AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: ribociclib
Target: Cyclin-dependent kinase 2 (Kinase)
Gene: CDK2
UniProt: P24941 (CDK2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.12
Assay: IMAP-FPT (Molecular Devices Trade Mark Technology) Endpoint Assay: The assay was run under the conditions identical to that for CDK1/cyclin B except 0.25 nM CDK1/cyclin B was replaced with 0.3 nM CDK2/cyclin A. A 384-well microtiter IMAP-FPT (Molecular Devices Trade Mark Technology) endpoint assay was used for CDK1/cyclin B kinase activity measurements. The same assay was used for IC50 determination of small molecule inhibitors. In general, the kinase reactions were carried out in 20 μL volumes in the reaction solution, which is composed of 2 μL compound (in 20% DMSO), 8 μL CDK1/cyclin B in the 1× Reaction Buffer (Molecular Devices, Cat. No. R8139), 10 μL substrate mixture of Tamra Histone-H1 peptide (Molecular Devices, Cat. No. R7384) and ATP (Amersham Pharmacia, Cat. No. 27-2056-01) in the 1× Reaction Buffer with 1 mM DTT freshly added. The final reaction mixture contains compound (inhibitor) with the concentration varying from 0.005-10 μM, 2% DMSO, 0.25 nM CDK1/cyclin B, 1
Drug: ribociclib
Target: Cyclin-dependent kinase 6 (Kinase)
Gene: CDK6
UniProt: Q00534 (CDK6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.409
Action type: INHIBITOR
Drug: ribociclib
Target: Cyclin-dependent kinase 4 (Kinase)
Gene: CDK4
UniProt: P11802 (CDK4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8
Action type: INHIBITOR
Drug: naldemedine
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.04
Action type: ANTAGONIST
Drug: naldemedine
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.95
Action type: ANTAGONIST
Drug: avelumab
Target: Programmed cell death 1 ligand 1 (CD molecules)
Gene: CD274
UniProt: Q9NZQ7 (PD1L1_HUMAN)
Organism: Homo sapiens
Action type: ANTIBODY BINDING
Drug: niraparib
Target: Tankyrase-2 (Enzyme)
Gene: TNKS2
UniProt: Q9H2K2 (TNKS2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.29
Assay: Inhibition of recombinant human TNKS2 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay
Drug: niraparib
Target: Tankyrase-1 (Enzyme)
Gene: TNKS
UniProt: O95271 (TNKS1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.24
Assay: Inhibition of human TANK1 C-terminal domain by trichloroacetic acid precipitation assay
Drug: niraparib
Target: Poly [ADP-ribose] polymerase 3 (Enzyme)
Gene: PARP3
UniProt: Q9Y6F1 (PARP3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.89
Assay: Inhibition of human PARP3 by trichloroacetic acid precipitation assay
Drug: niraparib
Target: Poly [ADP-ribose] polymerase 4 (Enzyme)
Gene: PARP4
UniProt: Q9UKK3 (PARP4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.48
Assay: Inhibition of human v-PARP catalytic domain by trichloroacetic acid precipitation assay
Drug: niraparib
Target: Poly [ADP-ribose] polymerase 10 (Enzyme)
Gene: PARP10
UniProt: Q53GL7 (PAR10_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.72
Assay: Inhibition of full length recombinant human His6-tagged PARP10 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay
Drug: niraparib
Target: Poly [ADP-ribose] polymerase 12 (Enzyme)
Gene: PARP12
UniProt: Q9H0J9 (PAR12_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.1
Assay: Inhibition of recombinant human His6-tagged PARP12 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay
Drug: niraparib
Target: Poly [ADP-ribose] polymerase 14 (Enzyme)
Gene: PARP14
UniProt: Q460N5 (PAR14_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.76
Assay: Inhibition of recombinant human His6-tagged PARP14 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay
Drug: niraparib
Target: Poly [ADP-ribose] polymerase 15 (Enzyme)
Gene: PARP15
UniProt: Q460N3 (PAR15_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.54
Assay: Inhibition of recombinant human His6-tagged PARP15 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay
Drug: niraparib
Target: Poly [ADP-ribose] polymerase 2 (Enzyme)
Gene: PARP2
UniProt: Q9UGN5 (PARP2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.68
Action type: INHIBITOR
Drug: niraparib
Target: Poly [ADP-ribose] polymerase 1 (Enzyme)
Gene: PARP1
UniProt: P09874 (PARP1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.42
Action type: INHIBITOR
Drug: ocrelizumab
Target: B-lymphocyte antigen CD20 (Surface antigen)
Gene: MS4A1
UniProt: P11836 (CD20_HUMAN)
Organism: Homo sapiens
Activity: Kd = 9.08
Action type: ANTIBODY BINDING
Drug: dupilumab
Target: Interleukin-4 receptor subunit alpha (Membrane receptor)
Gene: IL4R
UniProt: P24394 (IL4RA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 11.06
Action type: ANTIBODY BINDING
Assay: Value derived from an ELISA-based solution competition assay.
Drug: deutetrabenazine
Target: Synaptic vesicular amine transporter (Transporter)
Gene: SLC18A2
UniProt: Q05940 (VMAT2_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Drug: valbenazine
Target: Synaptic vesicular amine transporter (Transporter)
Gene: Slc18a2
UniProt: Q01827 (VMAT2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.73
Action type: INHIBITOR
Assay: Displacement binding assay using rat brain homogenate.
Drug: valbenazine
Target: Synaptic vesicular amine transporter (Transporter)
Gene: SLC18A2
UniProt: Q05940 (VMAT2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.523
Action type: INHIBITOR
Drug: forodesine
Target: Purine nucleoside phosphorylase (Enzyme)
Gene: PNP
UniProt: Q8T9Z7 (Q8T9Z7_PLAFA)
Organism: Plasmodium falciparum
Activity: Ki = 9.07
Assay: Inhibition of Plasmodium falciparum PNP expressed in Escherichia coli BL21(DE3) cells by spectrophotometry
Drug: forodesine
Target: Purine nucleoside phosphorylase (Enzyme)
Gene: PNP
UniProt: P55859 (PNPH_BOVIN)
Organism: Bos taurus
Activity: Ki = 10.64
Assay: Inhibitory activity of compound against bovine purine nucleoside phosphorylase (PNP)
Drug: forodesine
Target: Purine nucleoside phosphorylase (Enzyme)
Gene: PNP
UniProt: P00491 (PNPH_HUMAN)
Organism: Homo sapiens
Activity: Ki = 10.143
Action type: INHIBITOR
Drug: midostaurin
Target: Tyrosine-protein kinase JAK3 (Kinase)
Gene: JAK3
UniProt: P52333 (JAK3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.92
Assay: Binding constant for JAK3(Kin.Dom.2/JH1 - catalytic) kinase domain
Drug: midostaurin
Target: Platelet-derived growth factor receptor beta (Kinase)
Gene: PDGFRB
UniProt: P09619 (PGFRB_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.96
Assay: Binding constant for PDGFRB kinase domain
Drug: midostaurin
Target: Tyrosine-protein kinase ABL1 (Kinase)
Gene: ABL1
UniProt: P00519 (ABL1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.1
Assay: Binding constant for ABL1(T315I)-phosphorylated kinase domain
Drug: midostaurin
Target: Mast/stem cell growth factor receptor Kit (Kinase)
Gene: KIT
UniProt: P10721 (KIT_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.11
Assay: Binding constant for KIT(D816V) kinase domain
Drug: midostaurin
Target: Epidermal growth factor receptor (Kinase)
Gene: EGFR
UniProt: P00533 (EGFR_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.06
Assay: Binding constant for EGFR(L858R,T790M) kinase domain
Drug: midostaurin
Target: Proto-oncogene tyrosine-protein kinase Src (Kinase)
Gene: SRC
UniProt: P12931 (SRC_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.92
Assay: Binding constant for SRC kinase domain
Drug: midostaurin
Target: Tyrosine-protein kinase Lck (Kinase)
Gene: LCK
UniProt: P06239 (LCK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.55
Assay: Binding constant for LCK kinase domain
Drug: midostaurin
Target: Tyrosine-protein kinase Yes (Kinase)
Gene: YES1
UniProt: P07947 (YES_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.02
Assay: Binding constant for YES kinase domain
Drug: midostaurin
Target: Tyrosine-protein kinase Fyn (Kinase)
Gene: FYN
UniProt: P06241 (FYN_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.68
Assay: Binding constant for FYN kinase domain
Drug: midostaurin
Target: Proto-oncogene tyrosine-protein kinase receptor Ret (Kinase)
Gene: RET
UniProt: P07949 (RET_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.7
Assay: Binding constant for RET(V804M) kinase domain
Drug: midostaurin
Target: Vascular endothelial growth factor receptor 1 (Kinase)
Gene: FLT1
UniProt: P17948 (VGFR1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.35
Assay: Binding constant for FLT1 kinase domain
Drug: midostaurin
Target: Vascular endothelial growth factor receptor 2 (Kinase)
Gene: KDR
UniProt: P35968 (VGFR2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.6
Assay: Inhibition of recombinant GST-tagged VEGFR2 kinase domain (V789 to V1356) (unknown origin) expressed in insect Sf9 cells using polyGlu4:Tyr peptide as substrate after 120 mins by Kinase-Glo assay
Drug: midostaurin
Target: Vascular endothelial growth factor receptor 3 (Kinase)
Gene: FLT4
UniProt: P35916 (VGFR3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.17
Assay: Binding constant for FLT4 kinase domain
Drug: midostaurin
Target: Macrophage colony-stimulating factor 1 receptor (Kinase)
Gene: CSF1R
UniProt: P07333 (CSF1R_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.85
Assay: Inhibition of human FMS expressed in growth factor dependent mouse FDC-P1 cells assessed as inhibition of FMS-mediated cell proliferation in presence human CSF1 after 48 hrs by resazurin dye reduction assay
Drug: midostaurin
Target: Platelet-derived growth factor receptor alpha (Kinase)
Gene: PDGFRA
UniProt: P16234 (PGFRA_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.75
Assay: Binding affinity to PDGFRA
Drug: midostaurin
Target: Ribosomal protein S6 kinase alpha-3 (Kinase)
Gene: RPS6KA3
UniProt: P51812 (KS6A3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.13
Assay: Binding constant for RPS6KA3(Kin.Dom.1 - N-terminal) kinase domain
Drug: midostaurin
Target: Phosphorylase b kinase gamma catalytic chain, liver/testis isoform (Kinase)
Gene: PHKG2
UniProt: P15735 (PHKG2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.05
Assay: Binding affinity to PHKG2
Drug: midostaurin
Target: Serine/threonine-protein kinase pim-1 (Kinase)
Gene: PIM1
UniProt: P11309 (PIM1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.25
Assay: Binding constant for PIM1 kinase domain
Drug: midostaurin
Target: Myosin light chain kinase, smooth muscle (Kinase)
Gene: MYLK
UniProt: Q15746 (MYLK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.66
Assay: Binding affinity to MYLK
Drug: midostaurin
Target: Death-associated protein kinase 3 (Kinase)
Gene: DAPK3
UniProt: O43293 (DAPK3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.75
Assay: Binding constant for DAPK3 kinase domain
Drug: midostaurin
Target: Calcium/calmodulin-dependent protein kinase type 1 (Kinase)
Gene: CAMK1
UniProt: Q14012 (KCC1A_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.7
Assay: Binding constant for full-length CAMK1
Drug: midostaurin
Target: Mitogen-activated protein kinase 8 (Kinase)
Gene: MAPK8
UniProt: P45983 (MK08_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.36
Assay: Binding constant for full-length JNK1
Drug: midostaurin
Target: Fibroblast growth factor receptor 3 (Kinase)
Gene: FGFR3
UniProt: P22607 (FGFR3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.77
Assay: Binding constant for FGFR3 kinase domain
Drug: midostaurin
Target: Rho-associated protein kinase 1 (Kinase)
Gene: ROCK1
UniProt: Q13464 (ROCK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.11
Assay: Binding affinity to ROCK1
Drug: midostaurin
Target: Tyrosine-protein kinase HCK (Kinase)
Gene: HCK
UniProt: P08631 (HCK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.14
Assay: Binding constant for HCK kinase domain
Drug: midostaurin
Target: Tyrosine-protein kinase JAK1 (Kinase)
Gene: JAK1
UniProt: P23458 (JAK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.17
Assay: Binding affinity to JH1 catalytic domain JAK1
Drug: midostaurin
Target: Receptor tyrosine-protein kinase erbB-4 (Kinase)
Gene: ERBB4
UniProt: Q15303 (ERBB4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.51
Assay: Binding affinity to ERBB4
Drug: midostaurin
Target: Mitogen-activated protein kinase 10 (Kinase)
Gene: MAPK10
UniProt: P53779 (MK10_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.44
Assay: Binding constant for JNK3 kinase domain
Drug: midostaurin
Target: Death-associated protein kinase 2 (Kinase)
Gene: DAPK2
UniProt: Q9UIK4 (DAPK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.05
Assay: Binding constant for full-length DAPK2
Drug: midostaurin
Target: High affinity nerve growth factor receptor (Kinase)
Gene: NTRK1
UniProt: P04629 (NTRK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.42
Assay: Binding constant for TRKA kinase domain
Drug: midostaurin
Target: Protein kinase C delta type (Kinase)
Gene: PRKCD
UniProt: Q05655 (KPCD_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.5
Assay: Binding constant for PRKCD kinase domain
Drug: midostaurin
Target: cAMP-dependent protein kinase catalytic subunit beta (Kinase)
Gene: PRKACB
UniProt: P22694 (KAPCB_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.62
Assay: Binding constant for full-length PKAC-beta
Drug: midostaurin
Target: Tyrosine-protein kinase JAK2 (Kinase)
Gene: JAK2
UniProt: O60674 (JAK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.03
Assay: Binding constant for JAK2(Kin.Dom.2/JH1 - catalytic) kinase domain
Drug: midostaurin
Target: Rho-associated protein kinase 2 (Kinase)
Gene: ROCK2
UniProt: O75116 (ROCK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.64
Assay: Binding affinity to ROCK2
Drug: midostaurin
Target: Protein kinase C alpha type (Kinase)
Gene: PRKCA
UniProt: P17252 (KPCA_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.14
Assay: Binding affinity to PKAC-alpha
Drug: midostaurin
Target: Tyrosine-protein kinase SYK (Kinase)
Gene: SYK
UniProt: P43405 (KSYK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.06
Assay: Binding constant for SYK kinase domain
Drug: midostaurin
Target: Calcium/calmodulin-dependent protein kinase type II subunit delta (Kinase)
Gene: CAMK2D
UniProt: Q13557 (KCC2D_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.44
Assay: Binding constant for CAMK2D kinase domain
Drug: midostaurin
Target: Tyrosine-protein kinase CSK (Kinase)
Gene: CSK
UniProt: P41240 (CSK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.06
Assay: Binding constant for full-length CSK
Drug: midostaurin
Target: Angiopoietin-1 receptor (Kinase)
Gene: TEK
UniProt: Q02763 (TIE2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.72
Assay: Binding constant for TIE2 kinase domain
Drug: midostaurin
Target: Calcium/calmodulin-dependent protein kinase type II subunit gamma (Kinase)
Gene: CAMK2G
UniProt: Q13555 (KCC2G_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.85
Assay: Binding constant for CAMK2G kinase domain
Drug: midostaurin
Target: AP2-associated protein kinase 1 (Kinase)
Gene: AAK1
UniProt: Q2M2I8 (AAK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.32
Assay: Binding constant for AAK1 kinase domain
Drug: midostaurin
Target: Serine/threonine-protein kinase MARK2 (Kinase)
Gene: MARK2
UniProt: Q7KZI7 (MARK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7
Assay: Binding constant for MARK2 kinase domain
Drug: midostaurin
Target: Hepatocyte growth factor receptor (Kinase)
Gene: MET
UniProt: P08581 (MET_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.25
Assay: Binding constant for MET(Y1235D) kinase domain
Drug: midostaurin
Target: Tyrosine-protein kinase Lyn (Kinase)
Gene: LYN
UniProt: P07948 (LYN_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.38
Assay: Binding constant for LYN kinase domain
Drug: midostaurin
Target: Ribosomal protein S6 kinase alpha-2 (Kinase)
Gene: RPS6KA2
UniProt: Q15349 (KS6A2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.62
Assay: Binding affinity to RPS6KA5(Kin.Dom.1-N-terminal)
Drug: midostaurin
Target: 5'-AMP-activated protein kinase catalytic subunit alpha-1 (Kinase)
Gene: PRKAA1
UniProt: Q13131 (AAPK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.75
Assay: Binding constant for AMPK-alpha1 kinase domain
Drug: midostaurin
Target: Calcium/calmodulin-dependent protein kinase type II subunit beta (Kinase)
Gene: CAMK2B
UniProt: Q13554 (KCC2B_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.68
Assay: Binding constant for CAMK2B kinase domain
Drug: midostaurin
Target: Protein kinase C eta type (Kinase)
Gene: PRKCH
UniProt: P24723 (KPCL_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.54
Assay: Binding constant for PRKCH kinase domain
Drug: midostaurin
Target: Fibroblast growth factor receptor 1 (Kinase)
Gene: FGFR1
UniProt: P11362 (FGFR1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.8
Assay: Binding constant for FGFR1 kinase domain
Drug: midostaurin
Target: Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform (Kinase)
Gene: PHKG1
UniProt: Q16816 (PHKG1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.72
Assay: Binding affinity to PHKG1
Drug: midostaurin
Target: Calcium/calmodulin-dependent protein kinase type II subunit alpha (Kinase)
Gene: CAMK2A
UniProt: Q9UQM7 (KCC2A_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.7
Assay: Binding constant for CAMK2A kinase domain
Drug: midostaurin
Target: Serine/threonine-protein kinase 17B (Kinase)
Gene: STK17B
UniProt: O94768 (ST17B_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.33
Assay: Binding constant for full-length DRAK2
Drug: midostaurin
Target: Serine/threonine-protein kinase 10 (Kinase)
Gene: STK10
UniProt: O94804 (STK10_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.23
Assay: Binding constant for LOK kinase domain
Drug: midostaurin
Target: Tyrosine-protein kinase Fer (Kinase)
Gene: FER
UniProt: P16591 (FER_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.92
Assay: Binding constant for FER kinase domain
Drug: midostaurin
Target: Protein kinase C epsilon type (Kinase)
Gene: PRKCE
UniProt: Q02156 (KPCE_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.27
Assay: Binding constant for PRKCE kinase domain
Drug: midostaurin
Target: Serine/threonine-protein kinase PLK4 (Kinase)
Gene: PLK4
UniProt: O00444 (PLK4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.18
Assay: Binding constant for PLK4 kinase domain
Drug: midostaurin
Target: Aurora kinase C (Kinase)
Gene: AURKC
UniProt: Q9UQB9 (AURKC_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.77
Assay: Binding constant for full-length AURKC
Drug: midostaurin
Target: Serine/threonine-protein kinase 16 (Kinase)
Gene: STK16
UniProt: O75716 (STK16_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.55
Assay: Binding constant for STK16 kinase domain
Drug: midostaurin
Target: Dual specificity protein kinase TTK (Kinase)
Gene: TTK
UniProt: P33981 (TTK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.46
Assay: Binding constant for TTK kinase domain
Drug: midostaurin
Target: Fibroblast growth factor receptor 2 (Kinase)
Gene: FGFR2
UniProt: P21802 (FGFR2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.62
Assay: Binding constant for FGFR2 kinase domain
Drug: midostaurin
Target: Serine/threonine-protein kinase N1 (Kinase)
Gene: PKN1
UniProt: Q16512 (PKN1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.03
Assay: Binding constant for PKN1 kinase domain
Drug: midostaurin
Target: Protein kinase C theta type (Kinase)
Gene: PRKCQ
UniProt: Q04759 (KPCT_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.04
Assay: Binding constant for PRKCQ kinase domain
Drug: midostaurin
Target: Serine/threonine-protein kinase 17A (Kinase)
Gene: STK17A
UniProt: Q9UEE5 (ST17A_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.72
Assay: Binding constant for DRAK1 kinase domain
Drug: midostaurin
Target: TRAF2 and NCK-interacting protein kinase (Kinase)
Gene: TNIK
UniProt: Q9UKE5 (TNIK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.8
Assay: Binding constant for TNIK kinase domain
Drug: midostaurin
Target: Tyrosine-protein kinase Fgr (Kinase)
Gene: FGR
UniProt: P09769 (FGR_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.14
Assay: Binding constant for FGR kinase domain
Drug: midostaurin
Target: Aurora kinase A (Kinase)
Gene: AURKA
UniProt: O14965 (AURKA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.1
Assay: Inhibition of recombinant GST-tagged Aurora-A kinase domain (S123 to S401) (unknown origin) expressed in insect Sf9 cells using tetra(LRRASLG) peptide as substrate after 90 mins by Kinase-Glo assay
Drug: midostaurin
Target: ALK tyrosine kinase receptor (Kinase)
Gene: ALK
UniProt: Q9UM73 (ALK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.57
Assay: Binding constant for ALK kinase domain
Drug: midostaurin
Target: RAC-alpha serine/threonine-protein kinase (Kinase)
Gene: AKT1
UniProt: P31749 (AKT1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.02
Assay: Binding constant for AKT1 kinase domain
Drug: midostaurin
Target: BMP-2-inducible protein kinase (Kinase)
Gene: BMP2K
UniProt: Q9NSY1 (BMP2K_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.66
Assay: Binding constant for BIKE kinase domain
Drug: midostaurin
Target: Serine/threonine-protein kinase pim-2 (Kinase)
Gene: PIM2
UniProt: Q9P1W9 (PIM2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.51
Assay: Binding constant for PIM2 kinase domain
Drug: midostaurin
Target: Tyrosine-protein kinase FRK (Kinase)
Gene: FRK
UniProt: P42685 (FRK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.62
Assay: Binding constant for FRK kinase domain
Drug: midostaurin
Target: Dual specificity protein kinase CLK1 (Kinase)
Gene: CLK1
UniProt: P49759 (CLK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.46
Assay: Binding constant for full-length CLK1
Drug: midostaurin
Target: Dual specificity protein kinase CLK2 (Kinase)
Gene: CLK2
UniProt: P49760 (CLK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.07
Assay: Binding constant for CLK2 kinase domain
Drug: midostaurin
Target: Dual specificity protein kinase CLK3 (Kinase)
Gene: CLK3
UniProt: P49761 (CLK3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.44
Assay: Binding constant for CLK3 kinase domain
Drug: midostaurin
Target: Mitogen-activated protein kinase kinase kinase kinase 5 (Kinase)
Gene: MAP4K5
UniProt: Q9Y4K4 (M4K5_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.96
Assay: Binding constant for MAP4K5 kinase domain
Drug: midostaurin
Target: Cyclin-G-associated kinase (Kinase)
Gene: GAK
UniProt: O14976 (GAK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.42
Assay: Binding constant for GAK kinase domain
Drug: midostaurin
Target: Glycogen synthase kinase-3 beta (Kinase)
Gene: GSK3B
UniProt: P49841 (GSK3B_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.75
Assay: Binding constant for full-length GSK3B
Drug: midostaurin
Target: Calcium/calmodulin-dependent protein kinase type 1D (Kinase)
Gene: CAMK1D
UniProt: Q8IU85 (KCC1D_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.17
Assay: Binding constant for CAMK1D kinase domain
Drug: midostaurin
Target: Serine/threonine-protein kinase 4 (Kinase)
Gene: STK4
UniProt: Q13043 (STK4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.77
Assay: Binding affinity to MST1
Drug: midostaurin
Target: Activated CDC42 kinase 1 (Kinase)
Gene: TNK2
UniProt: Q07912 (ACK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.92
Assay: Binding constant for TNK2 kinase domain
Drug: midostaurin
Target: Ribosomal protein S6 kinase alpha-5 (Kinase)
Gene: RPS6KA5
UniProt: O75582 (KS6A5_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.62
Assay: Binding constant for RPS6KA5(Kin.Dom.1 - C-terminal) kinase domain
Drug: midostaurin
Target: STE20-like serine/threonine-protein kinase (Kinase)
Gene: SLK
UniProt: Q9H2G2 (SLK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.66
Assay: Binding constant for SLK kinase domain
Drug: midostaurin
Target: Dual specificity protein kinase CLK4 (Kinase)
Gene: CLK4
UniProt: Q9HAZ1 (CLK4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.39
Assay: Binding constant for CLK4 kinase domain
Drug: midostaurin
Target: MAP kinase-interacting serine/threonine-protein kinase 2 (Kinase)
Gene: MKNK2
UniProt: Q9HBH9 (MKNK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.02
Assay: Binding constant for MKNK2 kinase domain
Drug: midostaurin
Target: Mitogen-activated protein kinase 9 (Kinase)
Gene: MAPK9
UniProt: P45984 (MK09_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.3
Assay: Binding constant for JNK2 kinase domain