AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: sunitinib
Target: Serine/threonine-protein kinase DCLK1 (Kinase)
Gene: DCLK1
UniProt: O15075 (DCLK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.43
Assay: Binding constant for DCAMKL1 kinase domain
Drug: sunitinib
Target: Serine/threonine-protein kinase DCLK2 (Kinase)
Gene: DCLK2
UniProt: Q8N568 (DCLK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.57
Assay: Binding constant for DCAMKL2 kinase domain
Drug: sunitinib
Target: Myosin-IIIa (Kinase)
Gene: MYO3A
UniProt: Q8NEV4 (MYO3A_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.51
Assay: Binding constant for MYO3A kinase domain
Drug: sunitinib
Target: Myosin-IIIb (Kinase)
Gene: MYO3B
UniProt: Q8WXR4 (MYO3B_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.35
Assay: Binding constant for MYO3B kinase domain
Drug: sunitinib
Target: Serine/threonine-protein kinase PAK 4 (Kinase)
Gene: PAK4
UniProt: O96013 (PAK4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.64
Assay: Binding constant for PAK4 kinase domain
Drug: sunitinib
Target: Serine/threonine-protein kinase BRSK2 (Kinase)
Gene: BRSK2
UniProt: Q8IWQ3 (BRSK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.96
Assay: Binding constant for full-length BRSK2
Drug: sunitinib
Target: Serine/threonine-protein kinase SIK1 (Kinase)
Gene: SIK1
UniProt: P57059 (SIK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.49
Assay: Binding constant for SNF1LK kinase domain
Drug: sunitinib
Target: Mitogen-activated protein kinase 7 (Kinase)
Gene: MAPK7
UniProt: Q13164 (MK07_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5
Assay: Binding constant for ERK5 kinase domain
Drug: sunitinib
Target: Serine/threonine-protein kinase D2 (Kinase)
Gene: PRKD2
UniProt: Q9BZL6 (KPCD2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.42
Assay: Binding constant for PRKD2 kinase domain
Drug: sunitinib
Target: Serine/threonine-protein kinase D3 (Kinase)
Gene: PRKD3
UniProt: O94806 (KPCD3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.55
Assay: Binding constant for PRKD3 kinase domain
Drug: sunitinib
Target: Interferon-induced, double-stranded RNA-activated protein kinase (Kinase)
Gene: EIF2AK2
UniProt: P19525 (E2AK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.17
Assay: Binding constant for PRKR kinase domain
Drug: sunitinib
Target: Receptor-interacting serine/threonine-protein kinase 1 (Kinase)
Gene: RIPK1
UniProt: Q13546 (RIPK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.43
Assay: Binding constant for RIPK1 kinase domain
Drug: sunitinib
Target: Tyrosine-protein kinase Fes/Fps (Kinase)
Gene: FES
UniProt: P07332 (FES_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.02
Assay: Binding constant for FES kinase domain
Drug: sunitinib
Target: Fibroblast growth factor receptor 4 (Kinase)
Gene: FGFR4
UniProt: P22455 (FGFR4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.68
Assay: Binding constant for FGFR4 kinase domain
Drug: sunitinib
Target: Ribosomal protein S6 kinase alpha-1 (Kinase)
Gene: RPS6KA1
UniProt: Q15418 (KS6A1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.02
Assay: Binding affinity to RPS6KA4(Kin.Dom.1-N-terminal)
Drug: sunitinib
Target: Ribosomal protein S6 kinase alpha-4 (Kinase)
Gene: RPS6KA4
UniProt: O75676 (KS6A4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.02
Assay: Binding constant for RPS6KA4(Kin.Dom.1 - C-terminal) kinase domain
Drug: sunitinib
Target: Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (Kinase)
Gene: PIK3CG
UniProt: P48736 (PK3CG_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.89
Assay: Inhibition of recombinant PI3Kgamma by radioactive phosphotransfer assay in presence of 10 uM ATP
Drug: sunitinib
Target: Casein kinase I isoform alpha (Kinase)
Gene: CSNK1A1
UniProt: P48729 (KC1A_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7
Assay: Binding constant for CSNK1A1 kinase domain
Drug: sunitinib
Target: Mitogen-activated protein kinase kinase kinase kinase 2 (Kinase)
Gene: MAP4K2
UniProt: Q12851 (M4K2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.48
Assay: Binding constant for MAP4K2 kinase domain
Drug: sunitinib
Target: Misshapen-like kinase 1 (Kinase)
Gene: MINK1
UniProt: Q8N4C8 (MINK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.54
Assay: Binding affinity to MINK
Drug: sunitinib
Target: Serine/threonine-protein kinase TBK1 (Kinase)
Gene: TBK1
UniProt: Q9UHD2 (TBK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.92
Assay: Binding affinity to TBK1
Drug: sunitinib
Target: Interleukin-1 receptor-associated kinase 4 (Kinase)
Gene: IRAK4
UniProt: Q9NWZ3 (IRAK4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.18
Assay: Binding constant for IRAK4 kinase domain
Drug: sunitinib
Target: Cyclin-dependent kinase 4 (Kinase)
Gene: CDK4
UniProt: P11802 (CDK4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.7
Assay: Binding constant for CDK4-cyclinD3 kinase domain
Drug: sunitinib
Target: Cyclin-dependent kinase-like 2 (Kinase)
Gene: CDKL2
UniProt: Q92772 (CDKL2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.96
Assay: Binding affinity to CDKL2
Drug: sunitinib
Target: Serine/threonine-protein kinase Chk2 (Kinase)
Gene: CHEK2
UniProt: O96017 (CHK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.15
Assay: Binding affinity to CHEK2
Drug: sunitinib
Target: Protein delta homolog 1 (Unclassified)
Gene: DLK1
UniProt: P80370 (DLK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7
Assay: Binding affinity to DLK
Drug: sunitinib
Target: Dual specificity tyrosine-phosphorylation-regulated kinase 1A (Kinase)
Gene: DYRK1A
UniProt: Q13627 (DYR1A_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.7
Assay: Binding affinity to DYRK1A
Drug: sunitinib
Target: Dual specificity tyrosine-phosphorylation-regulated kinase 2 (Kinase)
Gene: DYRK2
UniProt: Q92630 (DYRK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.17
Assay: Binding affinity to DYRK2
Drug: sunitinib
Target: Ephrin type-B receptor 6 (Kinase)
Gene: EPHB6
UniProt: O15197 (EPHB6_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.07
Assay: Binding affinity to EPHB6
Drug: sunitinib
Target: Serine/threonine-protein kinase/endoribonuclease IRE1 (Kinase)
Gene: ERN1
UniProt: O75460 (ERN1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.22
Assay: Binding affinity to ERN1
Drug: sunitinib
Target: Rhodopsin kinase (Kinase)
Gene: GRK1
UniProt: Q15835 (RK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.54
Assay: Binding affinity to GRK1
Drug: sunitinib
Target: G protein-coupled receptor kinase 4 (Kinase)
Gene: GRK4
UniProt: P32298 (GRK4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.85
Assay: Binding affinity to GRK4
Drug: sunitinib
Target: G protein-coupled receptor kinase 7 (Kinase)
Gene: GRK7
UniProt: Q8WTQ7 (GRK7_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.74
Assay: Binding affinity to GRK7
Drug: sunitinib
Target: Homeodomain-interacting protein kinase 2 (Kinase)
Gene: HIPK2
UniProt: Q9H2X6 (HIPK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.51
Assay: Binding affinity to HIPK2
Drug: sunitinib
Target: Homeodomain-interacting protein kinase 3 (Kinase)
Gene: HIPK3
UniProt: Q9H422 (HIPK3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.39
Assay: Binding affinity to HIPK3
Drug: sunitinib
Target: Homeodomain-interacting protein kinase 4 (Kinase)
Gene: HIPK4
UniProt: Q8NE63 (HIPK4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.8
Assay: Binding affinity to HIPK4
Drug: sunitinib
Target: Hormonally up-regulated neu tumor-associated kinase (Kinase)
Gene: HUNK
UniProt: P57058 (HUNK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.3
Assay: Binding affinity to HUNK
Drug: sunitinib
Target: Serine/threonine-protein kinase ICK (Kinase)
Gene: ICK
UniProt: Q9UPZ9 (ICK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.33
Assay: Binding affinity to ICK
Drug: sunitinib
Target: Inhibitor of nuclear factor kappa-B kinase subunit alpha (Kinase)
Gene: CHUK
UniProt: O15111 (IKKA_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.28
Assay: Binding affinity to IKK-alpha
Drug: sunitinib
Target: Interleukin-1 receptor-associated kinase 1 (Kinase)
Gene: IRAK1
UniProt: P51617 (IRAK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.85
Assay: Binding affinity to IRAK1
Drug: sunitinib
Target: Mitogen-activated protein kinase kinase kinase 13 (Kinase)
Gene: MAP3K13
UniProt: O43283 (M3K13_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.02
Assay: Binding affinity to LZK
Drug: sunitinib
Target: Mitogen-activated protein kinase kinase kinase 2 (Kinase)
Gene: MAP3K2
UniProt: Q9Y2U5 (M3K2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.24
Assay: Binding affinity to MAP3K2
Drug: sunitinib
Target: Mitogen-activated protein kinase kinase kinase 3 (Kinase)
Gene: MAP3K3
UniProt: Q99759 (M3K3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.66
Assay: Binding affinity to MAP3K3
Drug: sunitinib
Target: Microtubule-associated serine/threonine-protein kinase 1 (Kinase)
Gene: MAST1
UniProt: Q9Y2H9 (MAST1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.7
Assay: Binding affinity to MAST1
Drug: sunitinib
Target: Serine/threonine-protein kinase 38 (Kinase)
Gene: STK38
UniProt: Q15208 (STK38_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.39
Assay: Binding affinity to NDR1
Drug: sunitinib
Target: Serine/threonine-protein kinase NIM1 (Kinase)
Gene: NIM1K
UniProt: Q8IY84 (NIM1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.07
Assay: Binding affinity to NIM1
Drug: sunitinib
Target: Serine/threonine-protein kinase OSR1 (Kinase)
Gene: OXSR1
UniProt: O95747 (OXSR1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.28
Assay: Binding affinity to OSR1
Drug: sunitinib
Target: U4/U6 small nuclear ribonucleoprotein Prp4 (Nuclear other)
Gene: PRPF4
UniProt: O43172 (PRP4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.41
Assay: Binding affinity to PRP4
Drug: sunitinib
Target: Serine/threonine-protein kinase RIO2 (Kinase)
Gene: RIOK2
UniProt: Q9BVS4 (RIOK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.31
Assay: Binding affinity to RIOK2
Drug: sunitinib
Target: SRSF protein kinase 3 (Kinase)
Gene: SRPK3
UniProt: Q9UPE1 (SRPK3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.23
Assay: Binding affinity to SRPK3
Drug: sunitinib
Target: STE20/SPS1-related proline-alanine-rich protein kinase (Kinase)
Gene: STK39
UniProt: Q9UEW8 (STK39_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.85
Assay: Binding affinity to STK39
Drug: sunitinib
Target: Mitogen-activated protein kinase kinase kinase 7 (Kinase)
Gene: MAP3K7
UniProt: O43318 (M3K7_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.03
Assay: Binding affinity to TAK1
Drug: sunitinib
Target: Serine/threonine-protein kinase TAO1 (Kinase)
Gene: TAOK1
UniProt: Q7L7X3 (TAOK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.05
Assay: Binding affinity to TAOK1
Drug: sunitinib
Target: Serine/threonine-protein kinase TAO3 (Kinase)
Gene: TAOK3
UniProt: Q9H2K8 (TAOK3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.68
Assay: Binding affinity to TAOK3
Drug: sunitinib
Target: Serine/threonine-protein kinase ULK1 (Kinase)
Gene: ULK1
UniProt: O75385 (ULK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.64
Assay: Binding affinity to ULK1
Drug: sunitinib
Target: Serine/threonine-protein kinase ULK2 (Kinase)
Gene: ULK2
UniProt: Q8IYT8 (ULK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.89
Assay: Binding affinity to ULK2
Drug: sunitinib
Target: Serine/threonine-protein kinase ULK3 (Kinase)
Gene: ULK3
UniProt: Q6PHR2 (ULK3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.38
Assay: Binding affinity to ULK3
Drug: sunitinib
Target: Mitogen-activated protein kinase kinase kinase 19 (Kinase)
Gene: MAP3K19
UniProt: Q56UN5 (M3K19_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.77
Assay: Binding affinity to YSK4
Drug: sunitinib
Target: Homeodomain-interacting protein kinase 1 (Kinase)
Gene: HIPK1
UniProt: Q86Z02 (HIPK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.26
Assay: Binding constant for HIPK1 kinase domain
Drug: sunitinib
Target: Mitogen-activated protein kinase kinase kinase 15 (Kinase)
Gene: MAP3K15
UniProt: Q6ZN16 (M3K15_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.89
Assay: Binding affinity to MAP3K15
Drug: sunitinib
Target: Serine/threonine-protein kinase PLK2 (Kinase)
Gene: PLK2
UniProt: Q9NYY3 (PLK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.33
Assay: Binding affinity to PLK2
Drug: sunitinib
Target: Receptor-interacting serine/threonine-protein kinase 4 (Kinase)
Gene: RIPK4
UniProt: P57078 (RIPK4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.68
Assay: Binding affinity to RIPK4
Drug: sunitinib
Target: Uncharacterized serine/threonine-protein kinase SBK3 (Kinase)
Gene: SBK3
UniProt: P0C264 (SBK3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.72
Assay: Binding affinity to SgK110
Drug: sunitinib
Target: Serine/threonine-protein kinase 35 (Kinase)
Gene: STK35
UniProt: Q8TDR2 (STK35_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.89
Assay: Binding affinity to STK35
Drug: sunitinib
Target: Tankyrase-2 (Enzyme)
Gene: TNKS2
UniProt: Q9H2K2 (TNKS2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.05
Assay: Binding affinity to TNK2
Drug: sunitinib
Target: Megakaryocyte-associated tyrosine-protein kinase (Kinase)
Gene: MATK
UniProt: P42679 (MATK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.11
Assay: Binding constant for CTK kinase domain
Drug: sunitinib
Target: Bone morphogenetic protein receptor type-1B (Kinase)
Gene: BMPR1B
UniProt: O00238 (BMR1B_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.62
Assay: Binding constant for BMPR1B kinase domain
Drug: sunitinib
Target: Serine/threonine-protein kinase SBK1 (Kinase)
Gene: SBK1
UniProt: Q52WX2 (SBK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.7
Assay: Binding constant for SBK1 kinase domain
Drug: sunitinib
Target: Serine/threonine-protein kinase PRP4 homolog (Kinase)
Gene: PRPF4B
UniProt: Q13523 (PRP4B_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.41
Assay: Binding constant for PRP4 kinase domain
Drug: sunitinib
Target: Mitogen-activated protein kinase kinase kinase 12 (Kinase)
Gene: MAP3K12
UniProt: Q12852 (M3K12_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7
Assay: Binding constant for DLK kinase domain
Drug: sunitinib
Target: Serine/threonine-protein kinase Sgk3 (Kinase)
Gene: SGK3
UniProt: Q96BR1 (SGK3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.66
Assay: Binding constant for SGK3 kinase domain
Drug: sunitinib
Target: SNF-related serine/threonine-protein kinase (Kinase)
Gene: SNRK
UniProt: Q9NRH2 (SNRK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.19
Assay: Binding constant for SNRK kinase domain
Drug: sunitinib
Target: Dual specificity mitogen-activated protein kinase kinase 5 (Kinase)
Gene: MAP2K5
UniProt: Q13163 (MP2K5_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.34
Assay: Binding constant for MEK5 kinase domain
Drug: sunitinib
Target: Myosin light chain kinase 3 (Kinase)
Gene: MYLK3
UniProt: Q32MK0 (MYLK3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.64
Assay: Binding constant for MLCK kinase domain
Drug: sunitinib
Target: Leucine-rich repeat serine/threonine-protein kinase 2 (Kinase)
Gene: LRRK2
UniProt: Q5S007 (LRRK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.12
Assay: Binding constant for LRRK2(G2019S) kinase domain
Drug: sunitinib
Target: Dual serine/threonine and tyrosine protein kinase (Kinase)
Gene: DSTYK
UniProt: Q6XUX3 (DUSTY_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.89
Assay: Binding constant for RIPK5 kinase domain
Drug: sunitinib
Target: Calcium-dependent protein kinase 1 (Kinase)
Gene: CPK1
UniProt: P62344 (CDPK1_PLAF7)
Organism: Plasmodium falciparum
Activity: Kd = 5.89
Assay: Binding constant for PFCDPK1(P.falciparum) kinase domain
Drug: sunitinib
Target: Serine/threonine-protein kinase PknB (Kinase)
Gene: pknB
UniProt: P9WI81 (PKNB_MYCTU)
Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv)
Activity: Kd = 7.06
Assay: Binding constant for PKNB(M.tuberculosis) kinase domain
Drug: sunitinib
Target: Bromodomain-containing protein 9 (Unclassified)
Gene: BRD9
UniProt: Q9H8M2 (BRD9_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.77
Assay: Binding affinity to BRD9 (unknown origin) assessed as dissociation constant by qPCR analysis
Drug: sunitinib
Target: Ephrin type-A receptor 7 (Kinase)
Gene: EPHA7
UniProt: Q15375 (EPHA7_HUMAN)
Organism: Homo sapiens
Activity: Kd  5.62
Drug: sunitinib
Target: Ephrin type-B receptor 4 (Kinase)
Gene: EPHB4
UniProt: P54760 (EPHB4_HUMAN)
Organism: Homo sapiens
Activity: Kd  5.509
Drug: sunitinib
Target: Proto-oncogene tyrosine-protein kinase receptor Ret (Kinase)
Gene: RET
UniProt: P07949 (RET_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.8
Action type: INHIBITOR
Drug: sunitinib
Target: Vascular endothelial growth factor receptor 1 (Kinase)
Gene: FLT1
UniProt: P17948 (VGFR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.229
Action type: INHIBITOR
Assay: inhibition at physiological ATP concentration
Drug: sunitinib
Target: Platelet-derived growth factor receptor alpha (Kinase)
Gene: PDGFRA
UniProt: P16234 (PGFRA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.959
Action type: INHIBITOR
Assay: inhibition at physiological ATP concentration
Drug: suprofen
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.06
Action type: INHIBITOR
Drug: suprofen
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.96
Action type: INHIBITOR
Drug: suprofen
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.347
Drug: secretin human
Target: Secretin receptor (GPCR)
Gene: SCTR
UniProt: P47872 (SCTR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 9.7
Action type: AGONIST
Drug: tacrine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.29
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: tacrine
Target: Aldehyde oxidase (Enzyme)
Gene: AOX1
UniProt: Q06278 (AOXA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.301
Drug: tacrine
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.523
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: tacrine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.954
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: tacrine
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P22303 (ACES_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.14
Action type: INHIBITOR
Drug: tacrine
Target: Acetylcholine receptor subunit epsilon (Ion channel)
Gene: CHRNE
UniProt: Q04844 (ACHE_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.36
Assay: Inhibition of acetylcholinesterase
Drug: tacrine
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.66
Assay: Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
Drug: tacrine
Target: Acetylcholinesterase (Enzyme)
Gene: ache
UniProt: P04058 (ACES_TORCA)
Organism: Torpedo californica
Activity: Ki = 7.4
Assay: Inhibition of Torpedo californica AChE
Drug: tacrine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.56
Drug: tacrine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: Chrm2
UniProt: P10980 (ACM2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.68
Assay: Binding affinity against mouse M2 muscarinic receptor using heart tissue and [3H]N-methylscopolamine
Drug: tacrine
Target: Acetylcholinesterase (Enzyme)
Gene: Ache
UniProt: P21836 (ACES_MOUSE)
Organism: Mus musculus
Activity: Kd = 7.74
Assay: Dissociation constant towards Acetylcholinesterase in mouse
Drug: tacrine
Target: Butyrylcholinesterase; Protein Bche (Enzyme)
Gene: Bche
UniProt: Q9JKC1 (Q9JKC1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.05
Assay: Inhibition of rat plasma butyrylcholine esterase in presence of butyrylcholine substrate by chemiluminescent assay
Drug: tacrine
Target: Acetylcholinesterase (Enzyme)
Gene: Ache
UniProt: P37136 (ACES_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.34
Assay: Inhibition of Acetylcholinesterase in rat red blood cell
Drug: tacrine
Target: Acetylcholinesterase (Enzyme)
Gene: ache
UniProt: O42275 (ACES_ELEEL)
Organism: Electrophorus electricus
Activity: Ki = 8
Assay: Tested for in vitro inhibition of acetylcholinesterase
Drug: tacrine
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P23795 (ACES_BOVIN)
Organism: Bos taurus
Activity: Ki = 7.4
Assay: Inhibition of fetal Bovine serum AChE
Drug: tacrine
Target: Choline O-acetyltransferase (Enzyme)
Gene: Chat
UniProt: P32738 (CLAT_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.82
Assay: Inhibition constant determined against Acetylcholinesterase (AChE) receptor.
Drug: tacrine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: Chrm1
UniProt: P12657 (ACM1_MOUSE)
Organism: Mus musculus
Activity: IC50 = 5.7
Assay: Binding affinity against mouse Muscarinic acetylcholine receptor M1 using cerebral cortex and [3H]pirenzepine
Drug: tacrine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: Chrm2
UniProt: Q9ERZ4 (ACM2_MOUSE)
Organism: Mus musculus
Activity: Ki = 6.66
Assay: Ability to displace [3H]oxotremorine ([3H]-OXO-M) from mouse cerebral cortex
Drug: tacrine
Target: Amine oxidase [flavin-containing] A (Enzyme)
Gene: Maoa
UniProt: P21396 (AOFA_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.4
Assay: Inhibition of mitochondrial MAO-A in rat liver homogenates using [14C]-(5-hydroxy-triptamine) as substrate preincubated for 30 mins by liquid scintillation counting
Drug: tacrine
Target: Cholinesterase (Enzyme)
Gene: Bche
UniProt: Q03311 (CHLE_MOUSE)
Organism: Mus musculus
Activity: IC50 = 7.2
Assay: Inhibition of BuChE in Swiss Webster mouse whole blood serum using butyrylthiocholine iodide as substrate preincubated for 10 mins followed substrate addition measured after 10 mins by Ellman's method
Drug: tacrine
Target: Histamine N-methyltransferase (Enzyme)
Gene: Hnmt
UniProt: Q01984 (HNMT_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.96
Assay: Inhibition of rat kidney Histamine N-Methyltransferase (HMT) activity determined by the formation of N-methyl-histamine
Drug: tacrine
Target: Butyrylcholinesterase (Enzyme)
Gene: BCHE
UniProt: Q9N1N9 (Q9N1N9_HORSE)
Organism: Equus caballus
Activity: Ki = 8.15
Assay: Inhibition of Equine Butyrylcholinesterase
Drug: tacrine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P06199 (ACM2_PIG)
Organism: Sus scrofa
Activity: EC50 = 5.2
Assay: Inhibition of [3H]NMS dissociation from porcine muscarinic M2 receptor
Drug: tacrine
Target: Cholinesterase (Enzyme)
Gene: BCHE
UniProt: P81908 (CHLE_HORSE)
Organism: Equus caballus
Activity: IC50 = 8.61
Assay: Inhibition of equine BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins before substrate addition measured for 10 mins by Ellman's method
Drug: tacrine
Target: Glutamate NMDA receptor; GRIN1/GRIN2B (Ion channel)
Gene: GRIN1|GRIN2B
UniProt: Q05586|Q13224 (NMDZ1_HUMAN|NMDE2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.36
Assay: Inhibition of dexamethasone-induced human NR1-1a/NR2B receptor-mediated excitotoxicity in (S)-glutamate/glycine-stimulated mouse L13-E6 cells assessed as LDH release after 30 mins
Drug: tacrine
Target: Glutamate NMDA receptor; GRIN1/GRIN2A (Ion channel)
Gene: GRIN1|GRIN2A
UniProt: Q05586|Q12879 (NMDZ1_HUMAN|NMDE1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.31
Assay: Inhibition of dexamethasone-induced human NR1-1a/NR2A receptor-mediated excitotoxicity in (S)-glutamate/glycine-stimulated mouse L12-G10 cells assessed as LDH release after 30 mins
Drug: tacrine
Target: Muscarinic acetylcholine receptor (GPCR)
Gene: Chrm1|Chrm3|Chrm4|Chrm5|Chrm2
UniProt: P08482|P08483|P08485|P08911|P10980 (ACM1_RAT|ACM3_RAT|ACM4_RAT|ACM5_RAT|ACM2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.23
Assay: Inhibition of [3H]quinuclidinyl benzilate (QNB) binding from rat forebrain membranes in the presence of Zn
Drug: tacrine
Target: Amyloid beta A4 protein (Unclassified)
Gene: APP
UniProt: P05067 (A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.91
Assay: Inhibition of self-mediated amyloid beta (1 to 42) (unknown origin) aggregation after 24 hrs by thioflavin T fluorescence assay