AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: fentanyl
Target: Delta-type opioid receptor (GPCR)
Gene: Oprd1
UniProt: P32300 (OPRD_MOUSE)
Organism: Mus musculus
Activity: IC50 = 8.03
Assay: Inhibition of delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
Drug: fentanyl
Target: Delta-type opioid receptor (GPCR)
Gene: Oprd1
UniProt: P33533 (OPRD_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.4
Assay: Binding affinity of compound evaluated for Opioid receptor delta 1 isolated from rat brain
Drug: fentanyl
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41144 (OPRK_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 6.71
Assay: Binding affinity towards Opioid receptor kappa 1 using [3H]U-69593 as radioligand.
Drug: fentanyl
Target: Histamine H1 receptor (GPCR)
Gene: Hrh1
UniProt: P31390 (HRH1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.7
Assay: Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug: fentanyl
Target: Sigma non-opioid intracellular receptor 1 (Membrane other)
Gene: SIGMAR1
UniProt: Q60492 (SGMR1_CAVPO)
Organism: Cavia porcellus
Activity: IC50 = 5.3
Assay: Displacement of [3H]pentazocine from LAL/HA/BR guinea pig brain sigma1 receptor incubated for 90 mins by liquid scintillation counting method
Drug: fentanyl
Target: Opioid receptor (GPCR)
Gene: Oprd1|Oprm1|Oprk1|Sigmar1
UniProt: P33533|P33535|P34975|Q9R0C9 (OPRD_RAT|OPRM_RAT|OPRK_RAT|SGMR1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.67
Assay: In vitro affinity to displace [3H]naloxone from opiate receptor in freshly prepared rat brain homogenates
Drug: fentanyl
Target: Monoamine oxidase (Enzyme)
Gene: MAOA|MAOB
UniProt: P21397|P27338 (AOFA_HUMAN|AOFB_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.26
Assay: Displacement of [3H]2-BFI (1 nM) from imidazoline receptor I-2 in human brain
Drug: fentanyl
Target: Sigma non-opioid intracellular receptor 1 (Unclassified)
Gene: SIGMAR1
UniProt: Q60492 (SGMR1_CAVPO)
Organism: Cavia porcellus
Activity: IC50 = 5.3
Assay: Displacement of [3H]pentazocine from LAL/HA/BR guinea pig brain sigma1 receptor incubated for 90 mins by liquid scintillation counting method
Drug: fentanyl
Target: Sigma non-opioid intracellular receptor 1 (Unclassified)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.45
Assay: Displacement of [3H]PPP from sigma1 receptor (unknown origin)
Drug: fentiazac
Target: Prostaglandin D2 receptor 2 (GPCR)
Gene: PTGDR2
UniProt: Q9Y5Y4 (PD2R2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.26
Assay: Displacement of[3H]PGD2 from human CRTH2 receptor expressed in HEK385-7 cells
Drug: fexofenadine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.67
Assay: Inhibition of human ERG in MCF7 cells
Drug: fexofenadine
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: Km = 5.699
Drug: fexofenadine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8
Action type: ANTAGONIST
Drug: fexofenadine
Target: Solute carrier organic anion transporter family member 1A2 (Transporter)
Gene: SLCO1A2
UniProt: P46721 (SO1A2_HUMAN)
Organism: Homo sapiens
Activity: Km = 5.699
Drug: finasteride
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.699
Assay: DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: finasteride
Target: Cytochrome P450 2C19 (Enzyme)
Gene: CYP2C19
UniProt: P33261 (CP2CJ_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Assay: DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: finasteride
Target: 3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1 (Enzyme)
Gene: HSD3B1
UniProt: P14060 (3BHS1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.96
Assay: Binding affinity for 3-beta-hydroxysteroid dehydrogenase
Drug: finasteride
Target: 3-oxo-5-alpha-steroid 4-dehydrogenase 1 (Enzyme)
Gene: Srd5a1
UniProt: P24008 (S5A1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.17
Assay: Inhibition of recombinant Steroid 5-alpha-reductase type I was evaluated as binding affinity (in vitro)
Drug: finasteride
Target: 3-oxo-5-alpha-steroid 4-dehydrogenase 2 (Enzyme)
Gene: Srd5a2
UniProt: P31214 (S5A2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 9.55
Assay: Inhibitory activity was measured on rat Steroid 5-alpha-reductase type 2
Drug: finasteride
Target: Steroid 5-alpha-reductase (Enzyme)
Gene: Srd5a1|Srd5a2
UniProt: P24008|P31214 (S5A1_RAT|S5A2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.26
Assay: Ability to inhibit Steroid 5-alpha-reductase in rat using Enzyme kinetics method.
Drug: finasteride
Target: 3-oxo-5-alpha-steroid 4-dehydrogenase 2 (Enzyme)
Gene: SRD5A2
UniProt: P31213 (S5A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.26
Action type: INHIBITOR
Drug: finasteride
Target: 3-oxo-5-alpha-steroid 4-dehydrogenase 1 (Enzyme)
Gene: SRD5A1
UniProt: P18405 (S5A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.58
Action type: INHIBITOR
Drug: flavoxate
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.704
Assay: DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole)
Drug: flavoxate
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
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2093863; PROTEIN FAMILY
Drug: flavoxate
Target: Phosphodiesterase 7 (Enzyme)
Gene: PDE7A|PDE7B
UniProt: Q13946|Q9NP56 (PDE7A_HUMAN|PDE7B_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2111411; PROTEIN FAMILY
Drug: flavoxate
Target: Phosphodiesterase 8 (Enzyme)
Gene: PDE8A|PDE8B
UniProt: O60658|O95263 (PDE8A_HUMAN|PDE8B_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2363067; PROTEIN FAMILY
Drug: flecainide
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.19
Action type: BLOCKER
Assay: Inhibition of human heart sodium channel Nav1.5 by patch-clamp method
Drug: flecainide
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.41
Assay: Inhibition of human Potassium channel HERG expressed in mammalian cells
Drug: flecainide
Target: Sodium channel protein type 4 subunit alpha (Ion channel)
Gene: SCN4A
UniProt: P35499 (SCN4A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.745
Drug: flecainide
Target: Potassium voltage-gated channel subfamily A member 5 (Ion channel)
Gene: KCNA5
UniProt: P22460 (KCNA5_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4
Action type: BLOCKER
Drug: flecainide
Target: Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 (Ion channel)
Gene: HCN4
UniProt: Q9Y3Q4 (HCN4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 2.77
Drug: flecainide
Target: Potassium voltage-gated channel subfamily A member 7 (Ion channel)
Gene: KCNA7
UniProt: Q96RP8 (KCNA7_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.1
Action type: BLOCKER
Drug: flecainide
Target: Potassium voltage-gated channel subfamily D member 2 (Ion channel)
Gene: Kcnd2
UniProt: Q63881 (KCND2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5
Assay: Inhibition of rat potassium channel Kv4.2 by patch-clamp method
Drug: flecainide
Target: Potassium voltage-gated channel subfamily C member 1 (Ion channel)
Gene: Kcnc1
UniProt: P15388 (KCNC1_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4
Action type: BLOCKER
Drug: fleroxacin
Target: DNA gyrase subunit A (Enzyme)
Gene: gyrA
UniProt: P0AES4 (GYRA_ECOLI)
Organism: Escherichia coli (strain K12)
Activity: IC50 = 4.79
Drug: floctafenine
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.959
Action type: INHIBITOR
Drug: floctafenine
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.268
Action type: INHIBITOR
Drug: flopropione
Target: Catechol O-methyltransferase (Enzyme)
Gene: COMT
UniProt: P21964 (COMT_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action
Drug: floxacillin
Target: Penicillin-binding protein 1A (Enzyme)
Gene: pbpA
UniProt: Q8XJ01 (PBPA_CLOPE)
Organism: Clostridium perfringens (strain 13 / Type A)
Drug: floxacillin
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.25
Drug: floxacillin
Target: Matrix metalloproteinase-9 (Enzyme)
Gene: MMP9
UniProt: P14780 (MMP9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.19
Drug: floxuridine
Target: Thymidylate synthase (Enzyme)
Gene: TYMS
UniProt: P04818 (TYSY_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Drug: floxuridine
Target: Thymidylate synthase (Enzyme)
Gene: Tyms
UniProt: P07607 (TYSY_MOUSE)
Organism: Mus musculus
Activity: IC50 = 9.4
Assay: Inhibition of thymidylate synthase in mouse L1210 cells assessed as inhibition of tritium release from [5-3H]deoxyuridine after preincubation for 4 hrs by liquid scintillation counting
Drug: fluconazole
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.1
Drug: fluconazole
Target: Lanosterol 14-alpha demethylase (Enzyme)
Gene: ERG11
UniProt: P10613 (CP51_CANAL)
Organism: Candida albicans (strain SC5314 / ATCC MYA-2876)
Activity: IC50 = 6.699
Action type: INHIBITOR
Drug: fluconazole
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.54
Drug: fluconazole
Target: Cytochrome P450 2C19 (Enzyme)
Gene: CYP2C19
UniProt: P33261 (CP2CJ_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.09
Drug: fluconazole
Target: Lanosterol 14-alpha demethylase (Enzyme)
Gene: CYP51A1
UniProt: Q16850 (CP51A_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.4
Assay: Binding affinity to human His-tagged CYP51 expressed in Escherichia coli
Drug: fluconazole
Target: Lanosterol 14-alpha demethylase (Enzyme)
Gene: cyp51
UniProt: P9WPP9 (CP51_MYCTU)
Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv)
Activity: Kd = 6.7
Assay: Binding affinity to Mycobacterium tuberculosis CYP51
Drug: fluconazole
Target: 14-alpha sterol demethylase Cyp51A (Enzyme)
UniProt: Q4WNT5 (Q4WNT5_ASPFU)
Organism: Neosartorya fumigata (strain ATCC MYA-4609 / Af293 / CBS 101355 / FGSC A1100)
Activity: Kd = 4.92
Assay: Binding affinity to Aspergillus fumigatus AF293 sterol 14-alpha demethylase isoenzyme A expressed in Escherichia coli
Drug: fluconazole
Target: 14-alpha sterol demethylase (Enzyme)
Gene: cyp51B
UniProt: Q96W81 (Q96W81_ASPFM)
Organism: Neosartorya fumigata
Activity: Kd = 5.39
Assay: Binding affinity to Aspergillus fumigatus AF293 sterol 14-alpha demethylase isoenzyme B expressed in Escherichia coli
Drug: fluconazole
Target: Mycocyclosin synthase (Enzyme)
Gene: cyp121
UniProt: P9WPP7 (CP121_MYCTU)
Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv)
Activity: Kd = 5.22
Assay: Binding affinity to Mycobacterium tuberculosis CYP121
Drug: fluconazole
Target: Sterol 14-alpha demethylase (Enzyme)
Gene: CYP51
UniProt: Q7Z1V1 (CP51_TRYCC)
Organism: Trypanosoma cruzi (strain CL Brener)
Activity: IC50 = 6.06
Assay: Inhibition of recombinant Trypanosoma cruzi Tulahuen CYP51 expressed in Escherichia coli JM109 cell membranes assessed as inhibition of microbe growth by fluorescence based analysis
Drug: flucytosine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.1
Drug: flucytosine
Target: Thymidylate synthase (Enzyme)
Gene: TMP1
UniProt: P0CS13 (TYSY_CRYNB)
Organism: Cryptococcus neoformans var. neoformans serotype D (strain B-3501A)
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL4665; SINGLE PROTEIN
Drug: flucytosine
Target: Thymidylate synthase (Enzyme)
Gene: TMP1
UniProt: P12461 (TYSY_CANAL)
Organism: Candida albicans (strain SC5314 / ATCC MYA-2876)
Action type: INHIBITOR
Drug: flucytosine
Target: ATP-dependent molecular chaperone HSP82 (Cytosolic other)
Gene: HSP82
UniProt: P02829 (HSP82_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: EC50 = 6.15
Drug: fludarabine phosphate
Target: Ribonucleoside-diphosphate reductase large subunit (Enzyme)
Gene: RRM1
UniProt: P23921 (RIR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Action type: INHIBITOR
Assay: Inhibition of ADP reduction by ribonucleotide reductase from HeLa cells
Drug: fludarabine phosphate
Target: Ribonucleoside-diphosphate reductase subunit M2 (Enzyme)
Gene: RRM2
UniProt: P31350 (RIR2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Action type: INHIBITOR
Assay: Inhibition of ADP reduction by ribonucleotide reductase from HeLa cells
Drug: fludarabine phosphate
Target: Carbonic anhydrase 5A, mitochondrial (Enzyme)
Gene: CA5A
UniProt: P35218 (CAH5A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.88
Assay: Inhibition of recombinant human carbonic anhydrase VA preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydration assay
Drug: fludarabine phosphate
Target: Adenosine receptor A1 (GPCR)
Gene: Adora1
UniProt: P25099 (AA1R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.23
Assay: Binding affinity to adenosine A1 receptor in rat brain membranes by measuring displacement of specific [3H]PIA as radioligand.
Drug: fludarabine phosphate
Target: Adenosine receptor A2a (GPCR)
Gene: Adora2a
UniProt: P30543 (AA2AR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.55
Assay: Binding affinity to adenosine A2A receptor in rat striatal membranes by measuring displacement of specific [3H]-CGS- 21680 as radioligand
Drug: fludarabine phosphate
Target: Adenosine receptor A3 (GPCR)
Gene: Adora3
UniProt: P28647 (AA3R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.98
Assay: Binding affinity determined by displacement of specific binding of [125I]N-(4-amino-3-iodophenethyl)-adenosine in membranes of CHO cells stably transfected with the rat adenosine A3 receptor
Drug: fludarabine phosphate
Target: DNA polymerase alpha catalytic subunit (Enzyme)
Gene: POLA1
UniProt: P09884 (DPOLA_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Drug: fludrocortisone acetate
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.2
Drug: fludrocortisone acetate
Target: Annexin A1 (Cytosolic other)
Gene: ANXA1
UniProt: P04083 (ANXA1_HUMAN)
Organism: Homo sapiens
Drug: fludrocortisone acetate
Target: Mineralocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C2
UniProt: P08235 (MCR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.92
Action type: AGONIST
Drug: flufenamic acid
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.93
Action type: INHIBITOR
Drug: flufenamic acid
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.52
Action type: INHIBITOR
Drug: flufenamic acid
Target: Transthyretin (Secreted)
Gene: TTR
UniProt: P02766 (TTHY_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.25
Drug: flufenamic acid
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.12
Drug: flufenamic acid
Target: Aldose reductase (Enzyme)
Gene: AKR1B1
UniProt: P15121 (ALDR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4
Assay: In vitro inhibition of rabbit lens aldose reductase.
Drug: flufenamic acid
Target: Aldo-keto reductase family 1 member C1 (Enzyme)
Gene: AKR1C1
UniProt: Q04828 (AK1C1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.22
Drug: flufenamic acid
Target: Aldo-keto reductase family 1 member C2 (Enzyme)
Gene: AKR1C2
UniProt: P52895 (AK1C2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Drug: flufenamic acid
Target: Aldo-keto reductase family 1 member C3 (Enzyme)
Gene: AKR1C3
UniProt: P42330 (AK1C3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.1
Drug: flufenamic acid
Target: Potassium channel subfamily K member 2 (Ion channel)
Gene: KCNK2
UniProt: O95069 (KCNK2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4
Assay: Activation of TREK1 (unknown origin) expressed in COS7 cells assessed as increase in whole cell currents at +50 mV relative to control
Drug: flufenamic acid
Target: Myeloperoxidase (Enzyme)
Gene: MPO
UniProt: P05164 (PERM_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.74
Assay: Inhibition of chlorinating activity of recombinant myeloperoxidase by taurine assay
Drug: flufenamic acid
Target: Potassium channel subfamily T member 2 (Ion channel)
Gene: KCNT2
UniProt: Q6UVM3 (KCNT2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.85
Action type: ACTIVATOR
Drug: flufenamic acid
Target: Transient receptor potential cation channel subfamily A member 1 (Ion channel)
Gene: TRPA1
UniProt: O75762 (TRPA1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.16
Assay: Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay
Drug: flufenamic acid
Target: Transient receptor potential cation channel subfamily M member 2 (Ion channel)
Gene: TRPM2
UniProt: O94759 (TRPM2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.15
Assay: Inhibition of human recombinant TRPM2
Drug: flufenamic acid
Target: Transient receptor potential cation channel subfamily M member 4 (Ion channel)
Gene: TRPM4
UniProt: Q8TD43 (TRPM4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.55
Assay: GRAC: human TRPM4 blocker
Drug: flufenamic acid
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P05979 (PGH1_SHEEP)
Organism: Ovis aries
Activity: IC50 = 4.85
Assay: Inhibition of ovine COX1 assessed as reduction in PGF2alpha production by ELISA
Drug: flufenamic acid
Target: Aldo-keto reductase family 1 member B10 (Enzyme)
Gene: AKR1B10
UniProt: O60218 (AK1BA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.12
Drug: flufenamic acid
Target: Transient receptor potential cation channel subfamily M member 5 (Ion channel)
Gene: TRPM5
UniProt: Q9NZQ8 (TRPM5_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.62
Drug: flufenamic acid
Target: Transient receptor potential cation channel subfamily M member 4 (Ion channel)
Gene: Trpm4
UniProt: Q7TN37 (TRPM4_MOUSE)
Organism: Mus musculus
Activity: IC50 = 5.6
Action type: GATING INHIBITOR
Drug: flufenamic acid
Target: Transcriptional enhancer factor TEF-3 (Transcription factor)
Gene: TEAD4
UniProt: Q15561 (TEAD4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.27
Assay: Inhibition of N-terminal His6-tagged human TEAD4 YAP binding domain (217 to 434 residues) expressed in Escherichia coli C43 (DE3) cells assessed reduction in autopalmitoylation preincubated for 2 hrs followed by palmitoyl alkyne coenzyme A addition and measured after 30 mins by immunoblot analysis
Drug: flufenamic acid
Target: Nicotinate phosphoribosyltransferase (Enzyme)
Gene: NAPRT
UniProt: Q6XQN6 (PNCB_HUMAN)
Organism: Homo sapiens
Activity: Ki = 11
Assay: Inhibition of NAPRT (unknown origin)
Drug: flufenamic acid
Target: Taste receptor type 2 member 14 (GPCR)
Gene: TAS2R14
UniProt: Q9NYV8 (T2R14_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.863
Action type: AGONIST
Assay: calcium imaging in ransfected human embryonic kidney (HEK)-293T
Drug: fluindione
Target: Arachidonate 5-lipoxygenase (Enzyme)
Gene: Alox5
UniProt: P12527 (LOX5_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.02
Assay: In vitro inhibition of 5-lipoxygenase activity in RBL-1 cells.
Drug: flumazenil
Target: Gamma-aminobutyric acid receptor subunit alpha-1 (Ion channel)
Gene: GABRA1
UniProt: P14867 (GBRA1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.7
Assay: Binding affinity to GABAA alpha-1-beta-2-gamma-2 receptor
Drug: flumazenil
Target: Gamma-aminobutyric acid receptor subunit alpha-2 (Ion channel)
Gene: GABRA2
UniProt: P47869 (GBRA2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.24
Assay: Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-2-beta-2-gamma-2 receptor expressed in HEK293T cells
Drug: flumazenil
Target: Gamma-aminobutyric acid receptor subunit alpha-3 (Ion channel)
Gene: GABRA3
UniProt: P34903 (GBRA3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.09
Assay: Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-3-beta-2-gamma-2 receptor expressed in HEK293T cells
Drug: flumazenil
Target: Gamma-aminobutyric acid receptor subunit alpha-5 (Ion channel)
Gene: GABRA5
UniProt: P31644 (GBRA5_HUMAN)
Organism: Homo sapiens
Activity: Kd = 9.3
Assay: Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptor
Drug: flumazenil
Target: Gamma-aminobutyric acid receptor subunit alpha-4 (Ion channel)
Gene: GABRA4
UniProt: P48169 (GBRA4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.7
Action type: ALLOSTERIC ANTAGONIST
Assay: Displacement of [3H]Ro-154513 from benzodiazepine binding site of GABAA alpha-4-beta-2-gamma-2 receptor expressed in HEK293T cells
Drug: flumazenil
Target: GABA-A receptor alpha-2/beta-3/gamma-2 (Ion channel)
Gene: GABRG2|GABRB3|GABRA2
UniProt: P18507|P28472|P47869 (GBRG2_HUMAN|GBRB3_HUMAN|GBRA2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.046
Action type: ALLOSTERIC ANTAGONIST
Drug: flumazenil
Target: GABA-A receptor alpha-3/beta-3/gamma-2 (Ion channel)
Gene: GABRG2|GABRB3|GABRA3
UniProt: P18507|P28472|P34903 (GBRG2_HUMAN|GBRB3_HUMAN|GBRA3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.979
Action type: ALLOSTERIC ANTAGONIST
Drug: flumazenil
Target: GABA-A receptor alpha-5/beta-3/gamma-2 (Ion channel)
Gene: GABRG2|GABRB3|GABRA5
UniProt: P18507|P28472|P31644 (GBRG2_HUMAN|GBRB3_HUMAN|GBRA5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.222
Action type: ALLOSTERIC ANTAGONIST
Drug: flumazenil
Target: GABA-A receptor alpha-1/beta-3/gamma-2 (Ion channel)
Gene: GABRA1|GABRG2|GABRB3
UniProt: P14867|P18507|P28472 (GBRA1_HUMAN|GBRG2_HUMAN|GBRB3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.097
Action type: ALLOSTERIC ANTAGONIST
Drug: flumazenil
Target: GABA-A receptor; anion channel (Ion channel)
Gene: Gabrp|Gabrb1|Gabrd|Gabrg2|Gabra5|Gabra3|Gabrg1|Gabra2|Gabra4|Gabrg3|Gabra6|Gabra1|Gabrb3|Gabrb2|Gabrq|Gabre
UniProt: O09028|P15431|P18506|P18508|P19969|P20236|P23574|P23576|P28471|P28473|P30191|P62813|P63079|P63138|Q91ZM7|Q9ES14 (GBRP_RAT|GBRB1_RAT|GBRD_RAT|GBRG2_RAT|GBRA5_RAT|GBRA3_RAT|GBRG1_RAT|GBRA2_RAT|GBRA4_RAT|GBRG3_RAT|GBRA6_RAT|GBRA1_RAT|GBRB3_RAT|GBRB2_RAT|Q91ZM7_RAT|GBRE_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.1
Assay: Binding affinity against Diazepam sensitive (DS) Gamma-aminobutyric acid A receptor in rat cerebellum.
Drug: flumazenil
Target: GABA-A receptor; anion channel (Ion channel)
Gene: GABRA1|GABRB1|GABRA2|GABRA3|GABRA4|GABRG2
UniProt: P08219|P08220|P10063|P10064|P20237|P22300 (GBRA1_BOVIN|GBRB1_BOVIN|GBRA2_BOVIN|GBRA3_BOVIN|GBRA4_BOVIN|GBRG2_BOVIN)
Organism: Bos taurus
Activity: Ki = 10.05
Assay: Displacement of [3H]- Ro.15-1788 from GABA-A central Benzodiazepine receptor (BzR) of Bovine cerebral cortex membrane
Drug: flumazenil
Target: GABA A receptor alpha-3/beta-2/gamma-2 (Ion channel)
Gene: Gabrg2|Gabra3|Gabrb2
UniProt: P18508|P20236|P63138 (GBRG2_RAT|GBRA3_RAT|GBRB2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.22
Assay: Binding affinity for rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells
Drug: flumazenil
Target: GABA A receptor alpha-6/beta-2/gamma-2 (Ion channel)
Gene: Gabrg2|Gabra6|Gabrb2
UniProt: P18508|P30191|P63138 (GBRG2_RAT|GBRA6_RAT|GBRB2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.82
Assay: Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr,gly)beta2gamma2 subunits expressed in HEK293 cells