AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: gefitinib
Target: Activated CDC42 kinase 1 (Kinase)
Gene: TNK2
UniProt: Q07912 (ACK1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.64
Assay: Kinase Assay: FlashPlates from Perkin Elmer (Boston, Mass., USA) with a 50 μl reaction volume are used. The reaction cocktail was pipetted in 4 steps in the following order: 15 μl of ATP solution (in H2O), 20 μl of assay buffer (see below), 5 μl of test sample in 10% DMSO, 10 μl of enzyme/substrate mixture (in H2O). The assay for all enzymes contained 60 mM HEPES-NaOH, pH 7.5, 3 mM MgCl2, 3 mM MnCl2, 3 μM Na-orthovanadate, 1.2 mM DTT, 50 μg/ml PEG20000, 1 μM [γ-33P]-ATP (approx. 8×10^5 cpm per well), protein kinase (variable amounts see Table 1), and substrate (variable amounts). Certain assays also contained 1 mM CaCl2, 4 mM EDTA, 5 μg/ml Phosphatidylserine and 1 μg/ml 1.2-Dioleyl-glycerol. The MYLK2, CAMK1D, CAMK2A, CAMK2B, CAMK2D, CAMK4, CAMKK2, DAPK2 and EEF2K assays additionally contained 1 μg/ml Calmodulin and 0.5 mM CaCl2. The PRKG1 and PRKG2 assays additionally contained 1 μM cGMP. Recombinant Protein Kinases: All protein kinases were expressed in Sf9 insect cells or
Drug: gefitinib
Target: STE20-like serine/threonine-protein kinase (Kinase)
Gene: SLK
UniProt: Q9H2G2 (SLK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.04
Assay: Binding constant for SLK kinase domain
Drug: gefitinib
Target: MAP kinase-interacting serine/threonine-protein kinase 2 (Kinase)
Gene: MKNK2
UniProt: Q9HBH9 (MKNK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.44
Assay: Average Binding Constant for MKNK2; NA=Not Active at 10 uM
Drug: gefitinib
Target: Mitogen-activated protein kinase 9 (Kinase)
Gene: MAPK9
UniProt: P45984 (MK09_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.85
Assay: Average Binding Constant for JNK2; NA=Not Active at 10 uM
Drug: gefitinib
Target: Ephrin type-B receptor 4 (Kinase)
Gene: EPHB4
UniProt: P54760 (EPHB4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.6
Assay: Binding constant for EPHB4 kinase domain
Drug: gefitinib
Target: Serine/threonine-protein kinase ULK3 (Kinase)
Gene: Ulk3
UniProt: Q3U3Q1 (ULK3_MOUSE)
Organism: Mus musculus
Activity: Kd = 5.85
Assay: Average Binding Constant for ULK3 m; NA=Not Active at 10 uM
Drug: gefitinib
Target: Protein-tyrosine kinase 6 (Kinase)
Gene: PTK6
UniProt: Q13882 (PTK6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.01
Assay: Kinase Assay: FlashPlates from Perkin Elmer (Boston, Mass., USA) with a 50 μl reaction volume are used. The reaction cocktail was pipetted in 4 steps in the following order: 15 μl of ATP solution (in H2O), 20 μl of assay buffer (see below), 5 μl of test sample in 10% DMSO, 10 μl of enzyme/substrate mixture (in H2O). The assay for all enzymes contained 60 mM HEPES-NaOH, pH 7.5, 3 mM MgCl2, 3 mM MnCl2, 3 μM Na-orthovanadate, 1.2 mM DTT, 50 μg/ml PEG20000, 1 μM [γ-33P]-ATP (approx. 8×10^5 cpm per well), protein kinase (variable amounts see Table 1), and substrate (variable amounts). Certain assays also contained 1 mM CaCl2, 4 mM EDTA, 5 μg/ml Phosphatidylserine and 1 μg/ml 1.2-Dioleyl-glycerol. The MYLK2, CAMK1D, CAMK2A, CAMK2B, CAMK2D, CAMK4, CAMKK2, DAPK2 and EEF2K assays additionally contained 1 μg/ml Calmodulin and 0.5 mM CaCl2. The PRKG1 and PRKG2 assays additionally contained 1 μM cGMP. Recombinant Protein Kinases: All protein kinases were expressed in Sf9 insect cells or
Drug: gefitinib
Target: Tyrosine-protein kinase receptor UFO (Kinase)
Gene: AXL
UniProt: P30530 (UFO_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.74
Assay: Binding constant for AXL kinase domain
Drug: gefitinib
Target: Cyclin-dependent kinase 7 (Kinase)
Gene: CDK7
UniProt: P50613 (CDK7_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.21
Assay: Binding constant for CDK7 kinase domain
Drug: gefitinib
Target: Serine/threonine-protein kinase D1 (Kinase)
Gene: PRKD1
UniProt: Q15139 (KPCD1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.46
Assay: Binding constant for PRKD1 kinase domain
Drug: gefitinib
Target: Serine/threonine-protein kinase DCLK3 (Kinase)
Gene: DCLK3
UniProt: Q9C098 (DCLK3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.54
Assay: Binding constant for DCAMKL3 kinase domain
Drug: gefitinib
Target: NUAK family SNF1-like kinase 2 (Kinase)
Gene: NUAK2
UniProt: Q9H093 (NUAK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.34
Assay: Binding constant for SNARK kinase domain
Drug: gefitinib
Target: Casein kinase I isoform delta (Kinase)
Gene: CSNK1D
UniProt: P48730 (KC1D_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.49
Assay: Binding constant for CSNK1D kinase domain
Drug: gefitinib
Target: Tyrosine-protein kinase TXK (Kinase)
Gene: TXK
UniProt: P42681 (TXK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.22
Assay: Binding constant for TXK kinase domain
Drug: gefitinib
Target: MAP kinase-interacting serine/threonine-protein kinase 1 (Kinase)
Gene: MKNK1
UniProt: Q9BUB5 (MKNK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.54
Assay: Binding constant for full-length MKNK1
Drug: gefitinib
Target: Serine/threonine-protein kinase NLK (Kinase)
Gene: NLK
UniProt: Q9UBE8 (NLK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.38
Assay: Binding constant for NLK kinase domain
Drug: gefitinib
Target: Interleukin-1 receptor-associated kinase 3 (Kinase)
Gene: IRAK3
UniProt: Q9Y616 (IRAK3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.82
Assay: Binding constant for IRAK3 kinase domain
Drug: gefitinib
Target: Serine/threonine-protein kinase SIK2 (Kinase)
Gene: SIK2
UniProt: Q9H0K1 (SIK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.68
Assay: Binding constant for full-length SNF1LK2
Drug: gefitinib
Target: Myotonin-protein kinase (Kinase)
Gene: DMPK
UniProt: Q09013 (DMPK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.16
Assay: Binding constant for DMPK kinase domain
Drug: gefitinib
Target: Leukocyte tyrosine kinase receptor (Kinase)
Gene: LTK
UniProt: P29376 (LTK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.26
Assay: Binding constant for LTK kinase domain
Drug: gefitinib
Target: Serine/threonine-protein kinase pim-3 (Kinase)
Gene: PIM3
UniProt: Q86V86 (PIM3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.24
Assay: Binding constant for PIM3 kinase domain
Drug: gefitinib
Target: Tyrosine-protein kinase Blk (Kinase)
Gene: BLK
UniProt: P51451 (BLK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.92
Assay: Binding constant for BLK kinase domain
Drug: gefitinib
Target: Citron Rho-interacting kinase (Kinase)
Gene: CIT
UniProt: O14578 (CTRO_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.89
Assay: Binding constant for CIT kinase domain
Drug: gefitinib
Target: Ephrin type-A receptor 1 (Kinase)
Gene: EPHA1
UniProt: P21709 (EPHA1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.4
Assay: Binding constant for EPHA1 kinase domain
Drug: gefitinib
Target: Tubulin alpha-1A chain (Structural)
Gene: Tuba1a
UniProt: P68370 (TBA1A_RAT)
Organism: Rattus norvegicus
Activity: Kd = 6.39
Assay: Binding constant for ERBB4 kinase domain
Drug: gefitinib
Target: Mitogen-activated protein kinase 6 (Kinase)
Gene: MAPK6
UniProt: Q16659 (MK06_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.8
Assay: Binding constant for ERK3 kinase domain
Drug: gefitinib
Target: Mitogen-activated protein kinase 4 (Kinase)
Gene: MAPK4
UniProt: P31152 (MK04_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.51
Assay: Binding constant for ERK4 kinase domain
Drug: gefitinib
Target: Ribosomal protein S6 kinase alpha-4 (Kinase)
Gene: RPS6KA4
UniProt: O75676 (KS6A4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.92
Assay: Binding constant for RPS6KA4(Kin.Dom.2-C-terminal) kinase domain
Drug: gefitinib
Target: Cruzipain (Enzyme)
UniProt: P25779 (CYSP_TRYCR)
Organism: Trypanosoma cruzi
Activity: IC50 = 4.06
Assay: Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in absence of Triton X-100
Drug: gefitinib
Target: Misshapen-like kinase 1 (Kinase)
Gene: MINK1
UniProt: Q8N4C8 (MINK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.74
Assay: Binding constant for MINK kinase domain
Drug: gefitinib
Target: Interleukin-1 receptor-associated kinase 4 (Kinase)
Gene: IRAK4
UniProt: Q9NWZ3 (IRAK4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.27
Assay: Binding constant for IRAK4 kinase domain
Drug: gefitinib
Target: Serine/threonine-protein kinase Chk2 (Kinase)
Gene: CHEK2
UniProt: O96017 (CHK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.1
Assay: Binding constant for CHEK2 kinase domain
Drug: gefitinib
Target: Ephrin type-B receptor 6 (Kinase)
Gene: EPHB6
UniProt: O15197 (EPHB6_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.49
Assay: Binding constant for EPHB6 kinase domain
Drug: gefitinib
Target: Homeodomain-interacting protein kinase 4 (Kinase)
Gene: HIPK4
UniProt: Q8NE63 (HIPK4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.51
Assay: Binding constant for HIPK4 kinase domain
Drug: gefitinib
Target: Interleukin-1 receptor-associated kinase 1 (Kinase)
Gene: IRAK1
UniProt: P51617 (IRAK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.16
Assay: Binding constant for IRAK1 kinase domain
Drug: gefitinib
Target: Mitogen-activated protein kinase kinase kinase 2 (Kinase)
Gene: MAP3K2
UniProt: Q9Y2U5 (M3K2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.48
Assay: Binding constant for MAP3K2 kinase domain
Drug: gefitinib
Target: Mitogen-activated protein kinase kinase kinase 3 (Kinase)
Gene: MAP3K3
UniProt: Q99759 (M3K3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.68
Assay: Binding constant for MAP3K3 kinase domain
Drug: gefitinib
Target: Mitogen-activated protein kinase kinase kinase 19 (Kinase)
Gene: MAP3K19
UniProt: Q56UN5 (M3K19_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.62
Assay: Binding constant for YSK4 kinase domain
Drug: gefitinib
Target: Receptor tyrosine-protein kinase erbB-3 (Kinase)
Gene: ERBB3
UniProt: P21860 (ERBB3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.1
Assay: Binding constant for ERBB3 kinase domain
Drug: gefitinib
Target: Quinolone resistance protein NorA (Transporter)
Gene: norA
UniProt: P0A0J7 (NORA_STAAU)
Organism: Staphylococcus aureus
Activity: IC50 = 5.01
Assay: Inhibition of NorA in Staphylococcus aureus SA1199B harboring GrlA A116E mutant assessed as inhibition of ethidium bromide efflux after 5 mins by fluorometric method
Drug: gefitinib
Target: Serine/threonine-protein kinase SBK1 (Kinase)
Gene: SBK1
UniProt: Q52WX2 (SBK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.25
Assay: Binding constant for SBK1 kinase domain
Drug: gefitinib
Target: Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma (Kinase)
Gene: PIP4K2C
UniProt: Q8TBX8 (PI42C_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.12
Assay: Binding constant for PIP5K2C kinase domain
Drug: gefitinib
Target: Dual specificity mitogen-activated protein kinase kinase 5 (Kinase)
Gene: MAP2K5
UniProt: Q13163 (MP2K5_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.22
Assay: Binding constant for MEK5 kinase domain
Drug: gefitinib
Target: Proto-oncogene tyrosine-protein kinase Src (Kinase)
Gene: SRC
UniProt: P12931 (SRC_HUMAN)
Organism: Homo sapiens
Activity: Kd  5.42
Drug: gemcitabine
Target: Thymidylate synthase (Enzyme)
Gene: TYMS
UniProt: P04818 (TYSY_HUMAN)
Organism: Homo sapiens
Drug: gemcitabine
Target: Deoxycytidine kinase (Kinase)
Gene: DCK
UniProt: P27707 (DCK_HUMAN)
Organism: Homo sapiens
Drug: gemcitabine
Target: Ribonucleoside-diphosphate reductase large subunit (Enzyme)
Gene: RRM1
UniProt: P23921 (RIR1_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Drug: gemcitabine
Target: Ribonucleoside-diphosphate reductase subunit M2 (Enzyme)
Gene: RRM2
UniProt: P31350 (RIR2_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Drug: gemcitabine
Target: UMP-CMP kinase (Kinase)
Gene: CMPK1
UniProt: P30085 (KCY_HUMAN)
Organism: Homo sapiens
Drug: gemcitabine
Target: DNA polymerase (alpha/delta/epsilon) (Enzyme)
Gene: POLA1|POLD1|POLE
UniProt: P09884|P28340|Q07864 (DPOLA_HUMAN|DPOD1_HUMAN|DPOE1_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2363042; PROTEIN FAMILY
Drug: gemfibrozil
Target: Lipoprotein lipase (Enzyme)
Gene: LPL
UniProt: P06858 (LIPL_HUMAN)
Organism: Homo sapiens
Drug: gemfibrozil
Target: Transthyretin (Secreted)
Gene: TTR
UniProt: P02766 (TTHY_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7
Drug: gemfibrozil
Target: Cytochrome P450 2C8 (Enzyme)
Gene: CYP2C8
UniProt: P10632 (CP2C8_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.74
Drug: gemfibrozil
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.523
Drug: gemfibrozil
Target: Peroxisome proliferator-activated receptor alpha (Nuclear hormone receptor)
Gene: PPARA
UniProt: Q07869 (PPARA_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.23
Action type: AGONIST
Drug: gemfibrozil
Target: Fatty acid-binding protein, liver (Unclassified)
Gene: Fabp1
UniProt: P02692 (FABPL_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.73
Assay: Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP high binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay
Drug: gemfibrozil
Target: CDGSH iron-sulfur domain-containing protein 1 (Unclassified)
Gene: CISD1
UniProt: Q9NZ45 (CISD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.14
Assay: Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by Cheng-Prusoff analysis
Drug: gemifloxacin
Target: DNA topoisomerase 4 subunit A (Enzyme)
Gene: parC
UniProt: P0C1U9 (PARC_STAAU)
Organism: Staphylococcus aureus
Activity: IC50 = 6.52
Drug: gemifloxacin
Target: DNA gyrase subunit B (Enzyme)
Gene: gyrB
UniProt: P0AES7 (GYRB_ECO57)
Organism: Escherichia coli O157:H7
Drug: gemifloxacin
Target: DNA topoisomerase 4 subunit A (Enzyme)
Gene: parC
UniProt: P72525 (PARC_STRPN)
Organism: Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4)
Action type: INHIBITOR
Drug: gestodene
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Drug: gestodene
Target: Cytochrome P450 3A5 (Enzyme)
Gene: CYP3A5
UniProt: P20815 (CP3A5_HUMAN)
Organism: Homo sapiens
Drug: gestrinone
Target: Sex hormone-binding globulin (Secreted)
Gene: SHBG
UniProt: P04278 (SHBG_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.11
Assay: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin
Drug: gimeracil
Target: Dihydropyrimidine dehydrogenase [NADP(+)] (Enzyme)
Gene: DPYD
UniProt: Q12882 (DPYD_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.638
Action type: INHIBITOR
Assay: Mechanism of Action
Drug: glafenine
Target: Bile salt export pump (Transporter)
Gene: ABCB11
UniProt: O95342 (ABCBB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.65
Drug: glafenine
Target: Bile salt export pump (Transporter)
Gene: Abcb11
UniProt: O70127 (ABCBB_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.49
Drug: glibornuride
Target: Sulfonylurea receptor 2, Kir6.2 (Ion channel)
Gene: ABCC9|KCNJ11
UniProt: O60706|Q14654 (ABCC9_HUMAN|KCJ11_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.17
Action type: BLOCKER
Drug: glibornuride
Target: Sulfonylurea receptor 1, Kir6.2 (Ion channel)
Gene: ABCC8|KCNJ11
UniProt: Q09428|Q14654 (ABCC8_HUMAN|KCJ11_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.046
Action type: BLOCKER
Assay: [86]Rb+ efflux in RINm5F insulinoma cells
Drug: gliclazide
Target: Sulfonylurea receptor 2, Kir6.2 (Ion channel)
Gene: ABCC9|KCNJ11
UniProt: O60706|Q14654 (ABCC9_HUMAN|KCJ11_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.13
Action type: BLOCKER
Drug: gliclazide
Target: Sulfonylurea receptor 1, Kir6.2 (Ion channel)
Gene: ABCC8|KCNJ11
UniProt: Q09428|Q14654 (ABCC8_HUMAN|KCJ11_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.222
Action type: BLOCKER
Assay: [86]Rb+ efflux in RINm5F insulinoma cells
Drug: glimepiride
Target: Sulfonylurea receptor 1, Kir6.2 (Ion channel)
Gene: ABCC8|KCNJ11
UniProt: Q09428|Q14654 (ABCC8_HUMAN|KCJ11_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.24
Action type: BLOCKER
Drug: glimepiride
Target: Sulfonylurea receptor 2, Kir6.2 (Ion channel)
Gene: ABCC9|KCNJ11
UniProt: O60706|Q14654 (ABCC9_HUMAN|KCJ11_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.98
Action type: BLOCKER
Drug: glipizide
Target: Sulfonylurea receptor 1, Kir6.2 (Ion channel)
Gene: ABCC8|KCNJ11
UniProt: Q09428|Q14654 (ABCC8_HUMAN|KCJ11_HUMAN)
Organism: Homo sapiens
Activity: Kd = 9.097
Action type: BLOCKER
Assay: [86]Rb+ efflux in RINm5F insulinoma cells
Drug: gliquidone
Target: Sulfonylurea receptor 1, Kir6.2 (Ion channel)
Gene: ABCC8|KCNJ11
UniProt: Q09428|Q14654 (ABCC8_HUMAN|KCJ11_HUMAN)
Organism: Homo sapiens
Activity: Kd = 9
Action type: BLOCKER
Assay: [86]Rb+ efflux in RINm5F insulinoma cells
Drug: glisoxepide
Target: Sulfonylurea receptor 1, Kir6.2 (Ion channel)
Gene: ABCC8|KCNJ11
UniProt: Q09428|Q14654 (ABCC8_HUMAN|KCJ11_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.959
Action type: BLOCKER
Assay: [86]Rb+ efflux in RINm5F insulinoma cells
Drug: glutamic acid
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.21
Assay: Inhibitory concentration against human Adenosine A3 receptor expressed in HEK293 cells using 0.1 nM [3H]AB-MECA
Drug: glutamic acid
Target: Glutathione reductase, mitochondrial (Enzyme)
Gene: GSR
UniProt: P00390 (GSHR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.37
Assay: Competitive inhibition of human erythrocyte Glutathione reductase using GSSG substrate by Lineweaver-Burk plot analysis
Drug: glutamic acid
Target: Glutamate receptor 1 (Ion channel)
Gene: GRIA1
UniProt: P42261 (GRIA1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.87
Assay: Compound was tested for binding affinity against human Ionotropic glutamate receptor AMPA 1 in HEK293 cells using [3H]-AMPA as radioligand
Drug: glutamic acid
Target: Glutamate receptor ionotropic, kainate 1 (Ion channel)
Gene: GRIK1
UniProt: P39086 (GRIK1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.15
Assay: Binding affinity against human ionotropic glutamate receptor kainate 1 in HK293 cells using [3H]kainate as radioligand
Drug: glutamic acid
Target: Glutamate receptor 2 (Ion channel)
Gene: GRIA2
UniProt: P42262 (GRIA2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.03
Assay: Compound was tested for binding affinity against human Ionotropic glutamate receptor AMPA 2 in HK293 cells using [3H]AMPA as radioligand
Drug: glutamic acid
Target: Metabotropic glutamate receptor 1 (GPCR)
Gene: GRM1
UniProt: Q13255 (GRM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.6
Assay: Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
Drug: glutamic acid
Target: Glutamate dehydrogenase 1, mitochondrial (Enzyme)
Gene: GLUD1
UniProt: P00367 (DHE3_HUMAN)
Organism: Homo sapiens
Drug: glutamic acid
Target: Glutamate dehydrogenase 2, mitochondrial (Enzyme)
Gene: GLUD2
UniProt: P49448 (DHE4_HUMAN)
Organism: Homo sapiens
Drug: glutamic acid
Target: Glutamate receptor ionotropic, kainate 5 (Ion channel)
Gene: GRIK5
UniProt: Q16478 (GRIK5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.15
Assay: Displacement of [3H]kainate from human Ionotropic glutamate receptor ionotropic kainate 1 expressed in HEK293 cells
Drug: glutamic acid
Target: Metabotropic glutamate receptor 5 (GPCR)
Gene: GRM5
UniProt: P41594 (GRM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.41
Assay: Binding affinity to mGluR5 receptor expressed in BHK cells
Drug: glutamic acid
Target: Metabotropic glutamate receptor 4 (GPCR)
Gene: GRM4
UniProt: Q14833 (GRM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.85
Assay: Displacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cells
Drug: glutamic acid
Target: Glutamate receptor 4 (Ion channel)
Gene: GRIA4
UniProt: P48058 (GRIA4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.06
Assay: Compound was tested for binding affinity against human Ionotropic glutamate receptor AMPA 4 in HEK293 cells using [3H]AMPA as radioligand
Drug: glutamic acid
Target: Glutamate receptor ionotropic, kainate 2 (Ion channel)
Gene: GRIK2
UniProt: Q13002 (GRIK2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.96
Assay: Binding affinity against human GluR6
Drug: glutamic acid
Target: Glutamate receptor ionotropic, kainate 3 (Ion channel)
Gene: GRIK3
UniProt: Q13003 (GRIK3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.1
Assay: Ability to bind to Ionotropic glutamate receptor ionotropic kainate 3 was evaluated
Drug: glutamic acid
Target: Metabotropic glutamate receptor 7 (GPCR)
Gene: GRM7
UniProt: Q14831 (GRM7_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.93
Assay: Agonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP production
Drug: glutamic acid
Target: Metabotropic glutamate receptor 6 (GPCR)
Gene: GRM6
UniProt: O15303 (GRM6_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.31
Assay: Compound was tested for the inhibition of Metabotropic glutamate receptor 6
Drug: glutamic acid
Target: Metabotropic glutamate receptor 2 (GPCR)
Gene: GRM2
UniProt: Q14416 (GRM2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.54
Assay: Compound was tested for the inhibition of metabotropic glutamate receptor 2 (mGluR2).
Drug: glutamic acid
Target: Excitatory amino acid transporter 1 (Transporter)
Gene: SLC1A3
UniProt: P43003 (EAA1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.46
Assay: Inhibition of [3H]D-Asp uptake at EAAT1 in HEK293 cells
Drug: glutamic acid
Target: Excitatory amino acid transporter 2 (Transporter)
Gene: SLC1A2
UniProt: P43004 (EAA2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.21
Assay: Inhibition of [3H]D-Asp uptake at human EAAT2 in HEK293 cells
Drug: glutamic acid
Target: Excitatory amino acid transporter 3 (Transporter)
Gene: SLC1A1
UniProt: P43005 (EAA3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.29
Assay: Inhibition of [3H]D-Asp uptake at human EAAT3 in HEK293 cells
Drug: glutamic acid
Target: Glutamate receptor 2 (Ion channel)
Gene: Gria2
UniProt: P19491 (GRIA2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.55
Drug: glutamic acid
Target: Glutamate receptor 3 (Ion channel)
Gene: GRIA3
UniProt: P42263 (GRIA3_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.595
Drug: glutamic acid
Target: Glutamate receptor ionotropic, kainate 4 (Ion channel)
Gene: GRIK4
UniProt: Q16099 (GRIK4_HUMAN)
Organism: Homo sapiens
Activity: Ki  7.738
Drug: glutamic acid
Target: Metabotropic glutamate receptor 3 (GPCR)
Gene: GRM3
UniProt: Q14832 (GRM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.4
Action type: AGONIST
Drug: glutamic acid
Target: Metabotropic glutamate receptor 8 (GPCR)
Gene: GRM8
UniProt: O00222 (GRM8_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.7
Action type: AGONIST
Drug: glutamic acid
Target: Glutamate receptor ionotropic, NMDA 1 (Ion channel)
Gene: Grin1
UniProt: P35439 (NMDZ1_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 5.54
Drug: glutamic acid
Target: Glutamate receptor ionotropic, kainate 2 (Ion channel)
Gene: Grik2
UniProt: P42260 (GRIK2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.48
Drug: glutamic acid
Target: Glutamate receptor ionotropic, kainate 1 (Ion channel)
Gene: Grik1
UniProt: P22756 (GRIK1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.85
Drug: glutamic acid
Target: Metabotropic glutamate receptor 4 (GPCR)
Gene: Grm4
UniProt: P31423 (GRM4_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 4.92
Drug: glutamic acid
Target: Metabotropic glutamate receptor 6 (GPCR)
Gene: Grm6
UniProt: P35349 (GRM6_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 4.8
Drug: glutamic acid
Target: Glutamate receptor 1 (Ion channel)
Gene: Gria1
UniProt: P19490 (GRIA1_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 4.46
Drug: glutamic acid
Target: Glutamate receptor 3 (Ion channel)
Gene: Gria3
UniProt: P19492 (GRIA3_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 4
Drug: glutamic acid
Target: Glutamate receptor 4 (Ion channel)
Gene: Gria4
UniProt: P19493 (GRIA4_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 4.77
Drug: glutamic acid
Target: Glutamate receptor ionotropic, kainate 3 (Ion channel)
Gene: Grik3
UniProt: P42264 (GRIK3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.31
Drug: glutamic acid
Target: Glutamate racemase (Enzyme)
Gene: murI
UniProt: Q03469 (MURI_LACFE)
Organism: Lactobacillus fermentum
Activity: Ki = 4.55