |
Other - CAMKK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
CaMKK1 | active (27.21%) | - |
CaMKK2 | active (7.93%) | - |
Other - Haspin
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
Haspin | active (18.46%) | active (50%) |
Other - IKK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
IKKa | inactive (106.5%) | inactive (93%) |
IKKb | inactive (97.84%) | inactive (107%) |
IKKe | active (23.86%) | - |
TBK1 | active (7.4%) | inactive (54%) |
Other - NEK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
NEK1 | inactive (50.86%) | - |
NEK11 | inactive (60.63%) | inactive (91%) |
NEK2 | inactive (93.76%) | inactive (113%) |
NEK4 | active (22.03%) | - |
NEK6 | inactive (93.08%) | inactive (108%) |
NEK7 | inactive (99.12%) | inactive (107%) |
NEK9 | active (23.41%) | - |
NEK3 | inactive (101.94%) | inactive (87%) |
Other - TOPK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
PBK | active (39.85%) | - |
Other - PLK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
PLK1 | inactive (50.22%) | inactive (88%) |
PLK2 | inactive (62.39%) | inactive (105%) |
PLK3 | inactive (52.49%) | inactive (88%) |
Other - SgK496
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
SgK496 | active (45.54%) | - |
Other - NAK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
MPSK1 | inactive (58.05%) | - |
Other - TTK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
TTK | inactive (76.43%) | - |
Other - ULK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
ULK1 | inactive (73.13%) | - |
ULK2 | inactive (89.1%) | inactive (114%) |
ULK3 | active (33%) | inactive (58%) |
Other - WEE
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
Wee1 | active (16.86%) | - |
Other - WNK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
Wnk2 | inactive (93.57%) | inactive (100%) |
Wnk3 | inactive (85.98%) | inactive (94%) |
Other - TLK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
TLK2 | active (14.11%) | inactive (62%) |
CK1
CK1
Test Member No. in Family |
---|
Family | no. Member on 518kinase | RBC | Millipore |
---|
CK1 | 7 | 6 | 4 |
VRK | 3 | 1 | 1 |
CK1 - CK1
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
CK1d | inactive (93.77%) | inactive (75%) |
CK1g1 | inactive (96.1%) | inactive (106%) |
CK1g2 | inactive (81.83%) | inactive (52%) |
CK1g3 | inactive (107.87%) | inactive (61%) |
CK1a | inactive (103.6%) | - |
CK1e | active (47.33%) | - |
CK1 - VRK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
VRK1 | inactive (90.16%) | - |
VRK2 | - | inactive (104%) |
CMGC
CMGC
Test Member No. in Family |
---|
Family | no. Member on 518kinase | RBC | Millipore |
---|
CK2 | 3 | 2 | 2 |
CLK | 4 | 4 | 2 |
DYRK | 10 | 9 | 4 |
MAPK | 14 | 10 | 10 |
GSK | 2 | 2 | 2 |
SRPK | 3 | 3 | 3 |
CMGC - CK2
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
CK2a1 | active (16.74%) | inactive (74%) |
CK2a2 | active (4.47%) | inactive (63%) |
CMGC - CLK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
CLK1 | active (43.08%) | - |
CLK2 | inactive (52.12%) | inactive (100%) |
CLK3 | inactive (97.02%) | inactive (95%) |
CLK4 | active (20.32%) | - |
CMGC - DYRK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
DYRK1A | active (8.74%) | - |
DYRK1B | active (3.15%) | - |
DYRK2 | active (5.94%) | inactive (91%) |
DYRK3 | active (16.58%) | - |
DYRK4 | inactive (87.77%) | - |
HIPK1 | inactive (93.61%) | inactive (104%) |
HIPK2 | active (32.57%) | active (42%) |
HIPK3 | active (49.89%) | active (-2%) |
HIPK4 | active (29.15%) | - |
CMGC - MAPK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
Erk1 | inactive (102.37%) | inactive (128%) |
Erk2 | inactive (88.68%) | inactive (115%) |
JNK3 | inactive (138.09%) | inactive (63%) |
NLK | inactive (74.13%) | inactive (109%) |
p38a | inactive (101.7%) | inactive (90%) |
p38b | inactive (107.94%) | inactive (115%) |
p38d | inactive (113.7%) | inactive (106%) |
p38g | inactive (112.88%) | inactive (97%) |
JNK1 | inactive (98.53%) | inactive (98%) |
JNK2 | inactive (96.15%) | inactive (102%) |
CMGC - GSK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
GSK3A | active (2.19%) | active (15%) |
GSK3B | active (4.6%) | active (40%) |
CMGC - SRPK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
MSSK1 | inactive (63.63%) | inactive (99%) |
SRPK1 | inactive (88.08%) | inactive (92%) |
SRPK2 | inactive (106.72%) | inactive (106%) |
Atypical
Atypical
Test Member No. in Family |
---|
Family | no. Member on 518kinase | RBC | Millipore |
---|
PDHK | 5 | 1 | - |
Alpha | 6 | - | 1 |
PIKK | 6 | - | 1 |
Atypical - PDHK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
PDHK1 | active (10.62%) | - |
Atypical - Alpha
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
eEF2K | - | inactive (111%) |
Atypical - PIKK
Bioactivity |
---|
Kinase | RBC | Millipore |
---|
FRAP | - | inactive (95%) |