AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: nimesulide
Target: Sodium-dependent neutral amino acid transporter B(0)AT1 (Transporter)
Gene: Slc6a19
UniProt: Q2A865 (S6A19_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.64
Action type: INHIBITOR
Drug: nimesulide
Target: Dipeptidyl peptidase 3 (Enzyme)
UniProt: L8I2E6 (L8I2E6_9CETA)
Organism: Bos mutus
Activity: Ki = 4.16
Assay: Mixed type inhibition of Capra hircus (goat) brain DPP-3 using Arg-Arg-4mbetaNA as substrate assessed as liberation of 4mbetaNA from substrate preincubated for 10 min by Cornish-Bowden plot analysis
Drug: nimodipine
Target: Sodium/nucleoside cotransporter 1 (Transporter)
Gene: SLC28A1
UniProt: O00337 (S28A1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.364
Assay: DRUGMATRIX: Sodium/nucleoside co-transporter radioligand binding (ligand: nitrobenzylthioinosine)
Drug: nimodipine
Target: Cannabinoid receptor 1 (GPCR)
Gene: CNR1
UniProt: P21554 (CNR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.863
Assay: DRUGMATRIX: Cannabinoid CB1 radioligand binding (ligand: [3H] SR141716A)
Drug: nimodipine
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.12
Drug: nimodipine
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.072
Drug: nimodipine
Target: Nuclear receptor subfamily 1 group I member 2 (Nuclear hormone receptor)
Gene: NR1I2
UniProt: O75469 (NR1I2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.41
Assay: Agonist activity at PXR (unknown origin) expressed in human HepG2 cells assessed as induction of CYP3A4 transactivation after 16 hrs by luciferase reporter gene assay
Drug: nimodipine
Target: Voltage-dependent calcium channel gamma-1 subunit (Ion channel)
Gene: CACNG1
UniProt: Q06432 (CCG1_HUMAN)
Organism: Homo sapiens
Drug: nimodipine
Target: Mineralocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C2
UniProt: P08235 (MCR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.8
Action type: ANTAGONIST
Drug: nimodipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: CACNA1C
UniProt: Q13936 (CAC1C_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: nimodipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1D (Ion channel)
Gene: CACNA1D
UniProt: Q01668 (CAC1D_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: nimodipine
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Assay: DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: nimodipine
Target: Voltage-dependent T-type calcium channel subunit alpha-1H (Ion channel)
Gene: CACNA1H
UniProt: O95180 (CAC1H_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.252
Drug: nimodipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1S (Ion channel)
Gene: CACNA1S
UniProt: Q13698 (CAC1S_HUMAN)
Organism: Homo sapiens
Activity: IC50 ~ 6
Action type: GATING INHIBITOR
Drug: nimodipine
Target: Cytochrome P450 2C19 (Enzyme)
Gene: CYP2C19
UniProt: P33261 (CP2CJ_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.398
Assay: DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: nimodipine
Target: Bile acid receptor (Nuclear hormone receptor)
Gene: NR1H4
UniProt: Q96RI1 (NR1H4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.05
Assay: Antagonist activity at human GTS-tagged FXR after 20 mins by TR-FRET assay
Drug: nimodipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1F (Ion channel)
Gene: CACNA1F
UniProt: O60840 (CAC1F_HUMAN)
Organism: Homo sapiens
Activity: IC50 ~ 6
Action type: GATING INHIBITOR
Drug: nimodipine
Target: Adenosine receptor A1 (GPCR)
Gene: Adora1
UniProt: P25099 (AA1R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.7
Assay: Displacement of [3H](R)-PIA binding to Adenosine A1 receptor in rat brain membranes
Drug: nimodipine
Target: Adenosine receptor A2a (GPCR)
Gene: Adora2a
UniProt: P30543 (AA2AR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.35
Assay: Displacement of [3H]-CGS- 21680 binding to Adenosine A2A receptor in rat striatal membranes
Drug: nimodipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: Cacna1c
UniProt: P22002 (CAC1C_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.8
Action type: GATING INHIBITOR
Drug: nimodipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1D (Ion channel)
Gene: Cacna1d
UniProt: P27732 (CAC1D_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.6
Action type: GATING INHIBITOR
Drug: nisoldipine
Target: Adenosine receptor A2a (GPCR)
Gene: ADORA2A
UniProt: P29274 (AA2AR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.642
Assay: DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA)
Drug: nisoldipine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.638
Drug: nisoldipine
Target: Voltage-dependent P/Q-type calcium channel subunit alpha-1A (Ion channel)
Gene: CACNA1A
UniProt: O00555 (CAC1A_HUMAN)
Organism: Homo sapiens
Drug: nisoldipine
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.395
Assay: DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
Drug: nisoldipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: CACNA1C
UniProt: Q13936 (CAC1C_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.1
Action type: GATING INHIBITOR
Drug: nisoldipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1D (Ion channel)
Gene: CACNA1D
UniProt: Q01668 (CAC1D_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: nisoldipine
Target: Voltage-dependent T-type calcium channel subunit alpha-1H (Ion channel)
Gene: CACNA1H
UniProt: O95180 (CAC1H_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.337
Drug: nisoldipine
Target: Cytochrome P450 1A2 (Enzyme)
Gene: CYP1A2
UniProt: P05177 (CP1A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Assay: DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: nisoldipine
Target: Sodium channel alpha subunits; brain (Types I, II, III) (Ion channel)
Gene: SCN1A|SCN2A|SCN3A
UniProt: P35498|Q99250|Q9NY46 (SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.59
Assay: Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex
Drug: nisoldipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: Cacna1c
UniProt: Q01815 (CAC1C_MOUSE)
Organism: Mus musculus
Activity: IC50 = 8
Action type: GATING INHIBITOR
Drug: nisoldipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1D (Ion channel)
Gene: Cacna1d
UniProt: Q99246 (CAC1D_MOUSE)
Organism: Mus musculus
Activity: IC50 = 7
Action type: GATING INHIBITOR
Drug: nitazoxanide
Target: Aldose reductase (Enzyme)
Gene: AKR1B1
UniProt: P15121 (ALDR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.09
Drug: nitazoxanide
Target: Pyruvate dehydrogenase [NADP(+)] (Enzyme)
Gene: PFOR
UniProt: Q968X7 (PNO_CRYPV)
Organism: Cryptosporidium parvum
Action type: INHIBITOR
Drug: nitazoxanide
Target: Pyruvate:ferredoxin oxidoreductase (Enzyme)
UniProt: Q24982 (Q24982_GIAIN)
Organism: Giardia intestinalis
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2364027; SINGLE PROTEIN
Drug: nitazoxanide
Target: Pyruvate-flavodoxin oxidoreductase (Enzyme)
UniProt: Q0P8E1 (Q0P8E1_CAMJE)
Organism: Campylobacter jejuni subsp. jejuni serotype O:2
Activity: Ki = 4.98
Assay: Inhibition of PFOR Campylobacter jejuni
Drug: nitisinone
Target: 4-hydroxyphenylpyruvate dioxygenase (Enzyme)
Gene: HPD
UniProt: P32754 (HPPD_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.398
Action type: INHIBITOR
Drug: nitisinone
Target: 4-hydroxyphenylpyruvate dioxygenase (Enzyme)
Gene: HPD
UniProt: Q02110 (HPPD_PIG)
Organism: Sus scrofa
Activity: IC50 = 7.4
Assay: Inhibition of 4-hydroxyphenylpyruvate dioxygenase of purified pig liver by enol-borate method
Drug: nitisinone
Target: 4-hydroxyphenylpyruvate dioxygenase (Unclassified)
Gene: Hpd
UniProt: P32755 (HPPD_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.4
Assay: Inhibition of Wistar rat liver cytosol HPPD using HPP as substrate assessed as reduction in O2 consumption
Drug: nitrazepam
Target: GABA-A receptor alpha-1/beta-2/gamma-2 (Ion channel)
Gene: GABRA1|GABRG2|GABRB2
UniProt: P14867|P18507|P47870 (GBRA1_HUMAN|GBRG2_HUMAN|GBRB2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: nitrazepam
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: IC50 = 7.42
Assay: Inhibition of [3H]flunitrazepam binding to GABA-A central Benzodiazepine receptor of bovine brain membranes
Drug: nitrendipine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5
Assay: Inhibition of human Potassium channel HERG expressed in mammalian cells
Drug: nitrendipine
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.081
Drug: nitrendipine
Target: Intermediate conductance calcium-activated potassium channel protein 4 (Ion channel)
Gene: KCNN4
UniProt: O15554 (KCNN4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.6
Action type: BLOCKER
Drug: nitrendipine
Target: Voltage-dependent calcium channel gamma-1 subunit (Ion channel)
Gene: CACNG1
UniProt: Q06432 (CCG1_HUMAN)
Organism: Homo sapiens
Drug: nitrendipine
Target: Transthyretin (Secreted)
Gene: TTR
UniProt: P02766 (TTHY_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.921
Drug: nitrendipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1D (Ion channel)
Gene: CACNA1D
UniProt: Q01668 (CAC1D_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.4
Action type: GATING INHIBITOR
Assay: Recombinant Cav1.3 calcium channel complexes expressed in tsA-cells
Drug: nitrendipine
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.523
Assay: DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: nitrendipine
Target: Voltage-dependent T-type calcium channel subunit alpha-1H (Ion channel)
Gene: CACNA1H
UniProt: O95180 (CAC1H_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.056
Drug: nitrendipine
Target: Cytochrome P450 2C19 (Enzyme)
Gene: CYP2C19
UniProt: P33261 (CP2CJ_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.523
Assay: DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: nitrendipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1F (Ion channel)
Gene: CACNA1F
UniProt: O60840 (CAC1F_HUMAN)
Organism: Homo sapiens
Activity: IC50 ~ 6
Action type: GATING INHIBITOR
Drug: nitrendipine
Target: Adenosine receptor A1 (GPCR)
Gene: Adora1
UniProt: P25099 (AA1R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.05
Assay: Displacement of [3H](R)-PIA binding to Adenosine A1 receptor in rat brain membranes
Drug: nitrendipine
Target: Adenosine receptor A2a (GPCR)
Gene: Adora2a
UniProt: P30543 (AA2AR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.64
Assay: Displacement of [3H]-CGS- 21680 binding to Adenosine A2A receptor in rat striatal membranes
Drug: nitrendipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: Cacna1c
UniProt: P22002 (CAC1C_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6
Action type: GATING INHIBITOR
Drug: nitrendipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1S (Ion channel)
Gene: Cacna1s
UniProt: Q02485 (CAC1S_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6
Action type: GATING INHIBITOR
Drug: nitrendipine
Target: Platelet-activating factor receptor (GPCR)
Gene: PTAFR
UniProt: P21556 (PTAFR_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 4.13
Assay: Tested for inhibition of [3H]PAF binding to rabbit Platelet activating factor receptor
Drug: nitrendipine
Target: Sodium channel alpha subunits; brain (Types I, II, III) (Ion channel)
Gene: SCN1A|SCN2A|SCN3A
UniProt: P35498|Q99250|Q9NY46 (SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.44
Assay: Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex
Drug: nitrendipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: CACNA1C
UniProt: Q13936 (CAC1C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.6
Action type: BLOCKER
Assay: Inhibition of [3H]nitrendipine binding to L-type calcium channel dihydropyridine site of porcine cardiac sarcolemma membrane vesicles
Drug: nitric oxide
Target: Soluble guanylate cyclase (Enzyme)
Gene: GUCY1B2|GUCY1A2|GUCY1A3|GUCY1B3
UniProt: O75343|P33402|Q02108|Q02153 (GCYB2_HUMAN|GCYA2_HUMAN|GCYA3_HUMAN|GCYB1_HUMAN)
Organism: Homo sapiens
Action type: ACTIVATOR
Assay: Mechanism of Action; CHEMBL2111348; PROTEIN COMPLEX GROUP
Drug: nitrofurantoin
Target: Glucose-6-phosphate 1-dehydrogenase (Enzyme)
Gene: G6PD
UniProt: P11413 (G6PD_HUMAN)
Organism: Homo sapiens
Drug: nitrofurantoin
Target: CDGSH iron-sulfur domain-containing protein 1 (Unclassified)
Gene: CISD1
UniProt: Q9NZ45 (CISD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.09
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: nitrofurazone
Target: Glucose-6-phosphate 1-dehydrogenase (Enzyme)
Gene: G6PD
UniProt: P11413 (G6PD_HUMAN)
Organism: Homo sapiens
Drug: nitrofurazone
Target: Snake venom metalloproteinase Bap1 (Enzyme)
UniProt: P83512 (VM1B1_BOTAS)
Organism: Bothrops asper
Activity: IC50 = 4.06
Assay: Inhibition of snake venom BaP1 using Abz-Ala-Gly-Leu-Ala-Nba as substrate incubated for 30 mins prior to substrate addition by fluorescence spectrophotometry
Drug: glyceryl trinitrate
Target: Atrial natriuretic peptide receptor 1 (Enzyme)
Gene: NPR1
UniProt: P16066 (ANPRA_HUMAN)
Organism: Homo sapiens
Drug: glyceryl trinitrate
Target: Soluble guanylate cyclase (Enzyme)
Gene: GUCY1B2|GUCY1A2|GUCY1A3|GUCY1B3
UniProt: O75343|P33402|Q02108|Q02153 (GCYB2_HUMAN|GCYA2_HUMAN|GCYA3_HUMAN|GCYB1_HUMAN)
Organism: Homo sapiens
Action type: ACTIVATOR
Assay: Mechanism of Action; CHEMBL2111348; PROTEIN COMPLEX GROUP
Drug: nitroxoline
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6
Assay: Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate assessed as formation of prostanoid products preincubated for 10 mins prior to substrate addition measured after 2 mins by Ellman's method
Drug: nitroxoline
Target: Cathepsin B (Enzyme)
Gene: CTSB
UniProt: P07858 (CATB_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.4
Assay: Mixed inhibition of cathepsin B (unknown origin) endopeptidase activity assessed as inhibition constant for enzyme-substrate-inhibitor complex
Drug: nitroxoline
Target: Methionine aminopeptidase 2 (Enzyme)
Gene: METAP2
UniProt: P50579 (MAP2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.26
Assay: Inhibition of human methionine aminopeptidase 2
Drug: nitroxoline
Target: Catechol O-methyltransferase (Enzyme)
Gene: Comt
UniProt: P22734 (COMT_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.7
Assay: Inhibition of Sprague-Dawley rat liver COMT after 10 mins using 0.05 uCi [14CH3]-SAM as substrate
Drug: nitroxoline
Target: Bromodomain-containing protein 4 (Unclassified)
Gene: BRD4
UniProt: O60885 (BRD4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.01
Assay: Inhibition of BRD4 in human MV4-11 cells using biotin labelled N-C:SGRG-K(Ac)-GG-K(Ac)-GLG-K(Ac)-GGA-K(Ac)-RHRKVGG-K as substrate preincubated for 15 mins followed by substrate addition measured after 5 mins by alpha screen assay
Drug: nizatidine
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.92
Action type: ANTAGONIST
Drug: nizatidine
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P22303 (ACES_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.251
Assay: DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine)
Drug: nomifensine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.85
Assay: Inhibition of human recombinant SERT expressed in HEK cells
Drug: nomifensine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.67
Action type: INHIBITOR
Drug: nomifensine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.93
Drug: nomifensine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.57
Drug: nomifensine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.31
Action type: INHIBITOR
Drug: nomifensine
Target: Amine oxidase [flavin-containing] A (Enzyme)
Gene: MAOA
UniProt: P21397 (AOFA_HUMAN)
Organism: Homo sapiens
Activity: Km = 2.947
Drug: nomifensine
Target: Myeloperoxidase (Enzyme)
Gene: MPO
UniProt: P05164 (PERM_HUMAN)
Organism: Homo sapiens
Activity: Km = 3.963
Drug: nomifensine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: Slc6a4
UniProt: P31652 (SC6A4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.06
Assay: Inhibition of serotonin (5-HT) uptake into rat brain synaptosomes
Drug: nomifensine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: Slc6a3
UniProt: P23977 (SC6A3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.59
Assay: Inhibition of DAT in rat synaptosomal membrane
Drug: nomifensine
Target: Transporter (Transporter)
Gene: Slc6a2
UniProt: Q9WTR4 (Q9WTR4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.42
Assay: Inhibition of uptake of tritiated norepinephrine (NE) in rat synaptosomes
Drug: nomifensine
Target: Transporter (Transporter)
Gene: NET
UniProt: Q63380 (Q63380_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.4
Assay: Inhibition of NET in rat synaptosomal membrane
Drug: nomifensine
Target: Hemoglobin HbA (Enzyme)
Gene: HBB|HBA1
UniProt: P68871|P69905 (HBB_HUMAN|HBA_HUMAN)
Organism: Homo sapiens
Activity: Km = 4.678
Drug: norelgestromin
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Drug: norepinephrine
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6
Action type: AGONIST
Drug: norepinephrine
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.4
Action type: AGONIST
Assay: Binding affinity to human adrenergic beta2 receptor
Drug: norepinephrine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.3
Assay: Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug: norepinephrine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.89
Assay: Displacement of [3H]spiperone from human D2S receptor expressed in CHO cells
Drug: norepinephrine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.18
Action type: AGONIST
Assay: Binding affinity for human Alpha-2A adrenergic receptor
Drug: norepinephrine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.82
Action type: AGONIST
Assay: Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101
Drug: norepinephrine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.48
Drug: norepinephrine
Target: Beta-3 adrenergic receptor (GPCR)
Gene: ADRB3
UniProt: P13945 (ADRB3_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.367
Drug: norepinephrine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.2
Action type: AGONIST
Assay: Binding affinity for human Alpha-2C adrenergic receptor
Drug: norepinephrine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.071
Drug: norepinephrine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.4
Action type: AGONIST
Drug: norepinephrine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.69
Action type: AGONIST
Assay: Displacement of [3H]prazosin from human adrenergic Alpha-1B receptor expressed in CHO cell membrane
Drug: norepinephrine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: Adra2b
UniProt: P19328 (ADA2B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.11
Assay: Binding affinity for rat Alpha-2B adrenergic receptor
Drug: norepinephrine
Target: Mu-type opioid receptor (GPCR)
Gene: Oprm1
UniProt: P33535 (OPRM_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.85
Assay: Compound was evaluated for binding affinity towards mu-specific opiate receptor from combinatorial peptoid library
Drug: norepinephrine
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: Q28044 (ADRB2_BOVIN)
Organism: Bos taurus
Activity: Ki = 5.22
Assay: Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
Drug: norepinephrine
Target: Beta-1 adrenergic receptor (GPCR)
Gene: Adrb1
UniProt: P18090 (ADRB1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.9
Assay: Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligand
Drug: norepinephrine
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P54833 (ADRB2_CANFA)
Organism: Canis familiaris
Activity: Ki = 5.3
Assay: Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
Drug: norepinephrine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P18130 (ADA1A_BOVIN)
Organism: Bos taurus
Activity: Ki = 6.35
Drug: norepinephrine
Target: Beta-2 adrenergic receptor (GPCR)
Gene: Adrb2
UniProt: P10608 (ADRB2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.38
Assay: Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
Drug: norepinephrine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P18841 (ADA1B_MESAU)
Organism: Mesocricetus auratus
Activity: Ki = 6.58
Drug: norepinephrine
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: B0FL73 (B0FL73_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 6.4
Assay: Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
Drug: norepinephrine
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 = 8.32
Assay: Tested for binding affinity against alpha-2 adrenergic receptor in rat brain using [3H]- rauwolscine as radioligand
Drug: norepinephrine
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 = 6.41
Assay: Binding affinity for alpha-1 adrenergic receptor in rat liver using [3H]prazosin.