AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: nadolol
Target: Beta-3 adrenergic receptor (GPCR)
Gene: ADRB3
UniProt: P13945 (ADRB3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.3
Action type: ANTAGONIST
Drug: nafamostat
Target: Plasminogen (Enzyme)
Gene: PLG
UniProt: P00747 (PLMN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.62
Assay: Compound was evaluated for inhibitory activity against plasmin.
Drug: nafamostat
Target: Prothrombin (Enzyme)
Gene: F2
UniProt: P00734 (THRB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.54
Assay: Compound was evaluated for inhibitory activity against Thrombin.
Drug: nafamostat
Target: Trypsin-1 (Enzyme)
Gene: PRSS1
UniProt: P07477 (TRY1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.77
Action type: INHIBITOR
Assay: In vitro for inhibition of purified bovine trypsin.
Drug: nafamostat
Target: Kallikrein-1 (Enzyme)
Gene: KLK1
UniProt: P06870 (KLK1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.19
Assay: Compound was evaluated for inhibitory activity against Kallikrein.
Drug: nafamostat
Target: Coagulation factor X (Enzyme)
Gene: F10
UniProt: P00742 (FA10_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.68
Assay: Inhibitory concentration against Coagulation factor X
Drug: nafamostat
Target: Suppressor of tumorigenicity 14 protein (Enzyme)
Gene: ST14
UniProt: Q9Y5Y6 (ST14_HUMAN)
Organism: Homo sapiens
Activity: Ki = 10.7
Drug: nafamostat
Target: Complement C1r subcomponent (Enzyme)
Gene: C1R
UniProt: P00736 (C1R_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Action type: INHIBITOR
Assay: Inhibition of C1r serine protease
Drug: nafamostat
Target: Complement C1s subcomponent (Enzyme)
Gene: C1S
UniProt: P09871 (C1S_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.85
Assay: Compound was evaluated for inhibitory activity against C1s serine protease.
Drug: nafamostat
Target: Acid-sensing ion channel 2 (Ion channel)
Gene: ASIC2
UniProt: Q16515 (ASIC2_HUMAN)
Organism: Homo sapiens
Activity: IC50 ~ 4.2
Action type: BLOCKER
Drug: nafamostat
Target: Acid-sensing ion channel 1 (Ion channel)
Gene: ASIC1
UniProt: P78348 (ASIC1_HUMAN)
Organism: Homo sapiens
Activity: IC50 ~ 4.9
Action type: BLOCKER
Drug: nafamostat
Target: Cationic trypsin (Enzyme)
UniProt: P00760 (TRY1_BOVIN)
Organism: Bos taurus
Activity: IC50 = 7.77
Assay: The compound was evaluated to inhibit trypsin and is expressed in IC50 (The concentration required to inhibit 50% of the enzyme).
Drug: nafamostat
Target: Acid-sensing ion channel 3 (Ion channel)
Gene: ASIC3
UniProt: Q9UHC3 (ASIC3_HUMAN)
Organism: Homo sapiens
Activity: IC50 ~ 5.6
Action type: BLOCKER
Drug: nafamostat
Target: Tryptase alpha/beta-1 (Enzyme)
Gene: TPSAB1
UniProt: Q15661 (TRYB1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 10
Action type: INHIBITOR
Drug: nafamostat
Target: Serine protease hepsin (Enzyme)
Gene: HPN
UniProt: P05981 (HEPS_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.28
Drug: nafamostat
Target: Hepatocyte growth factor activator (Enzyme)
Gene: HGFAC
UniProt: Q04756 (HGFA_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.6
Drug: nafamostat
Target: Transmembrane protease serine 2 (Enzyme)
Gene: TMPRSS2
UniProt: O15393 (TMPS2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7
Action type: INHIBITOR
Assay: Inhibition of TMPRSS2-dependent MERS-S-mediated membrane fusion in an in vitro reporter assay.
Drug: nafarelin
Target: Gonadotropin-releasing hormone receptor (GPCR)
Gene: GNRHR
UniProt: P30968 (GNRHR_HUMAN)
Organism: Homo sapiens
Activity: Kd = 9.699
Action type: AGONIST
Drug: nafcillin
Target: Penicillin-binding protein 1A (Enzyme)
Gene: pbpA
UniProt: Q8XJ01 (PBPA_CLOPE)
Organism: Clostridium perfringens (strain 13 / Type A)
Drug: nafcillin
Target: Penicillin-binding protein (Enzyme)
Gene: pbp4|mecA|pbpA|PBP2|pbpF
UniProt: P72355|Q53707|Q53725|Q53729|Q9XDB3 (P72355_STAAU|Q53707_STAAU|Q53725_STAAU|Q53729_STAAU|Q9XDB3_STAAU)
Organism: Staphylococcus aureus
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2362972; PROTEIN FAMILY
Drug: naftidrofuryl
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.82
Assay: Displacement of [3H]ketanserin from 5HT2A receptor expressed in HEK293 cells by liquid scintillation spectrophotometry
Drug: naftifine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.06
Assay: Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand
Drug: naftifine
Target: 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase (Enzyme)
Gene: EBP
UniProt: Q15125 (EBP_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.82
Assay: Affinity for human EMP expressed in ERG2 deficient strain of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine as radioligand
Drug: naftifine
Target: Squalene monooxygenase (Enzyme)
Gene: SQLE
UniProt: Q14534 (ERG1_HUMAN)
Organism: Homo sapiens
Drug: naftifine
Target: Squalene epoxidase (Enzyme)
UniProt: Q4JEY0 (Q4JEY0_TRIRU)
Organism: Trichophyton rubrum
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2364679; SINGLE PROTEIN
Drug: naftifine
Target: C-8 sterol isomerase (Enzyme)
Gene: ERG2
UniProt: P32352 (ERG2_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: Ki = 6.51
Assay: Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand
Drug: naftifine
Target: Dehydrosqualene desaturase (Enzyme)
Gene: crtN
UniProt: O07855 (CRTN_STAAE)
Organism: Staphylococcus aureus (strain Newman)
Activity: IC50 = 6.53
Assay: Inhibition of diapophytoene desaturase in Staphylococcus aureus Newman assessed as reduction in staphyloxanthin pigment formation
Drug: naftopidil
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P54833 (ADRB2_CANFA)
Organism: Canis familiaris
Activity: Ki = 6
Assay: Beta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lung
Drug: naftopidil
Target: Adrenergic receptor alpha-2 (GPCR)
Gene: Adra2b|Adra2c|Adra2a
UniProt: P19328|P22086|P22909 (ADA2B_RAT|ADA2C_RAT|ADA2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.8
Assay: Alpha-2 adrenergic receptor binding affinity by measuring the displacement of [3H]clonidine binding in rat cerebral cortex
Drug: naftopidil
Target: Adrenergic receptor alpha-1 (GPCR)
Gene: Adra1b|Adra1d|Adra1a
UniProt: P15823|P23944|P43140 (ADA1B_RAT|ADA1D_RAT|ADA1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.41
Assay: Alpha-1 adrenergic receptor binding affinity by measuring the displacement of [3H]prazosin binding in rat brain
Drug: naftopidil
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.432
Action type: ANTAGONIST
Drug: naftopidil
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.921
Action type: ANTAGONIST
Drug: naftopidil
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.699
Action type: ANTAGONIST
Drug: nalbuphine
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.8
Action type: AGONIST
Drug: nalbuphine
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8
Action type: AGONIST
Drug: nalbuphine
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6
Action type: AGONIST
Drug: nalbuphine
Target: Kappa-type opioid receptor (GPCR)
Gene: Oprk1
UniProt: P33534 (OPRK_MOUSE)
Organism: Mus musculus
Activity: IC50 = 7.4
Action type: AGONIST
Drug: nalidixic acid
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.1
Drug: nalidixic acid
Target: DNA gyrase (Enzyme)
Gene: gyrA|gyrB
UniProt: P0AES4|P0AES6 (GYRA_ECOLI|GYRB_ECOLI)
Organism: Escherichia coli (strain K12)
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2311224; PROTEIN COMPLEX
Drug: nalmefene
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Kd = 9.53
Action type: ANTAGONIST
Assay: Activity at human mu opioid receptor by [35S]GTPgammaS binding assay
Drug: nalmefene
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.92
Action type: ANTAGONIST
Assay: Displacement of [3H]U69593 form human kappa opioid receptor expressed in CHO cells
Drug: nalmefene
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: Kd = 9.04
Action type: ANTAGONIST
Assay: Activity at human delta opioid receptor by [35S]GTPgammaS binding assay
Drug: nalmefene
Target: Mu-type opioid receptor (GPCR)
Gene: Oprm1
UniProt: P33535 (OPRM_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.54
Assay: Binding affinity towards mu-opioid receptor by the displacement of [3H]Nal in rat brain homogenates
Drug: nalmefene
Target: Delta-type opioid receptor (GPCR)
Gene: Oprd1
UniProt: P33533 (OPRD_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.47
Assay: Binding affinity towards delta-opioid receptor by displacement of [3H]DADL in rat brain homogenates
Drug: nalmefene
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41144 (OPRK_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 8.7
Assay: Binding affinity towards kappa opioid receptor by displacement of [3H]EKC in guinea pig cortical tissue
Drug: nalorphine
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.72
Assay: Displacement of [3H]DAMGO form human mu opioid receptor expressed in CHO cells
Drug: nalorphine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.32
Assay: Inhibition of specific binding of [3H]NANM of sigma receptor in Guinea pig brain membranes
Drug: nalorphine
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.42
Assay: Displacement of [3H]U69593 form human kappa opioid receptor expressed in CHO cells
Drug: nalorphine
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.92
Assay: Displacement of [3H]Naltrindole form human delta opioid receptor expressed in CHO cells
Drug: nalorphine
Target: Mu-type opioid receptor (GPCR)
Gene: Oprm1
UniProt: P33535 (OPRM_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.7
Assay: Compound administered subcutaneously was evaluated for inhibition constant measured as the displacement of [3H]DAGO from rat brain
Drug: nalorphine
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41144 (OPRK_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 7.82
Assay: Binding affinity to Opioid receptor kappa 1 in guinea pig cortex using [3H]EKC as radioligand
Drug: nalorphine
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: EC50 = 8.82
Assay: Binding affinity to rat brain opioid receptor
Drug: nalorphine
Target: Opioid receptor (GPCR)
Gene: Sigmar1|Oprd1|Oprk1|Oprm1
UniProt: O55242|P32300|P33534|P42866 (SGMR1_MOUSE|OPRD_MOUSE|OPRK_MOUSE|OPRM_MOUSE)
Organism: Mus musculus
Activity: IC50 = 7.23
Assay: Concentration required to inhibit the stereospecific [3H]diprenorphine binding Opioid receptors in the absence of sodium(Na+) was determined in mouse isolated vas deferens
Drug: naloxone
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.81
Action type: ANTAGONIST
Drug: naloxone
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.699
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: naloxone
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.8
Assay: Inhibitory concentration against human Adenosine A3 receptor expressed in HEK293 cells using 0.1 nM [3H]AB-MECA
Drug: naloxone
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.5
Action type: ANTAGONIST
Drug: naloxone
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.27
Action type: ANTAGONIST
Drug: naloxone
Target: Mu-type opioid receptor (GPCR)
Gene: Oprm1
UniProt: P33535 (OPRM_RAT)
Organism: Rattus norvegicus
Activity: Kd = 9.4
Assay: Opioid receptor mu 1 affinity against the receptor site model site 1 (mu1)
Drug: naloxone
Target: Mu-type opioid receptor (GPCR)
Gene: Oprm1
UniProt: P42866 (OPRM_MOUSE)
Organism: Mus musculus
Activity: Ki = 9
Action type: ANTAGONIST
Drug: naloxone
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P97266 (OPRM_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 9.17
Assay: Affinity to mu-receptor, using [3H]DAMGO as radioligand in homogenates of guinea pig brain membranes
Drug: naloxone
Target: Delta-type opioid receptor (GPCR)
Gene: Oprd1
UniProt: P32300 (OPRD_MOUSE)
Organism: Mus musculus
Activity: Kd = 7.3
Assay: Tested for inhibitory activity against (DPDE)delta receptor in mouse vas deferens
Drug: naloxone
Target: Delta-type opioid receptor (GPCR)
Gene: Oprd1
UniProt: P33533 (OPRD_RAT)
Organism: Rattus norvegicus
Activity: Kd = 7.74
Assay: Affinity against the Opioid receptor delta 1
Drug: naloxone
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41144 (OPRK_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 8.5
Assay: Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig brain membrane
Drug: naloxone
Target: Kappa-type opioid receptor (GPCR)
Gene: Oprk1
UniProt: P34975 (OPRK_RAT)
Organism: Rattus norvegicus
Activity: Kd = 9
Assay: Compound was evaluated for Opioid receptor kappa 1 affinity against the receptor site model site 4(kappa)
Drug: naloxone
Target: Kappa-type opioid receptor (GPCR)
Gene: Oprk1
UniProt: P33534 (OPRK_MOUSE)
Organism: Mus musculus
Activity: IC50 = 8.3
Action type: ANTAGONIST
Drug: naloxone
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P79350 (OPRM_BOVIN)
Organism: Bos taurus
Activity: IC50 = 8.3
Assay: Inhibition of 0.5 nM [3H]- Bremazocine binding to Opioid receptor mu 1 of bovine striatum membrane
Drug: naloxone
Target: C-C chemokine receptor type 5 (GPCR)
Gene: Ccr5
UniProt: P51682 (CCR5_MOUSE)
Organism: Mus musculus
Activity: Kd = 7.98
Assay: Binding affinity to CCR5 in NY1DD transgenic mouse brain membrane
Drug: naloxone
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: Kd = 9
Assay: Displacement of [3H]-(-)-naloxone from opiate receptor in rat brain membrane
Drug: nandrolone
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Drug: nandrolone
Target: Corticosteroid-binding globulin (Secreted)
Gene: SERPINA6
UniProt: P08185 (CBG_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.14
Drug: nandrolone
Target: Sex hormone-binding globulin (Secreted)
Gene: SHBG
UniProt: P04278 (SHBG_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.3
Assay: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin
Drug: nandrolone
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.45
Assay: Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Drug: nandrolone
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.678
Assay: DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
Drug: nandrolone
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: Ki = 7.65
Assay: DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
Drug: nandrolone decanoate
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action; CHEMBL1871; SINGLE PROTEIN
Drug: nandrolone decanoate
Target: Corticosteroid-binding globulin (Secreted)
Gene: SERPINA6
UniProt: P08185 (CBG_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.14
Assay: Binding affinity to human CBG receptor (corticosteroid-binding globulins)
Drug: nandrolone decanoate
Target: Sex hormone-binding globulin (Secreted)
Gene: SHBG
UniProt: P04278 (SHBG_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.3
Assay: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin
Drug: nandrolone decanoate
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.46
Assay: Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Drug: nandrolone decanoate
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.68
Assay: DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
Drug: nandrolone decanoate
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: Ki = 7.65
Assay: DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
Drug: nandrolone phenpropionate
Target: Estrogen receptor (Nuclear hormone receptor)
Gene: ESR1
UniProt: P03372 (ESR1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.7
Drug: nandrolone phenpropionate
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 9.5
Action type: AGONIST
Drug: naproxen
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.6
Action type: INHIBITOR
Assay: Inhibition activity against recombinant human Prostaglandin G/H synthase 2
Drug: naproxen
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.16
Action type: INHIBITOR
Drug: naproxen
Target: Aldo-keto reductase family 1 member C2 (Enzyme)
Gene: AKR1C2
UniProt: P52895 (AK1C2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.5
Assay: Inhibition of human recombinant N-terminal His6-tagged AKR1C2 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis
Drug: naproxen
Target: Aldo-keto reductase family 1 member C3 (Enzyme)
Gene: AKR1C3
UniProt: P42330 (AK1C3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.32
Assay: Inhibition of recombinant human AKR1C3
Drug: naproxen
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P05979 (PGH1_SHEEP)
Organism: Ovis aries
Activity: IC50 = 6.74
Assay: Inhibition of ovine COX-1
Drug: naproxen
Target: Prostaglandin-H2 D-isomerase (Enzyme)
Gene: Ptgds
UniProt: O09114 (PTGDS_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4.89
Assay: Concentration required to inhibit 50% activity of prostaglandin synthetase was determined in vitro in mouse brain microsomes
Drug: naproxen
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P79208 (PGH2_SHEEP)
Organism: Ovis aries
Activity: IC50 = 5.47
Assay: Inhibition of ovine COX2 assessed as reduction in PGH2 production by enzyme immunoassay
Drug: naproxen
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: O62664 (PGH1_BOVIN)
Organism: Bos taurus
Activity: IC50 = 4.96
Assay: Inhibition of bovine seminal microsomal COX1 assessed as PGE2 production preincubated for 10 mins
Drug: naproxen
Target: Hormone-sensitive lipase (Enzyme)
Gene: Lipe
UniProt: P15304 (LIPS_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.92
Assay: Inhibition of HSL in Wistar rat isolated fat cells by spectrophotometric assay
Drug: naproxen
Target: Cyclooxygenase (Enzyme)
Gene: Ptgs2|Ptgs1
UniProt: P35355|Q63921 (PGH2_RAT|PGH1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.22
Assay: In vitro inhibitory activity against Prostaglandin G/H synthase in rat neutrophils
Drug: naratriptan
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.35
Assay: In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1A receptor
Drug: naratriptan
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.48
Action type: AGONIST
Assay: In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug: naratriptan
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.796
Action type: AGONIST
Drug: naratriptan
Target: 5-hydroxytryptamine receptor 1F (GPCR)
Gene: HTR1F
UniProt: P30939 (5HT1F_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.2
Action type: AGONIST
Drug: naratriptan
Target: 5-hydroxytryptamine receptor 1E (GPCR)
Gene: HTR1E
UniProt: P28566 (5HT1E_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.7
Action type: AGONIST
Drug: nateglinide
Target: Solute carrier family 22 member 6 (Transporter)
Gene: Slc22a6
UniProt: O35956 (S22A6_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.04
Assay: Inhibition of rat Oat1 expressed in Xenopus oocytes
Drug: nateglinide
Target: Sulfonylurea receptor 1, Kir6.2 (Ion channel)
Gene: ABCC8|KCNJ11
UniProt: Q09428|Q14654 (ABCC8_HUMAN|KCJ11_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.46
Action type: BLOCKER
Drug: nateglinide
Target: Sulfonylurea receptor 2, Kir6.2 (Ion channel)
Gene: ABCC9|KCNJ11
UniProt: O60706|Q14654 (ABCC9_HUMAN|KCJ11_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.99
Action type: BLOCKER
Drug: nebivolol
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.5
Action type: ANTAGONIST
Drug: nebivolol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.5
Action type: ANTAGONIST
Drug: nebivolol
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8
Drug: nebivolol
Target: Beta-3 adrenergic receptor (GPCR)
Gene: ADRB3
UniProt: P13945 (ADRB3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.66
Action type: ANTAGONIST
Assay: Radioligand binding
Drug: nedocromil
Target: Cysteinyl leukotriene receptor 1 (GPCR)
Gene: CYSLTR1
UniProt: Q9Y271 (CLTR1_HUMAN)
Organism: Homo sapiens
Drug: nedocromil
Target: G-protein coupled receptor 35 (GPCR)
Gene: GPR35
UniProt: Q9HC97 (GPR35_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.013
Action type: AGONIST
Assay: GPR35a–beta-arrestin-2 interaction assays performed using a CHO–K1 cell line stably expressing human GPR35 and beta-arrestin-2
Drug: nefazodone
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.745
Drug: nefazodone
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6
Action type: INHIBITOR
Drug: nefazodone
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.699
Action type: INHIBITOR
Drug: nefazodone
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.444
Action type: INHIBITOR
Drug: nefazodone
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.097