AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: quercetin
Target: Cyclin-dependent kinase 1/cyclin B (Kinase)
Gene: CCNB2|CDK1|CCNB1|CCNB3
UniProt: O95067|P06493|P14635|Q8WWL7 (CCNB2_HUMAN|CDK1_HUMAN|CCNB1_HUMAN|CCNB3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.12
Assay: Inhibition of cyclin-dependent kinase 1/cyclinB
Drug: quercetin
Target: Cyclin-dependent kinase 4/cyclin D1 (Kinase)
Gene: CDK4|CCND1
UniProt: P11802|P24385 (CDK4_HUMAN|CCND1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.21
Assay: Inhibitory activity against cyclin-dependent kinase 4-cyclin D1
Drug: quercetin
Target: Glycogen synthase kinase-3 (Kinase)
Gene: GSK3A|GSK3B
UniProt: P49840|P49841 (GSK3A_HUMAN|GSK3B_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.68
Assay: Inhibition of glycogen synthase kinase 3
Drug: quercetin
Target: Short transient receptor potential channel 5 (Ion channel)
Gene: TRPC5
UniProt: Q9UL62 (TRPC5_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.19
Assay: Inhibition of human TRPC5 expressed in HEK293 cells assessed as reduction in gadolinium-induced calcium entry after 30 mins by fluo-4 dye based fluorescence assay
Drug: quercetin
Target: Nitric oxide synthase, inducible (Enzyme)
Gene: Nos2
UniProt: P29477 (NOS2_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4.79
Assay: Inhibition of iNOS-mediated nitric oxide production in LPS-stimulated mouse RAW264.7 cells after 24 hrs by Griess reaction analysis
Drug: quercetin
Target: Sorbitol dehydrogenase (Enzyme)
Gene: SORD
UniProt: Q00796 (DHSO_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.45
Assay: In vitro inhibitory activity against sorbitol dehydrogenase (SD) from sheep liver
Drug: quercetin
Target: Chymotrypsin C (Enzyme)
Gene: CTRC
UniProt: Q99895 (CTRC_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4
Assay: Inhibitory activity against chymotrypsinogen
Drug: quercetin
Target: Cell division protein kinase 5 (Kinase)
Gene: Cdk5
UniProt: Q03114 (CDK5_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 4.2
Assay: Inhibition of rat fetal brain CDK5 assessed as phosphorylated histone H1 levels by immuno-precipitation
Drug: quercetin
Target: Hypoxia-inducible factor 1-alpha inhibitor (Enzyme)
Gene: HIF1AN
UniProt: Q9NWT6 (HIF1N_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.99
Assay: Inhibition of human recombinant FIH1
Drug: quercetin
Target: D-alanylalanine synthetase (Enzyme)
Gene: ddlB
UniProt: P07862 (DDLB_ECOLI)
Organism: Escherichia coli (strain K12)
Activity: IC50 = 4.7
Assay: Competitive inhibition of Escherichia coli DdlB using ATP as substrate
Drug: quercetin
Target: Lymphocyte differentiation antigen CD38 (Tumour-associated antigen)
Gene: CD38
UniProt: P28907 (CD38_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.42
Assay: Inhibition of human CD38 using 20 uM 1, N6-etheno NAD+ as substrate by continuous fluorimetric method
Drug: quercetin
Target: Phosphodiesterase 2A (Enzyme)
Gene: Pde2a
UniProt: Q01062 (PDE2A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.09
Assay: Inhibition of rat brain particulate cGMP phosphodiesterase
Drug: quercetin
Target: Cytosol aminopeptidase (Enzyme)
Gene: LAP3
UniProt: P28839 (AMPL_PIG)
Organism: Sus scrofa
Activity: IC50 = 4.46
Assay: Inhibition of pig kidney cytosolic Leucyl aminopeptidase
Drug: quercetin
Target: Glutathione reductase (Enzyme)
Gene: GLR1
UniProt: P41921 (GSHR_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: IC50 = 4.31
Assay: In vitro inhibitory activity against glutathione reductase (GR) from bakers yeast
Drug: quercetin
Target: Amyloid beta A4 protein (Unclassified)
Gene: APP
UniProt: P05067 (A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.1
Assay: Inhibition of amyloid beta (1 to 42) aggregation (unknown origin)
Drug: quercetin
Target: Cytochrome P450 1A1 (Enzyme)
Gene: CYP1A1
UniProt: P04798 (CP1A1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.06
Assay: Inhibition of human CYP1A1 transfected in HEK293 cells assessed as protection against CYP1A1 mediated B[a]P toxicity by measuring B[a]P EC50 at 20 uM by MTT assay (Rvb =1.2+/- 0.3 uM)
Drug: quercetin
Target: Solute carrier family 2, facilitated glucose transporter member 2 (Transporter)
Gene: SLC2A2
UniProt: P11168 (GTR2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.92
Assay: Inhibition of human GLUT2 expressed in Xenopus laevis oocytes assessed as reduction in [14C]fructose uptake by scintillation spectrometric method
Drug: quercetin
Target: ELAV-like protein 3 (Unclassified)
Gene: ELAVL3
UniProt: Q14576 (ELAV3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.75
Assay: Inhibition of ELAV3 (unknown origin)-artificial ARE complex formation after 30 mins in the presence of biotin-labeled RNA probe by chemiluminescence nucleic acid detection method
Drug: quercetin
Target: ELAV-like protein 1 (Unclassified)
Gene: ELAVL1
UniProt: Q15717 (ELAV1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.85
Assay: Inhibition of ELAV1 (unknown origin)-ARE TNFalpha complex formation after 20 mins by liquid scintillation counting method
Drug: quercetin
Target: Solute carrier family 2, facilitated glucose transporter member 4 (Transporter)
Gene: Slc2a4
UniProt: P19357 (GLUT4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.8
Assay: Competitive inhibition of GLUT4 in Wistar rat adipocytes assessed as reduction in insulin-stimulated 3-O-[3H]methyl-D-glucose uptake measured for 30 secs by Lineweaver-Burk plot analysis
Drug: quercetin
Target: Inositol polyphosphate multikinase (Kinase)
Gene: IPMK
UniProt: Q8NFU5 (IPMK_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.64
Assay: Inhibition of human IPMK using insP3 as substrate preincubated for 15 mins followed by substrate and measured after 30 mins by TR-FRET assay
Drug: quercetin
Target: Inositol hexakisphosphate kinase 2 (Kinase)
Gene: IP6K2
UniProt: Q9UHH9 (IP6K2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.16
Assay: Inhibition of human IP6K2 using insP6 as substrate preincubated for 15 mins followed by substrate and measured after 30 mins by TR-FRET assay
Drug: rapacuronium
Target: Muscle-type nicotinic acetylcholine receptor (Ion channel)
Gene: CHRNA1|CHRNG|CHRNB1|CHRNE|CHRND
UniProt: P02708|P07510|P11230|Q04844|Q07001 (ACHA_HUMAN|ACHG_HUMAN|ACHB_HUMAN|ACHE_HUMAN|ACHD_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Assay: Mechanism of Action; CHEMBL2362997; PROTEIN COMPLEX GROUP
Drug: rasagiline
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P22303 (ACES_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.72
Assay: Inhibition of human erythrocyte AChE using acetylthiocholine chloride as substrate incubated for 15 mins by Ellman's method
Drug: rasagiline
Target: Amine oxidase [flavin-containing] B (Enzyme)
Gene: MAOB
UniProt: P27338 (AOFB_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.15
Action type: INHIBITOR
Assay: Binding affinity towards monoamine oxidase B activity was measured using a benzylamine assay
Drug: rasagiline
Target: Cholinesterase (Enzyme)
Gene: BCHE
UniProt: P06276 (CHLE_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.32
Assay: Inhibition of human serum BChE using butyrylthiocholine chloride as substrate incubated for 15 mins by Ellman's method
Drug: rasagiline
Target: Amine oxidase [flavin-containing] A (Enzyme)
Gene: MAOA
UniProt: P21397 (AOFA_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.01
Assay: Binding affinity towards monoamine oxidase A activity was measured using a kynuramine assay
Drug: rasagiline
Target: Amine oxidase [flavin-containing] B (Enzyme)
Gene: Maob
UniProt: P19643 (AOFB_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.36
Assay: In vitro inhibitory concentration against Monoamine oxidase B of rat brain homogenates; value ranges from 0.0035-0.053
Drug: rasagiline
Target: Amine oxidase [flavin-containing] A (Enzyme)
Gene: Maoa
UniProt: P21396 (AOFA_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.39
Assay: In vitro inhibitory concentration against Monoamine oxidase A of rat brain homogenates; value ranges from 0.28-0.54
Drug: resorcinol
Target: Carbonic anhydrase 2 (Enzyme)
Gene: CA2
UniProt: P00918 (CAH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.11
Assay: Inhibition of human carbonic anhydrase 2 by stopped-flow CO2 hydrase assay
Drug: resorcinol
Target: Carbonic anhydrase 9 (Enzyme)
Gene: CA9
UniProt: Q16790 (CAH9_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.16
Assay: Inhibition of human carbonic anhydrase 9 catalytic domain by stopped-flow CO2 hydration assay
Drug: resorcinol
Target: Carbonic anhydrase 12 (Enzyme)
Gene: CA12
UniProt: O43570 (CAH12_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.12
Assay: Inhibition of human carbonic anhydrase 12 catalytic domain by stopped-flow CO2 hydration assay
Drug: resorcinol
Target: Carbonic anhydrase 5A, mitochondrial (Enzyme)
Gene: CA5A
UniProt: P35218 (CAH5A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.06
Assay: Inhibition of human carbonic anhydrase 5A by stopped-flow CO2 hydration assay
Drug: resorcinol
Target: Carbonic anhydrase 5B, mitochondrial (Enzyme)
Gene: CA5B
UniProt: Q9Y2D0 (CAH5B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.15
Assay: Inhibition of human carbonic anhydrase 5B by stopped-flow CO2 hydration assay
Drug: resorcinol
Target: Carbonic anhydrase 14 (Enzyme)
Gene: CA14
UniProt: Q9ULX7 (CAH14_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.97
Assay: Inhibition of human carbonic anhydrase 14 by stopped-flow CO2 hydration assay
Drug: resorcinol
Target: Carbonic anhydrase 13 (Enzyme)
Gene: Ca13
UniProt: Q9D6N1 (CAH13_MOUSE)
Organism: Mus musculus
Activity: Ki = 4.2
Assay: Inhibition of mouse carbonic anhydrase 13 by stopped-flow CO2 hydration assay
Drug: resorcinol
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P05979 (PGH1_SHEEP)
Organism: Ovis aries
Activity: Kd = 4.06
Assay: Binding affinity to COX1 in sheep seminal vesicle
Drug: resorcinol
Target: Carbonic anhydrase (Enzyme)
Gene: ca
UniProt: Q2PCB5 (Q2PCB5_DICLA)
Organism: Dicentrarchus labrax
Activity: Ki = 5.19
Assay: Inhibition of Dicentrarchus labrax CA using 4-nitrophenylacetate substrate by esterase assay
Drug: revaprazan
Target: Potassium-transporting ATPase (Transporter)
Gene: ATP4A|ATP4B
UniProt: P20648|P51164 (ATP4A_HUMAN|ATP4B_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action
Drug: rioprostil
Target: Prostaglandin E2 receptor EP2 subtype (GPCR)
Gene: PTGER2
UniProt: P43116 (PE2R2_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action
Drug: roflumilast
Target: cAMP-specific 3',5'-cyclic phosphodiesterase 4B (Enzyme)
Gene: PDE4B
UniProt: Q07343 (PDE4B_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.4
Assay: Inhibition of human recombinant PDE4B by scintillation proximity assay
Drug: roflumilast
Target: cAMP-specific 3',5'-cyclic phosphodiesterase 4A (Enzyme)
Gene: PDE4A
UniProt: P27815 (PDE4A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.46
Assay: Inhibition of human full length PDE4A4 expressed in baculovirus infected sf21 cells
Drug: roflumilast
Target: cAMP-specific 3',5'-cyclic phosphodiesterase 4D (Enzyme)
Gene: PDE4D
UniProt: Q08499 (PDE4D_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.57
Assay: Inhibition of human PDE4D3 assessed as inhibition of [3H]cAMP hydrolysis to [3H]AMP after 15 mins by scintillation proximity assay
Drug: roflumilast
Target: Phosphodiesterase 4 (Enzyme)
Gene: PDE4A|PDE4B|PDE4C|PDE4D
UniProt: P27815|Q07343|Q08493|Q08499 (PDE4A_HUMAN|PDE4B_HUMAN|PDE4C_HUMAN|PDE4D_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.1
Action type: INHIBITOR
Assay: Inhibition of human phosphodiesterase 4
Drug: roflumilast
Target: Phosphodiesterase (Enzyme)
Gene: PDEB1
UniProt: Q8WQX9 (Q8WQX9_9TRYP)
Organism: Trypanosoma brucei
Activity: Ki = 5.5
Assay: Inhibition of full length Trypanosoma brucei PDEB1 expressed in Sf21 insect cells using cAMP as substrate by scintillation proximity assay
Drug: ruboxistaurin
Target: Tyrosine-protein kinase JAK3 (Kinase)
Gene: JAK3
UniProt: P52333 (JAK3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.38
Assay: Binding constant for JAK3(Kin.Dom.2/JH1 - catalytic) kinase domain
Drug: ruboxistaurin
Target: Platelet-derived growth factor receptor beta (Kinase)
Gene: PDGFRB
UniProt: P09619 (PGFRB_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.15
Assay: Average Binding Constant for PDGFRB; NA=Not Active at 10 uM
Drug: ruboxistaurin
Target: Mast/stem cell growth factor receptor Kit (Kinase)
Gene: KIT
UniProt: P10721 (KIT_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.42
Assay: Average Binding Constant for KIT; NA=Not Active at 10 uM
Drug: ruboxistaurin
Target: Epidermal growth factor receptor (Kinase)
Gene: EGFR
UniProt: P00533 (EGFR_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.29
Assay: Binding constant for EGFR(E746-A750del) kinase domain
Drug: ruboxistaurin
Target: Tyrosine-protein kinase Lck (Kinase)
Gene: LCK
UniProt: P06239 (LCK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.89
Assay: Average Binding Constant for LCK; NA=Not Active at 10 uM
Drug: ruboxistaurin
Target: Receptor-type tyrosine-protein kinase FLT3 (Kinase)
Gene: FLT3
UniProt: P36888 (FLT3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.89
Assay: Binding constant for FLT3(D835Y) kinase domain
Drug: ruboxistaurin
Target: Ribosomal protein S6 kinase alpha-3 (Kinase)
Gene: RPS6KA3
UniProt: P51812 (KS6A3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.66
Assay: Average Binding Constant for RPS6KA3 (Kin.Dom. 1); NA=Not Active at 10 uM
Drug: ruboxistaurin
Target: Serine/threonine-protein kinase pim-1 (Kinase)
Gene: PIM1
UniProt: P11309 (PIM1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.3
Assay: Competitive binding affinity to PIM1 in presence of ATP
Drug: ruboxistaurin
Target: Myosin light chain kinase, smooth muscle (Kinase)
Gene: MYLK
UniProt: Q15746 (MYLK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.54
Assay: Binding constant for MYLK kinase domain
Drug: ruboxistaurin
Target: Death-associated protein kinase 3 (Kinase)
Gene: DAPK3
UniProt: O43293 (DAPK3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.89
Assay: Average Binding Constant for DAPK3; NA=Not Active at 10 uM
Drug: ruboxistaurin
Target: Tyrosine-protein kinase HCK (Kinase)
Gene: HCK
UniProt: P08631 (HCK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.55
Assay: Average Binding Constant for HCK; NA=Not Active at 10 uM
Drug: ruboxistaurin
Target: Protein kinase C beta type (Kinase)
Gene: PRKCB
UniProt: P05771 (KPCB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.33
Assay: Inhibition of Protein kinase C beta 1
Drug: ruboxistaurin
Target: Death-associated protein kinase 2 (Kinase)
Gene: DAPK2
UniProt: Q9UIK4 (DAPK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.59
Assay: Average Binding Constant for DAPK2; NA=Not Active at 10 uM
Drug: ruboxistaurin
Target: Protein kinase C delta type (Kinase)
Gene: PRKCD
UniProt: Q05655 (KPCD_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.44
Assay: Binding constant for PRKCD kinase domain
Drug: ruboxistaurin
Target: cAMP-dependent protein kinase catalytic subunit beta (Kinase)
Gene: PRKACB
UniProt: P22694 (KAPCB_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.49
Assay: Binding constant for full-length PKAC-beta
Drug: ruboxistaurin
Target: Protein kinase C alpha type (Kinase)
Gene: PRKCA
UniProt: P17252 (KPCA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.44
Assay: Inhibition of Protein kinase C alpha
Drug: ruboxistaurin
Target: Calcium/calmodulin-dependent protein kinase type II subunit delta (Kinase)
Gene: CAMK2D
UniProt: Q13557 (KCC2D_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.34
Assay: Binding constant for CAMK2D kinase domain
Drug: ruboxistaurin
Target: Protein kinase C gamma type (Kinase)
Gene: PRKCG
UniProt: P05129 (KPCG_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.52
Assay: Inhibition of Protein kinase C gamma
Drug: ruboxistaurin
Target: Calcium/calmodulin-dependent protein kinase type II subunit gamma (Kinase)
Gene: CAMK2G
UniProt: Q13555 (KCC2G_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.11
Assay: Binding constant for CAMK2G kinase domain
Drug: ruboxistaurin
Target: AP2-associated protein kinase 1 (Kinase)
Gene: AAK1
UniProt: Q2M2I8 (AAK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.05
Assay: Binding constant for AAK1 kinase domain
Drug: ruboxistaurin
Target: Serine/threonine-protein kinase MARK2 (Kinase)
Gene: MARK2
UniProt: Q7KZI7 (MARK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.64
Assay: Average Binding Constant for MARK2; NA=Not Active at 10 uM
Drug: ruboxistaurin
Target: Ribosomal protein S6 kinase alpha-2 (Kinase)
Gene: RPS6KA2
UniProt: Q15349 (KS6A2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.55
Assay: Binding constant for RPS6KA2(Kin.Dom.1 - N-terminal) kinase domain
Drug: ruboxistaurin
Target: Protein kinase C eta type (Kinase)
Gene: PRKCH
UniProt: P24723 (KPCL_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.74
Assay: Binding constant for PRKCH kinase domain
Drug: ruboxistaurin
Target: Fibroblast growth factor receptor 1 (Kinase)
Gene: FGFR1
UniProt: P11362 (FGFR1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.29
Assay: Average Binding Constant for FGFR1; NA=Not Active at 10 uM
Drug: ruboxistaurin
Target: Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform (Kinase)
Gene: PHKG1
UniProt: Q16816 (PHKG1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.57
Assay: Average Binding Constant for PHkg1; NA=Not Active at 10 uM
Drug: ruboxistaurin
Target: Calcium/calmodulin-dependent protein kinase type II subunit alpha (Kinase)
Gene: CAMK2A
UniProt: Q9UQM7 (KCC2A_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.35
Assay: Binding constant for CAMK2A kinase domain
Drug: ruboxistaurin
Target: Serine/threonine-protein kinase 10 (Kinase)
Gene: STK10
UniProt: O94804 (STK10_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.55
Assay: Binding constant for LOK kinase domain
Drug: ruboxistaurin
Target: Protein kinase C epsilon type (Kinase)
Gene: PRKCE
UniProt: Q02156 (KPCE_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.96
Assay: Binding constant for PRKCE kinase domain
Drug: ruboxistaurin
Target: Serine/threonine-protein kinase PLK4 (Kinase)
Gene: PLK4
UniProt: O00444 (PLK4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.43
Assay: Average Binding Constant for STK18; NA=Not Active at 10 uM
Drug: ruboxistaurin
Target: Aurora kinase C (Kinase)
Gene: AURKC
UniProt: Q9UQB9 (AURKC_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.52
Assay: Average Binding Constant for Aurora3; NA=Not Active at 10 uM
Drug: ruboxistaurin
Target: Serine/threonine-protein kinase N1 (Kinase)
Gene: PKN1
UniProt: Q16512 (PKN1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.46
Assay: Binding constant for PKN1 kinase domain
Drug: ruboxistaurin
Target: Protein kinase C theta type (Kinase)
Gene: PRKCQ
UniProt: Q04759 (KPCT_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.6
Assay: Binding constant for PRKCQ kinase domain
Drug: ruboxistaurin
Target: TRAF2 and NCK-interacting protein kinase (Kinase)
Gene: TNIK
UniProt: Q9UKE5 (TNIK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.24
Assay: Average Binding Constant for TNIK; NA=Not Active at 10 uM
Drug: ruboxistaurin
Target: BMP-2-inducible protein kinase (Kinase)
Gene: BMP2K
UniProt: Q9NSY1 (BMP2K_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.37
Assay: Binding constant for BIKE kinase domain
Drug: ruboxistaurin
Target: Serine/threonine-protein kinase pim-2 (Kinase)
Gene: PIM2
UniProt: Q9P1W9 (PIM2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.89
Assay: Average Binding Constant for PIM2; NA=Not Active at 10 uM
Drug: ruboxistaurin
Target: Dual specificity protein kinase CLK1 (Kinase)
Gene: CLK1
UniProt: P49759 (CLK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.04
Assay: Binding constant for full-length CLK1
Drug: ruboxistaurin
Target: Dual specificity protein kinase CLK2 (Kinase)
Gene: CLK2
UniProt: P49760 (CLK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.38
Assay: Binding constant for CLK2 kinase domain
Drug: ruboxistaurin
Target: Mitogen-activated protein kinase kinase kinase kinase 5 (Kinase)
Gene: MAP4K5
UniProt: Q9Y4K4 (M4K5_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.08
Assay: Average Binding Constant for MAP4K5; NA=Not Active at 10 uM
Drug: ruboxistaurin
Target: Cyclin-G-associated kinase (Kinase)
Gene: GAK
UniProt: O14976 (GAK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.96
Assay: Binding constant for GAK kinase domain
Drug: ruboxistaurin
Target: Glycogen synthase kinase-3 beta (Kinase)
Gene: GSK3B
UniProt: P49841 (GSK3B_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.59
Assay: Binding constant for full-length GSK3B
Drug: ruboxistaurin
Target: Calcium/calmodulin-dependent protein kinase type 1D (Kinase)
Gene: CAMK1D
UniProt: Q8IU85 (KCC1D_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.59
Assay: Average Binding Constant for CAMK1D; NA=Not Active at 10 uM
Drug: ruboxistaurin
Target: Cyclin-dependent kinase 16 (Kinase)
Gene: CDK16
UniProt: Q00536 (CDK16_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.59
Assay: Binding constant for PCTK1 kinase domain
Drug: ruboxistaurin
Target: Serine/threonine-protein kinase 4 (Kinase)
Gene: STK4
UniProt: Q13043 (STK4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.66
Assay: Average Binding Constant for STK4; NA=Not Active at 10 uM
Drug: ruboxistaurin
Target: Ribosomal protein S6 kinase alpha-5 (Kinase)
Gene: RPS6KA5
UniProt: O75582 (KS6A5_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.89
Assay: Binding constant for RPS6KA5(Kin.Dom.1 - C-terminal) kinase domain
Drug: ruboxistaurin
Target: STE20-like serine/threonine-protein kinase (Kinase)
Gene: SLK
UniProt: Q9H2G2 (SLK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.4
Assay: Binding constant for SLK kinase domain
Drug: ruboxistaurin
Target: Dual specificity protein kinase CLK4 (Kinase)
Gene: CLK4
UniProt: Q9HAZ1 (CLK4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.72
Assay: Binding constant for CLK4 kinase domain
Drug: ruboxistaurin
Target: Calcium/calmodulin-dependent protein kinase kinase 2 (Kinase)
Gene: CAMKK2
UniProt: Q96RR4 (KKCC2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.96
Assay: Average Binding Constant for CAMKK2; NA=Not Active at 10 uM
Drug: ruboxistaurin
Target: Calcium/calmodulin-dependent protein kinase kinase 1 (Kinase)
Gene: CAMKK1
UniProt: Q8N5S9 (KKCC1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.82
Assay: Average Binding Constant for CAMKK1; NA=Not Active at 10 uM
Drug: ruboxistaurin
Target: 3-phosphoinositide-dependent protein kinase 1 (Kinase)
Gene: PDPK1
UniProt: O15530 (PDPK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.15
Assay: Binding constant for full-length PDPK1
Drug: ruboxistaurin
Target: Serine/threonine-protein kinase 3 (Kinase)
Gene: Stk3
UniProt: Q9JI10 (STK3_MOUSE)
Organism: Mus musculus
Activity: Kd = 7.05
Assay: Average Binding Constant for STK3_m; NA=Not Active at 10 uM
Drug: ruboxistaurin
Target: Cyclin-dependent kinase 7 (Kinase)
Gene: CDK7
UniProt: P50613 (CDK7_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.77
Assay: Binding constant for CDK7 kinase domain
Drug: ruboxistaurin
Target: Ribosomal protein S6 kinase beta-1 (Kinase)
Gene: RPS6KB1
UniProt: P23443 (KS6B1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.68
Assay: Binding constant for S6K1 kinase domain
Drug: ruboxistaurin
Target: Serine/threonine-protein kinase N2 (Kinase)
Gene: PKN2
UniProt: Q16513 (PKN2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.82
Assay: Binding constant for PKN2 kinase domain
Drug: ruboxistaurin
Target: RAC-beta serine/threonine-protein kinase (Kinase)
Gene: AKT2
UniProt: P31751 (AKT2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.06
Assay: Binding constant for AKT2 kinase domain
Drug: ruboxistaurin
Target: Serine/threonine-protein kinase 3 (Kinase)
Gene: STK3
UniProt: Q13188 (STK3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.02
Assay: Binding constant for MST2 kinase domain
Drug: ruboxistaurin
Target: Ribosomal protein S6 kinase alpha-6 (Kinase)
Gene: RPS6KA6
UniProt: Q9UK32 (KS6A6_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.64
Assay: Binding constant for RPS6KA6(Kin.Dom.1 - C-terminal) kinase domain
Drug: ruboxistaurin
Target: NUAK family SNF1-like kinase 2 (Kinase)
Gene: NUAK2
UniProt: Q9H093 (NUAK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.49
Assay: Binding constant for SNARK kinase domain
Drug: ruboxistaurin
Target: Serine/threonine-protein kinase Chk1 (Kinase)
Gene: CHEK1
UniProt: O14757 (CHK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.27
Assay: Binding constant for CHEK1 kinase domain