Compound Information
Test on : DRxCompound Name : 5-[(2,6-dichlorophenyl)methylsulfonyl]-3-[[3,5-dimethyl-4-[oxo-[(2R)-2-(1-pyrrolidinylmethyl)-1-pyrrolidinyl]methyl]-1H-pyrrol-2-yl]methylidene]-1H-indol-2-oneInchikey : OYONTEXKYJZFHA-OAQYLSRUSA-NPubchem CID : 66596670
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 (320nM) BIKE active (47nM) GAK active (1300nM) MPSK1 inactive (4800nM)
Other - Aur Bioactivity Kinase DRx AurA inactive (10001nM) AurB active (2000nM) AurC active (300nM)
Other - CAMKK Bioactivity Kinase DRx CaMKK1 active (64nM) CaMKK2 active (73nM)
Other - PEK Bioactivity Kinase DRx HRI inactive (10001nM) PKR inactive (10001nM)
Other - IRE Bioactivity Kinase DRx IRE1 inactive (10001nM)
Other - IKK Bioactivity Kinase DRx IKKa inactive (10001nM) IKKb inactive (10001nM) IKKe active (700nM) TBK1 active (970nM)
Other - NEK Bioactivity Kinase DRx NEK1 inactive (10001nM) NEK11 inactive (10001nM) NEK2 active (600nM) NEK3 inactive (10001nM) NEK4 inactive (10001nM) NEK5 inactive (10001nM) NEK6 inactive (10001nM) NEK7 inactive (10001nM) NEK9 inactive (10001nM)
Other - WEE Bioactivity Kinase DRx MYT1 inactive (10001nM) Wee1 inactive (10001nM) Wee1B inactive (10001nM)
Other - PLK Bioactivity Kinase DRx PLK1 inactive (10001nM) PLK2 inactive (8300nM) PLK3 inactive (10001nM) PLK4 active (410nM)
Other - SgK496 Bioactivity Kinase DRx SgK496 inactive (10001nM)
Other - NKF1 Bioactivity Kinase DRx SBK inactive (10001nM) SgK110 inactive (10001nM)
Other - NKF4 Bioactivity Kinase DRx CLIK1 inactive (10001nM)
Other - ULK Bioactivity Kinase DRx Fused inactive (10001nM) ULK1 active (2000nM) ULK2 active (1500nM) ULK3 inactive (10001nM)
Other - TLK Bioactivity Kinase DRx TLK1 inactive (10001nM) TLK2 inactive (10001nM)
Other - TTK Bioactivity Kinase DRx TTK inactive (10001nM)
TK
TK - Abl Bioactivity Kinase DRx ABL1 active (2600nM) ABL2 inactive (6900nM)
TK - ALK Bioactivity Kinase DRx ALK active (2700nM) LTK inactive (10001nM)
TK - Axl Bioactivity Kinase DRx AXL active (110nM) MER active (1300nM) TYRO3 active (2000nM)
TK - Src Bioactivity Kinase DRx BLK active (1900nM) BRK inactive (10001nM) FGR active (1900nM) FRK inactive (10001nM) FYN inactive (10001nM) HCK inactive (10001nM) LCK active (320nM) LYN inactive (10001nM) SRC inactive (10001nM) SRM inactive (10001nM) YES active (1400nM)
TK - Tec Bioactivity Kinase DRx BMX inactive (10001nM) BTK inactive (10001nM) ITK inactive (10001nM) TEC inactive (10001nM) TXK inactive (10001nM)
TK - PDGFR Bioactivity Kinase DRx FMS active (700nM) FLT3 active (250nM) KIT inactive (3200nM) PDGFRa active (2000nM) PDGFRb active (1900nM)
TK - Csk Bioactivity Kinase DRx CSK inactive (10001nM) CTK inactive (10001nM)
TK - DDR Bioactivity Kinase DRx DDR1 active (70nM) DDR2 inactive (7600nM)
TK - EGFR Bioactivity Kinase DRx EGFR inactive (10001nM) ErbB2 inactive (10001nM) ErbB3 inactive (10001nM) ErbB4 inactive (10001nM)
TK - Eph Bioactivity Kinase DRx EphA1 inactive (10001nM) EphA2 inactive (10001nM) EphA3 inactive (10001nM) EphA4 inactive (10001nM) EphA5 inactive (10001nM) EphA6 inactive (10001nM) EphA7 inactive (10001nM) EphA8 inactive (3900nM) EphB1 inactive (10001nM) EphB2 inactive (10001nM) EphB3 inactive (10001nM) EphB4 inactive (10001nM) EphB6 active (2900nM)
TK - FAK Bioactivity Kinase DRx FAK active (1900nM) PYK2 active (910nM)
TK - Fer Bioactivity Kinase DRx FER inactive (10001nM) FES inactive (10001nM)
TK - FGFR Bioactivity Kinase DRx FGFR1 inactive (10001nM) FGFR2 inactive (5200nM) FGFR3 inactive (5200nM) FGFR4 inactive (10001nM)
TK - VEGFR Bioactivity Kinase DRx FLT1 inactive (10001nM) FLT4 active (1400nM) KDR inactive (10001nM)
TK - InsR Bioactivity Kinase DRx IGF1R inactive (10001nM) INSR active (2300nM) IRR inactive (3500nM)
TK - JakA Bioactivity Kinase DRx JAK1 inactive (10001nM) JAK2 active (430nM) JAK3 active (470nM) TYK2 inactive (10001nM)
TK - Met Bioactivity Kinase DRx MET active (0.27nM) RON active (2000nM)
TK - Musk Bioactivity Kinase DRx MUSK inactive (10001nM)
TK - Ret Bioactivity Kinase DRx RET active (690nM)
TK - Sev Bioactivity Kinase DRx ROS active (3000nM)
TK - Syk Bioactivity Kinase DRx SYK inactive (10001nM) ZAP70 inactive (10001nM)
TK - Tie Bioactivity Kinase DRx TIE1 active (1200nM) TIE2 inactive (6700nM)
TK - Ack Bioactivity Kinase DRx TNK1 inactive (10001nM) ACK inactive (10001nM)
TK - Trk Bioactivity Kinase DRx TRKA active (320nM) TRKB active (800nM) TRKC active (930nM)
TKL
TKL - STKR Bioactivity Kinase DRx ALK2 inactive (10001nM) ALK4 inactive (10001nM) ACTR2 inactive (10001nM) ACTR2B inactive (10001nM) ALK1 inactive (10001nM) BMPR1A inactive (10001nM) BMPR1B inactive (10001nM) BMPR2 inactive (6200nM) TGFbR1 inactive (10001nM) TGFbR2 inactive (10001nM)
TKL - RIPK Bioactivity Kinase DRx SgK288 inactive (10001nM) RIPK1 active (1500nM) RIPK2 inactive (10001nM) ANKRD3 inactive (10001nM)
TKL - RAF Bioactivity Kinase DRx BRAF inactive (10001nM) RAF1 inactive (10001nM)
TKL - MLK Bioactivity Kinase DRx DLK active (670nM) LZK inactive (3200nM) MLK1 inactive (10001nM) MLK2 inactive (10001nM) MLK3 inactive (10001nM) TAK1 inactive (5300nM) HH498 inactive (10001nM) ZAK inactive (10001nM)
TKL - IRAK Bioactivity Kinase DRx IRAK1 active (1600nM) IRAK3 active (610nM) IRAK4 active (2500nM)
TKL - LISK Bioactivity Kinase DRx LIMK1 inactive (10001nM) LIMK2 inactive (10001nM) TESK1 inactive (10001nM)
TKL - LRRK Bioactivity Kinase DRx LRRK2 inactive (10001nM)
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 (470nM) RIOK2 inactive (10001nM) RIOK3 active (390nM)
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 inactive (10001nM) DMPK1 inactive (10001nM) DMPK2 inactive (10001nM) MRCKa inactive (10001nM) MRCKb inactive (10001nM) ROCK1 inactive (10001nM) ROCK2 inactive (8700nM)
AGC - GRK Bioactivity Kinase DRx RHOK active (1100nM) GPRK4 active (420nM) GPRK7 active (61nM)
AGC - NDR Bioactivity Kinase DRx LATS1 inactive (10001nM) LATS2 inactive (10001nM) NDR1 inactive (10001nM) NDR2 inactive (10001nM)
AGC - MAST Bioactivity Kinase DRx MAST1 inactive (10001nM)
AGC - PDK1 Bioactivity Kinase DRx PDK1 inactive (10001nM)
AGC - PKA Bioactivity Kinase DRx PKACa inactive (10001nM) PKACb inactive (10001nM) PRKX inactive (10001nM)
AGC - PKN Bioactivity Kinase DRx PKN1 inactive (10001nM) PKN2 inactive (10001nM)
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 inactive (10001nM) PKG2 inactive (10001nM)
AGC - RSK Bioactivity Kinase DRx p70S6K inactive (4100nM)
AGC - SGK Bioactivity Kinase DRx SGK3 inactive (10001nM)
AGC - YANK Bioactivity Kinase DRx YANK1 inactive (10001nM) YANK2 inactive (10001nM) YANK3 inactive (10001nM)
CAMK
CAMK - CAMKL Bioactivity Kinase DRx AMPKa1 active (310nM) AMPKa2 active (770nM) NuaK1 active (620nM) BRSK1 inactive (10001nM) BRSK2 inactive (10001nM) CHK1 inactive (10001nM) HUNK active (1400nM) LKB1 active (2600nM) MARK1 inactive (10001nM) MARK2 inactive (3600nM) MARK3 inactive (10001nM) MARK4 inactive (10001nM) MELK inactive (10001nM) NIM1 inactive (8700nM) QSK inactive (10001nM) SIK inactive (10001nM) QIK active (2500nM) NuaK2 active (910nM) SNRK inactive (10001nM)
CAMK - CAMK1 Bioactivity Kinase DRx CaMK1a active (2100nM) CaMK1d active (1500nM) CaMK1g inactive (10001nM) CaMK4 inactive (10001nM)
CAMK - CAMK2 Bioactivity Kinase DRx CaMK2a inactive (3400nM) CaMK2b inactive (10001nM) CaMK2d active (2900nM) CaMK2g active (2000nM)
CAMK - CASK Bioactivity Kinase DRx CASK active (1700nM)
CAMK - RAD53 Bioactivity Kinase DRx CHK2 inactive (10001nM)
CAMK - DAPK Bioactivity Kinase DRx DAPK1 inactive (10001nM) DAPK2 inactive (10001nM) DAPK3 inactive (10001nM) DRAK1 inactive (4000nM) DRAK2 inactive (3500nM)
CAMK - DCAMKL Bioactivity Kinase DRx DCLK1 active (1400nM) DCLK2 active (990nM) DCLK3 inactive (4500nM)
CAMK - MAPKAPK Bioactivity Kinase DRx MAPKAPK2 inactive (10001nM) MAPKAPK5 inactive (10001nM) MNK1 inactive (10001nM) MNK2 inactive (10001nM)
CAMK - MLCK Bioactivity Kinase DRx caMLCK inactive (10001nM) smMLCK inactive (7900nM) skMLCK active (960nM) SgK085 inactive (10001nM)
CAMK - PHK Bioactivity Kinase DRx PHKg1 active (1900nM) PHKg2 active (2400nM)
CAMK - PIM Bioactivity Kinase DRx PIM1 inactive (10001nM) PIM2 inactive (10001nM) PIM3 inactive (10001nM)
CAMK - PKD Bioactivity Kinase DRx PKD1 inactive (10001nM) PKD2 inactive (10001nM) PKD3 inactive (10001nM)
CAMK - STK33 Bioactivity Kinase DRx STK33 active (840nM)
CAMK - TSSK Bioactivity Kinase DRx TSSK1 active (2100nM)
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 inactive (5200nM) MAP3K3 inactive (5900nM) MAP3K4 active (1800nM) MAP3K8 active (78nM)
STE - STE20 Bioactivity Kinase DRx HPK1 active (150nM) LOK active (290nM) GCK inactive (3600nM) KHS2 active (490nM) HGK active (280nM) KHS1 active (79nM) MINK active (250nM) MST1 inactive (10001nM) MST2 active (1900nM) MST3 inactive (10001nM) MST4 inactive (3800nM) MYO3A inactive (10001nM) MYO3B inactive (10001nM) OSR1 inactive (10001nM) PAK1 active (2900nM) PAK2 inactive (10001nM) PAK3 active (1100nM) PAK4 inactive (10001nM) PAK6 inactive (10001nM) PAK5 active (2600nM) SLK active (350nM) STLK3 inactive (10001nM) TAO1 active (460nM) TAO2 active (1200nM) TAO3 active (43nM) TNIK active (310nM) YSK1 inactive (10001nM)
STE - STE7 Bioactivity Kinase DRx MAP2K1 active (1100nM) MAP2K2 active (980nM) MAP2K3 inactive (10001nM) MAP2K4 inactive (10001nM) MAP2K5 active (1400nM) MAP2K6 inactive (10001nM) MAP2K7 inactive (10001nM)
CMGC
CMGC - CDK Bioactivity Kinase DRx PITSLRE inactive (10001nM) CHED inactive (10001nM) CDK11 inactive (10001nM) PCTAIRE1 active (1100nM) PCTAIRE2 active (880nM) PCTAIRE3 active (1500nM) PFTAIRE2 active (510nM) PFTAIRE1 active (1300nM)
CMGC - CDKL Bioactivity Kinase DRx CDKL1 inactive (10001nM) CDKL2 active (2400nM) CDKL3 inactive (10001nM) CDKL5 inactive (10001nM)
CMGC - CLK Bioactivity Kinase DRx CLK1 active (730nM) CLK2 active (410nM) CLK3 inactive (3600nM) CLK4 inactive (10001nM)
CMGC - CK2 Bioactivity Kinase DRx CK2a1 inactive (10001nM) CK2a2 inactive (5600nM)
CMGC - DYRK Bioactivity Kinase DRx DYRK1A inactive (10001nM) DYRK1B inactive (10001nM) DYRK2 inactive (10001nM) HIPK1 active (93nM) HIPK2 active (120nM) HIPK3 active (63nM) HIPK4 active (1300nM) PRP4 active (2600nM)
CMGC - MAPK Bioactivity Kinase DRx Erk1 inactive (10001nM) Erk2 inactive (10001nM) Erk3 inactive (10001nM) Erk4 inactive (10001nM) Erk5 active (1700nM) Erk7 inactive (10001nM) JNK1 inactive (10001nM) JNK2 inactive (10001nM) JNK3 inactive (10001nM) NLK inactive (10001nM) p38a inactive (10001nM) p38b inactive (10001nM) p38d inactive (10001nM) p38g inactive (10001nM)
CMGC - GSK Bioactivity Kinase DRx GSK3A inactive (10001nM) GSK3B inactive (10001nM)
CMGC - RCK Bioactivity Kinase DRx ICK active (400nM) MAK active (890nM)
CMGC - SRPK Bioactivity Kinase DRx SRPK1 active (41nM) SRPK2 active (500nM) MSSK1 active (1600nM)
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 inactive (10001nM) CK1a2 inactive (10001nM) CK1d inactive (4200nM) CK1e active (860nM) CK1g1 inactive (10001nM) CK1g2 inactive (10001nM) CK1g3 inactive (10001nM)
CK1 - VRK Bioactivity Kinase DRx VRK2 inactive (10001nM)