AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: nifedipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: CACNA1C
UniProt: O35505 (CAC1C_CAVPO)
Organism: Cavia porcellus
Activity: IC50 = 8.59
Assay: Antagonist activity at Cavia porcellus albino (guinea pig) calcium channel assessed as inhibition of KCl-induced ileal longitudinal smooth muscle contraction
Drug: nifedipine
Target: Sodium channel alpha subunits; brain (Types I, II, III) (Ion channel)
Gene: SCN1A|SCN2A|SCN3A
UniProt: P35498|Q99250|Q9NY46 (SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.43
Assay: Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex
Drug: nifedipine
Target: Voltage-gated L-type calcium channel (Ion channel)
Gene: Cacna1c|Cacna1d|Cacna1s
UniProt: P22002|P27732|Q02485 (CAC1C_RAT|CAC1D_RAT|CAC1S_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.33
Assay: Inhibition of [3H]nitrendipine binding to L-type calcium channel from rat brain cortex homogenate
Drug: nifedipine
Target: Indoleamine 2,3-dioxygenase 1 (Enzyme)
Gene: Ido1
UniProt: P28776 (I23O1_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4.34
Assay: Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
Drug: nifedipine
Target: Bile salt export pump (Transporter)
Gene: Abcb11
UniProt: O70127 (ABCBB_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.34
Drug: nifedipine
Target: Potassium voltage-gated channel subfamily A member 7 (Ion channel)
Gene: Kcna7
UniProt: Q17ST2 (KCNA7_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4.9
Action type: BLOCKER
Drug: nifedipine
Target: Potassium voltage-gated channel subfamily A member 1 (Ion channel)
Gene: Kcna1
UniProt: P16388 (KCNA1_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4
Action type: BLOCKER
Drug: nifedipine
Target: Potassium voltage-gated channel subfamily A member 2 (Ion channel)
Gene: Kcna2
UniProt: P63142 (KCNA2_RAT)
Organism: Rattus norvegicus
Activity: Kd = 4.7
Action type: BLOCKER
Drug: nifedipine
Target: Potassium channel subfamily K member 2 (Ion channel)
Gene: Kcnk2
UniProt: Q8HY88 (Q8HY88_BOVIN)
Organism: Bos taurus
Activity: IC50 = 5.09
Assay: Activation of bovine TREK1 expressed in AZT cells assessed as reduction in channel currents
Drug: nifedipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: CACNA1C
UniProt: Q13936 (CAC1C_HUMAN)
Organism: Homo sapiens
Activity: Kd = 9.4
Action type: BLOCKER
Assay: Displacement of [3H]nitrendipine from dihydropyridine receptor of guinea pig myocardial membranes
Drug: nifekalant
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5
Assay: Inhibitory concentration against IKr potassium channel
Drug: nifekalant
Target: Solute carrier family 22 member 2 (Transporter)
Gene: SLC22A2
UniProt: O15244 (S22A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.99
Assay: Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Drug: nifekalant
Target: Multidrug and toxin extrusion protein 1 (Transporter)
Gene: SLC47A1
UniProt: Q96FL8 (S47A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.19
Assay: Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis
Drug: nifekalant
Target: Multidrug and toxin extrusion protein 2 (Transporter)
Gene: SLC47A2
UniProt: Q86VL8 (S47A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.57
Assay: Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Drug: niflumic acid
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.037
Assay: DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid)
Drug: niflumic acid
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.973
Assay: DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid)
Drug: niflumic acid
Target: Dihydroorotate dehydrogenase (quinone), mitochondrial (Enzyme)
Gene: DHODH
UniProt: Q02127 (PYRD_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.77
Assay: Inhibition of human recombinant DHODH
Drug: niflumic acid
Target: Transthyretin (Secreted)
Gene: TTR
UniProt: P02766 (TTHY_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.59
Drug: niflumic acid
Target: Chloride channel protein ClC-Ka (Ion channel)
Gene: CLCNKA
UniProt: P51800 (CLCKA_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5
Action type: ACTIVATOR
Drug: niflumic acid
Target: Potassium channel subfamily T member 2 (Ion channel)
Gene: KCNT2
UniProt: Q6UVM3 (KCNT2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.68
Action type: ACTIVATOR
Drug: niflumic acid
Target: G-protein coupled receptor 35 (GPCR)
Gene: GPR35
UniProt: Q9HC97 (GPR35_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.44
Assay: Displacement of [3H]PSB-13253 from human recombinant GPR35 exprssed in CHO cells by liquid scintillation counting analysis
Drug: niflumic acid
Target: Chloride channel protein ClC-Kb (Ion channel)
Gene: CLCNKB
UniProt: P51801 (CLCKB_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5
Action type: ACTIVATOR
Drug: niflumic acid
Target: Transcriptional enhancer factor TEF-3 (Transcription factor)
Gene: TEAD4
UniProt: Q15561 (TEAD4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.55
Assay: Binding affinity to human His-tagged TEAD4 YBD (217 to 434 residues) expressed in Escherichia coli BL21(DE3) after 30 mins by ITC assay
Drug: nifuroxazide
Target: Signal transducer and activator of transcription 3 (Transcription factor)
Gene: STAT3
UniProt: P40763 (STAT3_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.52
Assay: Inhibition of STAT3 expressed in human U3A cells after 1 hr by luciferase reporter gene assay
Drug: nilotinib
Target: Carbonic anhydrase 2 (Enzyme)
Gene: CA2
UniProt: P00918 (CAH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.39
Assay: Inhibition of human carbonic anhydrase 2 by stopped flow CO2 hydration assay
Drug: nilotinib
Target: Carbonic anhydrase 1 (Enzyme)
Gene: CA1
UniProt: P00915 (CAH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.53
Assay: Inhibition of human carbonic anhydrase 1 by stopped flow CO2 hydration assay
Drug: nilotinib
Target: Carbonic anhydrase 4 (Enzyme)
Gene: CA4
UniProt: P22748 (CAH4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.35
Assay: Inhibition of human carbonic anhydrase 4 by stopped flow CO2 hydration assay
Drug: nilotinib
Target: Ribosyldihydronicotinamide dehydrogenase [quinone] (Enzyme)
Gene: NQO2
UniProt: P16083 (NQO2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.42
Assay: Inhibition of full length human His6/GST-tagged NQO2 expressed in Escherichia coli Tuner(DE3)pLysS using menadione as substrate and CCHP as co-substrate preincubated with enzyme followed by substrate addition by MTT dye based continuous spectrophotometric assay
Drug: nilotinib
Target: Carbonic anhydrase 9 (Enzyme)
Gene: CA9
UniProt: Q16790 (CAH9_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.38
Assay: Inhibition of human carbonic anhydrase 9 by stopped flow CO2 hydration assay
Drug: nilotinib
Target: Carbonic anhydrase 12 (Enzyme)
Gene: CA12
UniProt: O43570 (CAH12_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.52
Assay: Inhibition of human carbonic anhydrase 12 by stopped flow CO2 hydration assay
Drug: nilotinib
Target: Platelet-derived growth factor receptor beta (Kinase)
Gene: PDGFRB
UniProt: P09619 (PGFRB_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.8
Assay: Binding affinity to human PDGFRbeata
Drug: nilotinib
Target: Tyrosine-protein kinase ABL1 (Kinase)
Gene: ABL1
UniProt: P00519 (ABL1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.44
Action type: INHIBITOR
Assay: Binding affinity to human ABL1
Drug: nilotinib
Target: Mast/stem cell growth factor receptor Kit (Kinase)
Gene: KIT
UniProt: P10721 (KIT_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.77
Assay: Binding affinity to human c-Kit
Drug: nilotinib
Target: Carbonic anhydrase 5A, mitochondrial (Enzyme)
Gene: CA5A
UniProt: P35218 (CAH5A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.26
Assay: Inhibition of human carbonic anhydrase 5A by stopped flow CO2 hydration assay
Drug: nilotinib
Target: Carbonic anhydrase 5B, mitochondrial (Enzyme)
Gene: CA5B
UniProt: Q9Y2D0 (CAH5B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.83
Assay: Inhibition of human carbonic anhydrase 5B by stopped flow CO2 hydration assay
Drug: nilotinib
Target: Carbonic anhydrase 7 (Enzyme)
Gene: CA7
UniProt: P43166 (CAH7_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7
Assay: Inhibition of human carbonic anhydrase 7 by stopped flow CO2 hydration assay
Drug: nilotinib
Target: Proto-oncogene tyrosine-protein kinase Src (Kinase)
Gene: SRC
UniProt: P12931 (SRC_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.72
Assay: Binding constant for SRC kinase domain
Drug: nilotinib
Target: Tyrosine-protein kinase Lck (Kinase)
Gene: LCK
UniProt: P06239 (LCK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.33
Assay: Binding constant for LCK kinase domain
Drug: nilotinib
Target: Tyrosine-protein kinase Yes (Kinase)
Gene: YES1
UniProt: P07947 (YES_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.96
Assay: Binding constant for YES kinase domain
Drug: nilotinib
Target: Tyrosine-protein kinase Fyn (Kinase)
Gene: FYN
UniProt: P06241 (FYN_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.8
Assay: Binding constant for FYN kinase domain
Drug: nilotinib
Target: Ephrin type-A receptor 2 (Kinase)
Gene: EPHA2
UniProt: P29317 (EPHA2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.64
Assay: Binding constant for EPHA2 kinase domain
Drug: nilotinib
Target: RAF proto-oncogene serine/threonine-protein kinase (Kinase)
Gene: RAF1
UniProt: P04049 (RAF1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.41
Assay: Binding constant for RAF1 kinase domain
Drug: nilotinib
Target: Serine/threonine-protein kinase B-raf (Kinase)
Gene: BRAF
UniProt: P15056 (BRAF_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.24
Assay: Binding constant for BRAF(V600E) kinase domain
Drug: nilotinib
Target: Receptor-type tyrosine-protein kinase FLT3 (Kinase)
Gene: FLT3
UniProt: P36888 (FLT3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.4
Assay: Binding affinity to human FLT3
Drug: nilotinib
Target: Proto-oncogene tyrosine-protein kinase receptor Ret (Kinase)
Gene: RET
UniProt: P07949 (RET_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.06
Assay: Binding constant for RET kinase domain
Drug: nilotinib
Target: Macrophage colony-stimulating factor 1 receptor (Kinase)
Gene: CSF1R
UniProt: P07333 (CSF1R_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.35
Assay: Binding constant for CSF1R kinase domain
Drug: nilotinib
Target: Platelet-derived growth factor receptor alpha (Kinase)
Gene: PDGFRA
UniProt: P16234 (PGFRA_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.13
Assay: Binding affinity to human PDGFRalpha
Drug: nilotinib
Target: Insulin receptor (Kinase)
Gene: INSR
UniProt: P06213 (INSR_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.387
Drug: nilotinib
Target: Mitogen-activated protein kinase 8 (Kinase)
Gene: MAPK8
UniProt: P45983 (MK08_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.35
Assay: Binding constant for JNK1 kinase domain
Drug: nilotinib
Target: Tyrosine-protein kinase HCK (Kinase)
Gene: HCK
UniProt: P08631 (HCK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.41
Assay: Binding constant for HCK kinase domain
Drug: nilotinib
Target: Carbonic anhydrase 3 (Enzyme)
Gene: CA3
UniProt: P07451 (CAH3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.35
Assay: Inhibition of human carbonic anhydrase 3 by stopped flow CO2 hydration assay
Drug: nilotinib
Target: Carbonic anhydrase 6 (Enzyme)
Gene: CA6
UniProt: P23280 (CAH6_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.34
Assay: Inhibition of human carbonic anhydrase 6 by stopped flow CO2 hydration assay
Drug: nilotinib
Target: Mitogen-activated protein kinase 10 (Kinase)
Gene: MAPK10
UniProt: P53779 (MK10_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.7
Assay: Binding constant for JNK3 kinase domain
Drug: nilotinib
Target: Tyrosine-protein kinase JAK2 (Kinase)
Gene: JAK2
UniProt: O60674 (JAK2_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.069
Drug: nilotinib
Target: Tyrosine-protein kinase CSK (Kinase)
Gene: CSK
UniProt: P41240 (CSK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.62
Assay: Binding constant for CSK kinase domain
Drug: nilotinib
Target: Angiopoietin-1 receptor (Kinase)
Gene: TEK
UniProt: Q02763 (TIE2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6
Assay: Binding constant for TIE2 kinase domain
Drug: nilotinib
Target: Ephrin type-A receptor 8 (Kinase)
Gene: EPHA8
UniProt: P29322 (EPHA8_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.43
Assay: Binding constant for EPHA8 kinase domain
Drug: nilotinib
Target: Tyrosine-protein kinase Lyn (Kinase)
Gene: LYN
UniProt: P07948 (LYN_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7
Assay: Binding constant for LYN kinase domain
Drug: nilotinib
Target: Cytoplasmic tyrosine-protein kinase BMX (Kinase)
Gene: BMX
UniProt: P51813 (BMX_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.318
Drug: nilotinib
Target: Carbonic anhydrase 14 (Enzyme)
Gene: CA14
UniProt: Q9ULX7 (CAH14_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.65
Assay: Inhibition of human carbonic anhydrase 14 by stopped flow CO2 hydration assay
Drug: nilotinib
Target: Fibroblast growth factor receptor 1 (Kinase)
Gene: FGFR1
UniProt: P11362 (FGFR1_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.096
Drug: nilotinib
Target: Serine/threonine-protein kinase 10 (Kinase)
Gene: STK10
UniProt: O94804 (STK10_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.17
Assay: Binding constant for LOK kinase domain
Drug: nilotinib
Target: Abelson tyrosine-protein kinase 2 (Kinase)
Gene: ABL2
UniProt: P42684 (ABL2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.59
Assay: Binding constant for ABL2 kinase domain
Drug: nilotinib
Target: Mitogen-activated protein kinase 11 (Kinase)
Gene: MAPK11
UniProt: Q15759 (MK11_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.44
Assay: Binding constant for p38-beta kinase domain
Drug: nilotinib
Target: Ephrin type-A receptor 5 (Kinase)
Gene: EPHA5
UniProt: P54756 (EPHA5_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.72
Assay: Binding constant for EPHA5 kinase domain
Drug: nilotinib
Target: Ephrin type-A receptor 4 (Kinase)
Gene: EPHA4
UniProt: P54764 (EPHA4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.48
Assay: Binding constant for EPHA4 kinase domain
Drug: nilotinib
Target: Fibroblast growth factor receptor 2 (Kinase)
Gene: FGFR2
UniProt: P21802 (FGFR2_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.141
Drug: nilotinib
Target: Ephrin type-A receptor 6 (Kinase)
Gene: EPHA6
UniProt: Q9UF33 (EPHA6_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.19
Assay: Binding constant for EPHA6 kinase domain
Drug: nilotinib
Target: Tyrosine-protein kinase Fgr (Kinase)
Gene: FGR
UniProt: P09769 (FGR_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.49
Assay: Binding constant for FGR kinase domain
Drug: nilotinib
Target: Ephrin type-A receptor 3 (Kinase)
Gene: EPHA3
UniProt: P29320 (EPHA3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.96
Assay: Binding constant for EPHA3 kinase domain
Drug: nilotinib
Target: Mitogen-activated protein kinase 14 (Kinase)
Gene: MAPK14
UniProt: Q16539 (MK14_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.34
Assay: Binding constant for p38-alpha kinase domain
Drug: nilotinib
Target: Tyrosine-protein kinase FRK (Kinase)
Gene: FRK
UniProt: P42685 (FRK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.07
Assay: Binding constant for FRK kinase domain
Drug: nilotinib
Target: Dual specificity protein kinase CLK1 (Kinase)
Gene: CLK1
UniProt: P49759 (CLK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.68
Assay: Binding constant for CLK1 kinase domain
Drug: nilotinib
Target: Ephrin type-B receptor 1 (Kinase)
Gene: EPHB1
UniProt: P54762 (EPHB1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.89
Assay: Binding constant for EPHB1 kinase domain
Drug: nilotinib
Target: Dual specificity protein kinase CLK4 (Kinase)
Gene: CLK4
UniProt: Q9HAZ1 (CLK4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.15
Assay: Binding constant for CLK4 kinase domain
Drug: nilotinib
Target: Mitogen-activated protein kinase 9 (Kinase)
Gene: MAPK9
UniProt: P45984 (MK09_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.24
Assay: Binding constant for JNK2 kinase domain
Drug: nilotinib
Target: Epithelial discoidin domain-containing receptor 1 (Kinase)
Gene: DDR1
UniProt: Q08345 (DDR1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.96
Assay: Binding constant for DDR1 kinase domain
Drug: nilotinib
Target: Ephrin type-B receptor 4 (Kinase)
Gene: EPHB4
UniProt: P54760 (EPHB4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.14
Assay: Binding constant for EPHB4 kinase domain
Drug: nilotinib
Target: Carbonic anhydrase 13 (Enzyme)
Gene: Ca13
UniProt: Q9D6N1 (CAH13_MOUSE)
Organism: Mus musculus
Activity: Ki = 5.33
Assay: Inhibition of mouse carbonic anhydrase 13 by stopped flow CO2 hydration assay
Drug: nilotinib
Target: Carbonic anhydrase 15 (Enzyme)
Gene: Ca15
UniProt: Q99N23 (CAH15_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.1
Assay: Inhibition of mouse carbonic anhydrase 15 by stopped flow CO2 hydration assay
Drug: nilotinib
Target: BDNF/NT-3 growth factors receptor (Kinase)
Gene: NTRK2
UniProt: Q16620 (NTRK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.31
Assay: Binding constant for TRKB kinase domain
Drug: nilotinib
Target: Ephrin type-B receptor 2 (Kinase)
Gene: EPHB2
UniProt: P29323 (EPHB2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.19
Assay: Binding constant for EPHB2 kinase domain
Drug: nilotinib
Target: Mitogen-activated protein kinase kinase kinase MLT (Kinase)
Gene: ZAK
UniProt: Q9NYL2 (MLTK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.96
Assay: Binding constant for ZAK kinase domain
Drug: nilotinib
Target: Tyrosine-protein kinase receptor Tie-1 (Kinase)
Gene: TIE1
UniProt: P35590 (TIE1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6
Assay: Binding constant for TIE1 kinase domain
Drug: nilotinib
Target: NT-3 growth factor receptor (Kinase)
Gene: NTRK3
UniProt: Q16288 (NTRK3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.22
Assay: Binding constant for TRKC kinase domain
Drug: nilotinib
Target: Serine/threonine-protein kinase TNNI3K (Kinase)
Gene: TNNI3K
UniProt: Q59H18 (TNI3K_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.44
Assay: Binding constant for TNNI3K kinase domain
Drug: nilotinib
Target: Discoidin domain-containing receptor 2 (Kinase)
Gene: DDR2
UniProt: Q16832 (DDR2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.22
Assay: Binding affinity to wild type DDR2 (unknown origin) by FLiK assay
Drug: nilotinib
Target: Mitogen-activated protein kinase kinase kinase kinase 1 (Kinase)
Gene: MAP4K1
UniProt: Q92918 (M4K1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.05
Assay: Binding constant for HPK1 kinase domain
Drug: nilotinib
Target: Tyrosine-protein kinase Blk (Kinase)
Gene: BLK
UniProt: P51451 (BLK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.3
Assay: Binding constant for BLK kinase domain
Drug: nilotinib
Target: Serine/threonine-protein kinase MRCK beta (Kinase)
Gene: CDC42BPB
UniProt: Q9Y5S2 (MRCKB_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.04
Assay: Binding constant for MRCKB kinase domain
Drug: nilotinib
Target: Ephrin type-A receptor 1 (Kinase)
Gene: EPHA1
UniProt: P21709 (EPHA1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.23
Assay: Binding constant for EPHA1 kinase domain
Drug: nilotinib
Target: Ephrin type-B receptor 3 (Kinase)
Gene: EPHB3
UniProt: P54753 (EPHB3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6
Assay: Binding constant for EPHB3 kinase domain
Drug: nilotinib
Target: Ephrin type-B receptor 6 (Kinase)
Gene: EPHB6
UniProt: O15197 (EPHB6_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.3
Assay: Binding constant for EPHB6 kinase domain
Drug: nilotinib
Target: Serine/threonine-protein kinase TAO1 (Kinase)
Gene: TAOK1
UniProt: Q7L7X3 (TAOK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.33
Assay: Binding constant for TAOK1 kinase domain
Drug: nilotinib
Target: Serine/threonine-protein kinase TAO3 (Kinase)
Gene: TAOK3
UniProt: Q9H2K8 (TAOK3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.77
Assay: Binding constant for TAOK3 kinase domain
Drug: nilotinib
Target: Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma (Kinase)
Gene: PIP4K2C
UniProt: Q8TBX8 (PI42C_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.06
Assay: Binding constant for PIP5K2C kinase domain
Drug: nilotinib
Target: Dual specificity mitogen-activated protein kinase kinase 5 (Kinase)
Gene: MAP2K5
UniProt: Q13163 (MP2K5_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.72
Assay: Binding constant for MEK5 kinase domain
Drug: nilotinib
Target: Calcium-dependent protein kinase 1 (Kinase)
Gene: CPK1
UniProt: P62344 (CDPK1_PLAF7)
Organism: Plasmodium falciparum
Activity: Kd = 6.1
Assay: Binding constant for PFCDPK1(P.falciparum) kinase domain
Drug: nilotinib
Target: Bcr/Abl fusion protein (Kinase)
Gene: ABL1|BCR
UniProt: P00519|P11274 (ABL1_HUMAN|BCR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.48
Assay: Inhibition of Bcr-Abl kinase (unknown origin) after 30 mins by HTRF assay
Drug: nilutamide
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.05
Action type: ANTAGONIST
Assay: Inhibition of 1.0 nM [3H]mibolerone binding to human androgen receptor of PC3/AR cell lysate
Drug: nilvadipine
Target: Voltage-dependent calcium channel gamma-1 subunit (Ion channel)
Gene: CACNG1
UniProt: Q06432 (CCG1_HUMAN)
Organism: Homo sapiens
Drug: nilvadipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: CACNA1C
UniProt: Q13936 (CAC1C_HUMAN)
Organism: Homo sapiens
Drug: nilvadipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1D (Ion channel)
Gene: CACNA1D
UniProt: Q01668 (CAC1D_HUMAN)
Organism: Homo sapiens
Drug: nilvadipine
Target: Voltage-gated L-type calcium channel (Ion channel)
Gene: CACNA1D|CACNA1C
UniProt: Q01668|Q13936 (CAC1D_HUMAN|CAC1C_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Assay: Mechanism of Action
Drug: nimesulide
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.91
Drug: nimesulide
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.42
Assay: Inhibition of COX1 in human whole blood assessed as inhibition of calcium ionophore A-23187-stimulated platelet aggregation by measuring TXB2 production
Drug: nimesulide
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.927
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: nimesulide
Target: Aromatase (Enzyme)
Gene: CYP19A1
UniProt: P11511 (CP19A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.57
Drug: nimesulide
Target: cAMP-specific 3',5'-cyclic phosphodiesterase 4A (Enzyme)
Gene: PDE4A
UniProt: P27815 (PDE4A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.7
Drug: nimesulide
Target: Myeloperoxidase (Enzyme)
Gene: MPO
UniProt: P05164 (PERM_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.68
Assay: Inhibition of recombinant human myeloperoxidase
Drug: nimesulide
Target: Interstitial collagenase (Enzyme)
Gene: MMP1
UniProt: P03956 (MMP1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.632
Assay: DRUGMATRIX: Peptidase, Matrix Metalloproteinase-1 (MMP-1) enzyme inhibition (substrate: Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2)
Drug: nimesulide
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P05979 (PGH1_SHEEP)
Organism: Ovis aries
Activity: IC50 = 5.21
Assay: Inhibition of ovine COX1 assessed as PGF2alpha level by EIA
Drug: nimesulide
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P79208 (PGH2_SHEEP)
Organism: Ovis aries
Activity: IC50 = 6.4
Assay: Inhibition of ovine COX2 assessed as PGF2alpha level by EIA