AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: sotagliflozin
Target: Sodium/glucose cotransporter 2 (Transporter)
Gene: SLC5A2
UniProt: P31639 (SC5A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.745
Action type: INHIBITOR
Drug: sotagliflozin
Target: Sodium/glucose cotransporter 1 (Transporter)
Gene: SLC5A1
UniProt: P13866 (SC5A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.444
Action type: INHIBITOR
Drug: quizartinib
Target: Platelet-derived growth factor receptor beta (Kinase)
Gene: PDGFRB
UniProt: P09619 (PGFRB_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.8
Assay: Binding affinity to PDGFRbeta
Drug: quizartinib
Target: Tyrosine-protein kinase ABL1 (Kinase)
Gene: ABL1
UniProt: P00519 (ABL1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.5
Assay: Binding affinity to ABL1 T315I mutant
Drug: quizartinib
Target: Mast/stem cell growth factor receptor Kit (Kinase)
Gene: KIT
UniProt: P10721 (KIT_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.8
Assay: Binding affinity to cKIT
Drug: quizartinib
Target: Tyrosine-protein kinase Lck (Kinase)
Gene: LCK
UniProt: P06239 (LCK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.6
Assay: Binding constant for LCK kinase domain
Drug: quizartinib
Target: Proto-oncogene tyrosine-protein kinase receptor Ret (Kinase)
Gene: RET
UniProt: P07949 (RET_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.8
Assay: Binding affinity to RET
Drug: quizartinib
Target: Vascular endothelial growth factor receptor 1 (Kinase)
Gene: FLT1
UniProt: P17948 (VGFR1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.39
Assay: Binding affinity to FLT1
Drug: quizartinib
Target: Vascular endothelial growth factor receptor 2 (Kinase)
Gene: KDR
UniProt: P35968 (VGFR2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.06
Assay: Binding affinity to VEGFR2
Drug: quizartinib
Target: Vascular endothelial growth factor receptor 3 (Kinase)
Gene: FLT4
UniProt: P35916 (VGFR3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.39
Assay: Binding affinity to FLT4
Drug: quizartinib
Target: Macrophage colony-stimulating factor 1 receptor (Kinase)
Gene: CSF1R
UniProt: P07333 (CSF1R_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.8
Assay: Binding affinity to CSF1R
Drug: quizartinib
Target: Platelet-derived growth factor receptor alpha (Kinase)
Gene: PDGFRA
UniProt: P16234 (PGFRA_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.8
Assay: Binding affinity to PDGFRalpha
Drug: quizartinib
Target: Myosin light chain kinase, smooth muscle (Kinase)
Gene: MYLK
UniProt: Q15746 (MYLK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.39
Assay: Binding affinity to MLCK
Drug: quizartinib
Target: High affinity nerve growth factor receptor (Kinase)
Gene: NTRK1
UniProt: P04629 (NTRK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.64
Assay: Binding affinity to TRKA
Drug: quizartinib
Target: Tyrosine-protein kinase Lyn (Kinase)
Gene: LYN
UniProt: P07948 (LYN_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.24
Assay: Binding constant for LYN kinase domain
Drug: quizartinib
Target: Serine/threonine-protein kinase 10 (Kinase)
Gene: STK10
UniProt: O94804 (STK10_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.68
Assay: Binding constant for LOK kinase domain
Drug: quizartinib
Target: Ephrin type-A receptor 6 (Kinase)
Gene: EPHA6
UniProt: Q9UF33 (EPHA6_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.04
Assay: Binding constant for EPHA6 kinase domain
Drug: quizartinib
Target: TRAF2 and NCK-interacting protein kinase (Kinase)
Gene: TNIK
UniProt: Q9UKE5 (TNIK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.55
Assay: Binding constant for TNIK kinase domain
Drug: quizartinib
Target: Ephrin type-A receptor 3 (Kinase)
Gene: EPHA3
UniProt: P29320 (EPHA3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.19
Assay: Binding constant for EPHA3 kinase domain
Drug: quizartinib
Target: Tyrosine-protein kinase FRK (Kinase)
Gene: FRK
UniProt: P42685 (FRK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.75
Assay: Binding affinity to FRK
Drug: quizartinib
Target: Mitogen-activated protein kinase kinase kinase kinase 5 (Kinase)
Gene: MAP4K5
UniProt: Q9Y4K4 (M4K5_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.36
Assay: Binding affinity to MAP4K5
Drug: quizartinib
Target: Receptor-interacting serine/threonine-protein kinase 2 (Kinase)
Gene: RIPK2
UniProt: O43353 (RIPK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.57
Assay: Binding constant for RIPK2 kinase domain
Drug: quizartinib
Target: Ephrin type-A receptor 7 (Kinase)
Gene: EPHA7
UniProt: Q15375 (EPHA7_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.43
Assay: Binding constant for EPHA7 kinase domain
Drug: quizartinib
Target: STE20-like serine/threonine-protein kinase (Kinase)
Gene: SLK
UniProt: Q9H2G2 (SLK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.34
Assay: Binding constant for SLK kinase domain
Drug: quizartinib
Target: MAP kinase-interacting serine/threonine-protein kinase 2 (Kinase)
Gene: MKNK2
UniProt: Q9HBH9 (MKNK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.58
Assay: Binding affinity to MKNK2
Drug: quizartinib
Target: Epithelial discoidin domain-containing receptor 1 (Kinase)
Gene: DDR1
UniProt: Q08345 (DDR1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.09
Assay: Binding affinity to DDR1
Drug: quizartinib
Target: BDNF/NT-3 growth factors receptor (Kinase)
Gene: NTRK2
UniProt: Q16620 (NTRK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.21
Assay: Binding affinity to TRKB
Drug: quizartinib
Target: Tyrosine-protein kinase receptor Tie-1 (Kinase)
Gene: TIE1
UniProt: P35590 (TIE1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.5
Assay: Binding affinity to TIE1
Drug: quizartinib
Target: NT-3 growth factor receptor (Kinase)
Gene: NTRK3
UniProt: Q16288 (NTRK3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.26
Assay: Binding affinity to TRKC
Drug: quizartinib
Target: Discoidin domain-containing receptor 2 (Kinase)
Gene: DDR2
UniProt: Q16832 (DDR2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.16
Assay: Binding affinity to DDR2
Drug: quizartinib
Target: Mitogen-activated protein kinase kinase kinase kinase 4 (Kinase)
Gene: MAP4K4
UniProt: O95819 (M4K4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.6
Assay: Binding affinity to MAP4K4
Drug: quizartinib
Target: Muscle, skeletal receptor tyrosine-protein kinase (Kinase)
Gene: MUSK
UniProt: O15146 (MUSK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6
Assay: Binding affinity to MUSK
Drug: quizartinib
Target: Mitogen-activated protein kinase 15 (Kinase)
Gene: MAPK15
UniProt: Q8TD08 (MK15_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.57
Assay: Binding affinity to ERK8
Drug: quizartinib
Target: Receptor-interacting serine/threonine-protein kinase 1 (Kinase)
Gene: RIPK1
UniProt: Q13546 (RIPK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.05
Assay: Binding constant for RIPK1 kinase domain
Drug: quizartinib
Target: Ephrin type-B receptor 6 (Kinase)
Gene: EPHB6
UniProt: O15197 (EPHB6_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.92
Assay: Binding affinity to EPHB6
Drug: quizartinib
Target: Homeodomain-interacting protein kinase 4 (Kinase)
Gene: HIPK4
UniProt: Q8NE63 (HIPK4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.5
Assay: Binding affinity to HIPK4
Drug: quizartinib
Target: Mitogen-activated protein kinase kinase kinase 7 (Kinase)
Gene: MAP3K7
UniProt: O43318 (M3K7_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.07
Assay: Binding affinity to TAK1
Drug: quizartinib
Target: Mitogen-activated protein kinase kinase kinase 19 (Kinase)
Gene: MAP3K19
UniProt: Q56UN5 (M3K19_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.7
Assay: Binding affinity to YSK4
Drug: quizartinib
Target: Myosin light chain kinase 3 (Kinase)
Gene: MYLK3
UniProt: Q32MK0 (MYLK3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.39
Assay: Binding constant for MLCK kinase domain
Drug: quizartinib
Target: Receptor-type tyrosine-protein kinase FLT3 (Kinase)
Gene: FLT3
UniProt: P36888 (FLT3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.796
Action type: INHIBITOR
Assay: FLT3 binding affinity in biochemical assay
Drug: relebactam
Target: Beta-lactamase (Enzyme)
Gene: ampC
UniProt: Q8RL90 (Q8RL90_PSEAI)
Organism: Pseudomonas aeruginosa
Activity: IC50 = 6.33
Assay: Spectrophotometric Assay: Enzyme activities were measured in the presence of the test inhibitor in spectrophotometric assay.
Drug: relebactam
Target: Beta-lactamase (Enzyme)
Gene: blaCTX-M-15
UniProt: Q2PUH3 (Q2PUH3_KLEPN)
Organism: Klebsiella pneumoniae
Activity: IC50 = 6.4
Action type: INHIBITOR
Drug: relebactam
Target: Beta-lactamase (Enzyme)
Gene: L2camp
UniProt: Q9X5A7 (Q9X5A7_STEMA)
Organism: Stenotrophomonas maltophilia
Activity: IC50 = 6.33
Action type: INHIBITOR
Drug: relebactam
Target: Beta-lactamase (Enzyme)
Gene: KPC-2
UniProt: Q93LQ9 (Q93LQ9_KLEPN)
Organism: Klebsiella pneumoniae
Activity: IC50 = 6.64
Action type: INHIBITOR
Drug: relebactam
Target: Beta-lactamase (Enzyme)
Gene: bla
UniProt: Q93DC4 (Q93DC4_KLEPN)
Organism: Klebsiella pneumoniae
Activity: IC50 = 6.59
Action type: INHIBITOR
Drug: relebactam
Target: Beta-lactamase (Enzyme)
Gene: blaKPC-4
UniProt: B1PL86 (B1PL86_KLEPN)
Organism: Klebsiella pneumoniae
Activity: IC50 = 6.04
Action type: INHIBITOR
Drug: pexidartinib
Target: Tyrosine-protein kinase Lck (Kinase)
Gene: LCK
UniProt: P06239 (LCK_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.07
Action type: INHIBITOR
Drug: pexidartinib
Target: Vascular endothelial growth factor receptor 1 (Kinase)
Gene: FLT1
UniProt: P17948 (VGFR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.06
Action type: INHIBITOR
Drug: pexidartinib
Target: Vascular endothelial growth factor receptor 2 (Kinase)
Gene: KDR
UniProt: P35968 (VGFR2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.36
Action type: INHIBITOR
Drug: pexidartinib
Target: NT-3 growth factor receptor (Kinase)
Gene: NTRK3
UniProt: Q16288 (NTRK3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.05
Action type: INHIBITOR
Drug: pexidartinib
Target: Cyclin-dependent kinase 19 (Kinase)
Gene: CDK19
UniProt: Q9BWU1 (CDK19_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.85
Action type: INHIBITOR
Drug: pexidartinib
Target: Mast/stem cell growth factor receptor Kit (Kinase)
Gene: KIT
UniProt: P10721 (KIT_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.56
Action type: INHIBITOR
Drug: pexidartinib
Target: Receptor-type tyrosine-protein kinase FLT3 (Kinase)
Gene: FLT3
UniProt: P36888 (FLT3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.79
Action type: INHIBITOR
Drug: pexidartinib
Target: Macrophage colony-stimulating factor 1 receptor (Kinase)
Gene: CSF1R
UniProt: P07333 (CSF1R_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.88
Action type: INHIBITOR
Drug: entrectinib
Target: Tyrosine-protein kinase JAK3 (Kinase)
Gene: JAK3
UniProt: P52333 (JAK3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.46
Assay: Inhibition of JAK3 (unknown origin) in presence of gamma33-ATP
Drug: entrectinib
Target: Receptor-type tyrosine-protein kinase FLT3 (Kinase)
Gene: FLT3
UniProt: P36888 (FLT3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.79
Assay: Inhibition of FLT3 (unknown origin) in presence of gamma33-ATP
Drug: entrectinib
Target: Proto-oncogene tyrosine-protein kinase receptor Ret (Kinase)
Gene: RET
UniProt: P07949 (RET_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.41
Assay: Inhibition of RET (unknown origin) in presence of gamma33-ATP
Drug: entrectinib
Target: Insulin-like growth factor 1 receptor (Kinase)
Gene: IGF1R
UniProt: P08069 (IGF1R_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.91
Assay: Inhibition of IGF1R (unknown origin) in presence of gamma33-ATP
Drug: entrectinib
Target: Insulin receptor (Kinase)
Gene: INSR
UniProt: P06213 (INSR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.68
Assay: Inhibition of IR (unknown origin) in presence of gamma33-ATP
Drug: entrectinib
Target: Focal adhesion kinase 1 (Kinase)
Gene: PTK2
UniProt: Q05397 (FAK1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.85
Assay: Inhibition of FAK (unknown origin) in presence of gamma33-ATP
Drug: entrectinib
Target: Tyrosine-protein kinase JAK1 (Kinase)
Gene: JAK1
UniProt: P23458 (JAK1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.95
Assay: Inhibition of JAK1 (unknown origin) in presence of gamma33-ATP
Drug: entrectinib
Target: Aurora kinase A (Kinase)
Gene: AURKA
UniProt: O14965 (AURKA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.67
Assay: Inhibition of AUR2 (unknown origin) in presence of gamma33-ATP
Drug: entrectinib
Target: Protein-tyrosine kinase 6 (Kinase)
Gene: PTK6
UniProt: Q13882 (PTK6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.71
Assay: Inhibition of BRK (unknown origin) in presence of gamma33-ATP
Drug: entrectinib
Target: Aurora kinase B (Kinase)
Gene: AURKB
UniProt: Q96GD4 (AURKB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.47
Assay: Biochemical Assay: The inhibitory activity of putative kinase inhibitors and the potency of selected compounds were determined using a trans-phosphorylation assay.A specific substrate was incubated with the kinase in appropriate buffer conditions in the presence of ATP traced with .sup.33P-.gamma.-ATP (gamma phosphate-labeled, Redivue.TM. Code Number AH9968, 1000-3000 Ci/mmole, Amersham Biosciences Piscataway, N.J., USA), optimal cofactors and test compound.At the end of the phosphorylation reaction, more than 98% cold and radioactive ATP were captured by an excess of Dowex ion exchange resin. The resin was allowed to settle to the bottom of reaction wells by gravity. Supernatant, containing substrate peptide, was subsequently withdrawn and transferred into a counting plate, and radioactivity (corresponding to phosphate incorporated into peptide) was evaluated by .beta.-counting. Assay Conditions:The kinase assay was run with a final enzyme concentration of 6 nM, in the prese
Drug: entrectinib
Target: Tyrosine-protein kinase JAK2 (Kinase)
Gene: JAK2
UniProt: O60674 (JAK2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.4
Action type: INHIBITOR
Drug: entrectinib
Target: Activated CDC42 kinase 1 (Kinase)
Gene: TNK2
UniProt: Q07912 (ACK1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.15
Action type: INHIBITOR
Drug: entrectinib
Target: High affinity nerve growth factor receptor (Kinase)
Gene: NTRK1
UniProt: P04629 (NTRK1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9
Action type: INHIBITOR
Drug: entrectinib
Target: ALK tyrosine kinase receptor (Kinase)
Gene: ALK
UniProt: Q9UM73 (ALK_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.92
Action type: INHIBITOR
Drug: entrectinib
Target: BDNF/NT-3 growth factors receptor (Kinase)
Gene: NTRK2
UniProt: Q16620 (NTRK2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.52
Action type: INHIBITOR
Drug: entrectinib
Target: NT-3 growth factor receptor (Kinase)
Gene: NTRK3
UniProt: Q16288 (NTRK3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.3
Action type: INHIBITOR
Drug: entrectinib
Target: Proto-oncogene tyrosine-protein kinase ROS (Kinase)
Gene: ROS1
UniProt: P08922 (ROS1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.15
Action type: INHIBITOR
Drug: upadacitinib
Target: Non-receptor tyrosine-protein kinase TYK2 (Kinase)
Gene: TYK2
UniProt: P29597 (TYK2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.33
Action type: INHIBITOR
Drug: upadacitinib
Target: Tyrosine-protein kinase JAK3 (Kinase)
Gene: JAK3
UniProt: P52333 (JAK3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.63
Action type: INHIBITOR
Drug: upadacitinib
Target: Tyrosine-protein kinase JAK1 (Kinase)
Gene: JAK1
UniProt: P23458 (JAK1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.33
Action type: INHIBITOR
Drug: upadacitinib
Target: Tyrosine-protein kinase JAK2 (Kinase)
Gene: JAK2
UniProt: O60674 (JAK2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.92
Action type: INHIBITOR
Drug: fedratinib
Target: Platelet-derived growth factor receptor beta (Kinase)
Gene: PDGFRB
UniProt: P09619 (PGFRB_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.35
Assay: Binding constant for PDGFRB kinase domain
Drug: fedratinib
Target: Tyrosine-protein kinase ABL1 (Kinase)
Gene: ABL1
UniProt: P00519 (ABL1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.4
Assay: Binding constant for ABL1(E255K)-phosphorylated kinase domain
Drug: fedratinib
Target: Mast/stem cell growth factor receptor Kit (Kinase)
Gene: KIT
UniProt: P10721 (KIT_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.34
Assay: Binding constant for KIT(A829P) kinase domain
Drug: fedratinib
Target: Epidermal growth factor receptor (Kinase)
Gene: EGFR
UniProt: P00533 (EGFR_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.24
Assay: Binding constant for EGFR(T790M) kinase domain
Drug: fedratinib
Target: Proto-oncogene tyrosine-protein kinase Src (Kinase)
Gene: SRC
UniProt: P12931 (SRC_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.12
Assay: Binding constant for SRC kinase domain
Drug: fedratinib
Target: Tyrosine-protein kinase Lck (Kinase)
Gene: LCK
UniProt: P06239 (LCK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.14
Assay: Binding constant for LCK kinase domain
Drug: fedratinib
Target: Tyrosine-protein kinase Yes (Kinase)
Gene: YES1
UniProt: P07947 (YES_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.92
Assay: Binding constant for YES kinase domain
Drug: fedratinib
Target: Tyrosine-protein kinase Fyn (Kinase)
Gene: FYN
UniProt: P06241 (FYN_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.42
Assay: Binding constant for FYN kinase domain
Drug: fedratinib
Target: Ephrin type-A receptor 2 (Kinase)
Gene: EPHA2
UniProt: P29317 (EPHA2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.36
Assay: Binding constant for EPHA2 kinase domain
Drug: fedratinib
Target: Serine/threonine-protein kinase B-raf (Kinase)
Gene: BRAF
UniProt: P15056 (BRAF_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.03
Assay: Binding constant for BRAF(V600E) kinase domain
Drug: fedratinib
Target: Proto-oncogene tyrosine-protein kinase receptor Ret (Kinase)
Gene: RET
UniProt: P07949 (RET_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.32
Assay: Inhibition of RET (unknown origin)
Drug: fedratinib
Target: Vascular endothelial growth factor receptor 1 (Kinase)
Gene: FLT1
UniProt: P17948 (VGFR1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.37
Assay: Binding constant for FLT1 kinase domain
Drug: fedratinib
Target: Vascular endothelial growth factor receptor 2 (Kinase)
Gene: KDR
UniProt: P35968 (VGFR2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.28
Assay: Binding constant for VEGFR2 kinase domain
Drug: fedratinib
Target: Vascular endothelial growth factor receptor 3 (Kinase)
Gene: FLT4
UniProt: P35916 (VGFR3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.7
Assay: Binding constant for FLT4 kinase domain
Drug: fedratinib
Target: Macrophage colony-stimulating factor 1 receptor (Kinase)
Gene: CSF1R
UniProt: P07333 (CSF1R_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.21
Assay: Binding constant for CSF1R kinase domain
Drug: fedratinib
Target: Platelet-derived growth factor receptor alpha (Kinase)
Gene: PDGFRA
UniProt: P16234 (PGFRA_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.57
Assay: Binding constant for PDGFRA kinase domain
Drug: fedratinib
Target: Ribosomal protein S6 kinase alpha-3 (Kinase)
Gene: RPS6KA3
UniProt: P51812 (KS6A3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.09
Assay: Binding constant for RSK2(Kin.Dom.1-N-terminal) kinase domain
Drug: fedratinib
Target: Phosphorylase b kinase gamma catalytic chain, liver/testis isoform (Kinase)
Gene: PHKG2
UniProt: P15735 (PHKG2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.8
Assay: Binding constant for PHKG2 kinase domain
Drug: fedratinib
Target: Insulin-like growth factor 1 receptor (Kinase)
Gene: IGF1R
UniProt: P08069 (IGF1R_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.66
Assay: Binding constant for IGF1R kinase domain
Drug: fedratinib
Target: Myosin light chain kinase, smooth muscle (Kinase)
Gene: MYLK
UniProt: Q15746 (MYLK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.28
Assay: Binding constant for MYLK kinase domain
Drug: fedratinib
Target: Insulin receptor (Kinase)
Gene: INSR
UniProt: P06213 (INSR_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.07
Assay: Binding constant for INSR kinase domain
Drug: fedratinib
Target: Death-associated protein kinase 3 (Kinase)
Gene: DAPK3
UniProt: O43293 (DAPK3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.92
Assay: Binding constant for DAPK3 kinase domain
Drug: fedratinib
Target: Calcium/calmodulin-dependent protein kinase type 1 (Kinase)
Gene: CAMK1
UniProt: Q14012 (KCC1A_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.8
Assay: Binding constant for CAMK1 kinase domain
Drug: fedratinib
Target: Mitogen-activated protein kinase 8 (Kinase)
Gene: MAPK8
UniProt: P45983 (MK08_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.58
Assay: Binding constant for JNK1 kinase domain
Drug: fedratinib
Target: Fibroblast growth factor receptor 3 (Kinase)
Gene: FGFR3
UniProt: P22607 (FGFR3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.44
Assay: Binding constant for FGFR3 kinase domain
Drug: fedratinib
Target: Rho-associated protein kinase 1 (Kinase)
Gene: ROCK1
UniProt: Q13464 (ROCK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.68
Assay: Binding constant for ROCK1 kinase domain
Drug: fedratinib
Target: Focal adhesion kinase 1 (Kinase)
Gene: PTK2
UniProt: Q05397 (FAK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.38
Assay: Binding constant for FAK kinase domain
Drug: fedratinib
Target: Tyrosine-protein kinase HCK (Kinase)
Gene: HCK
UniProt: P08631 (HCK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.68
Assay: Binding constant for HCK kinase domain
Drug: fedratinib
Target: Serine/threonine-protein kinase PLK1 (Kinase)
Gene: PLK1
UniProt: P53350 (PLK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.55
Assay: Binding constant for PLK1 kinase domain
Drug: fedratinib
Target: Receptor tyrosine-protein kinase erbB-4 (Kinase)
Gene: ERBB4
UniProt: Q15303 (ERBB4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.7
Assay: Binding constant for ERBB4 kinase domain
Drug: fedratinib
Target: Mitogen-activated protein kinase 10 (Kinase)
Gene: MAPK10
UniProt: P53779 (MK10_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.7
Assay: Binding constant for JNK3 kinase domain
Drug: fedratinib
Target: Death-associated protein kinase 2 (Kinase)
Gene: DAPK2
UniProt: Q9UIK4 (DAPK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.54
Assay: Binding constant for DAPK2 kinase domain
Drug: fedratinib
Target: High affinity nerve growth factor receptor (Kinase)
Gene: NTRK1
UniProt: P04629 (NTRK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.08
Assay: Binding constant for TRKA kinase domain
Drug: fedratinib
Target: Rho-associated protein kinase 2 (Kinase)
Gene: ROCK2
UniProt: O75116 (ROCK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.66
Assay: Binding constant for ROCK2 kinase domain
Drug: fedratinib
Target: Tyrosine-protein kinase SYK (Kinase)
Gene: SYK
UniProt: P43405 (KSYK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.57
Assay: Binding constant for SYK kinase domain
Drug: fedratinib
Target: Calcium/calmodulin-dependent protein kinase type II subunit delta (Kinase)
Gene: CAMK2D
UniProt: Q13557 (KCC2D_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.23
Assay: Binding constant for CAMK2D kinase domain
Drug: fedratinib
Target: Myosin light chain kinase 2, skeletal/cardiac muscle (Kinase)
Gene: MYLK2
UniProt: Q9H1R3 (MYLK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.52
Assay: Binding constant for MYLK2 kinase domain
Drug: fedratinib
Target: Tyrosine-protein kinase CSK (Kinase)
Gene: CSK
UniProt: P41240 (CSK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.23
Assay: Binding constant for CSK kinase domain
Drug: fedratinib
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: fedratinib
Target: Ephrin type-A receptor 8 (Kinase)
Gene: EPHA8
UniProt: P29322 (EPHA8_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.11
Assay: Binding constant for EPHA8 kinase domain
Drug: fedratinib
Target: Calcium/calmodulin-dependent protein kinase type II subunit gamma (Kinase)
Gene: CAMK2G
UniProt: Q13555 (KCC2G_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.27
Assay: Binding constant for CAMK2G kinase domain
Drug: fedratinib
Target: AP2-associated protein kinase 1 (Kinase)
Gene: AAK1
UniProt: Q2M2I8 (AAK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.46
Assay: Binding constant for AAK1 kinase domain
Drug: fedratinib
Target: Serine/threonine-protein kinase MARK2 (Kinase)
Gene: MARK2
UniProt: Q7KZI7 (MARK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.51
Assay: Binding constant for MARK2 kinase domain