AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: norepinephrine
Target: Adrenergic receptor alpha (GPCR)
Gene: Adra1b|Adra2b|Adra2c|Adra2a|Adra1d|Adra1a
UniProt: P15823|P19328|P22086|P22909|P23944|P43140 (ADA1B_RAT|ADA2B_RAT|ADA2C_RAT|ADA2A_RAT|ADA1D_RAT|ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.8
Assay: Binding affinity against Alpha adrenergic receptor using [3H]dihydroergocryptine radioligand in rat brain homogenate
Drug: norepinephrine
Target: Adrenergic receptor beta (GPCR)
Gene: Adrb2|Adrb1|Adrb3
UniProt: P10608|P18090|P26255 (ADRB2_RAT|ADRB1_RAT|ADRB3_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6
Assay: Inhibitory concentration required for displacement of Beta adrenergic receptor specific ligand [3H]dihydroalprenolol from rat brain cerebral cortical membranes
Drug: norepinephrine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: Adra2c
UniProt: Q01337 (ADA2C_MOUSE)
Organism: Mus musculus
Activity: Ki = 6.19
Assay: Binding affinity to mouse alpha-2C receptor expressed in COS7 cells
Drug: norepinephrine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: Adra2a
UniProt: Q01338 (ADA2A_MOUSE)
Organism: Mus musculus
Activity: Ki = 5.24
Assay: Binding affinity to mouse alpha-2A receptor expressed in COS7 cells
Drug: norethisterone
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.618
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: norethisterone
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.706
Assay: DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
Drug: norethisterone
Target: Estrogen receptor (Nuclear hormone receptor)
Gene: ESR1
UniProt: P03372 (ESR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.636
Assay: DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol)
Drug: norethisterone
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.12
Drug: norethisterone
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Activity: ED50 = 11.26
Action type: AGONIST
Drug: norethisterone
Target: Sex hormone-binding globulin (Secreted)
Gene: SHBG
UniProt: P04278 (SHBG_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.97
Assay: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin
Drug: norethisterone
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.92
Assay: Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881)
Drug: norethisterone
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: Ki = 8.914
Assay: DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
Drug: norethisterone
Target: Estrogen receptor (Transcription factor)
Gene: Esr1|Esr2
UniProt: P06211|Q62986 (ESR1_RAT|ESR2_RAT)
Organism: Rattus norvegicus
Activity: Kd = 9.2
Assay: Equilibrium dissociation constant for rat uterine estrogen receptor binding [3H]estradiol
Drug: norethindrone acetate
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.62
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: norethindrone acetate
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.533
Assay: DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
Drug: norethindrone acetate
Target: Estrogen receptor (Nuclear hormone receptor)
Gene: ESR1
UniProt: P03372 (ESR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.64
Assay: DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol)
Drug: norethindrone acetate
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.12
Drug: norethindrone acetate
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Activity: ED50 = 11.26
Action type: AGONIST
Drug: norethindrone acetate
Target: Cytochrome P450 2C19 (Enzyme)
Gene: CYP2C19
UniProt: P33261 (CP2CJ_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.097
Assay: DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: norethindrone acetate
Target: Sex hormone-binding globulin (Secreted)
Gene: SHBG
UniProt: P04278 (SHBG_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.97
Assay: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin
Drug: norethindrone acetate
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.149
Assay: DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
Drug: norethindrone acetate
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: Ki = 8.441
Assay: DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
Drug: norethynodrel
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action; CHEMBL208; SINGLE PROTEIN
Drug: norethynodrel
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.81
Assay: Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881)
Drug: norfloxacin
Target: Gamma-aminobutyric acid receptor subunit alpha-1 (Ion channel)
Gene: GABRA1
UniProt: P14867 (GBRA1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.29
Drug: norfloxacin
Target: Gamma-aminobutyric acid receptor subunit alpha-2 (Ion channel)
Gene: GABRA2
UniProt: P47869 (GBRA2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.29
Drug: norfloxacin
Target: Gamma-aminobutyric acid receptor subunit alpha-3 (Ion channel)
Gene: GABRA3
UniProt: P34903 (GBRA3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.29
Drug: norfloxacin
Target: Gamma-aminobutyric acid receptor subunit alpha-5 (Ion channel)
Gene: GABRA5
UniProt: P31644 (GBRA5_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.29
Drug: norfloxacin
Target: DNA topoisomerase 4 subunit A (Enzyme)
Gene: parC
UniProt: P0AFI2 (PARC_ECOLI)
Organism: Escherichia coli (strain K12)
Activity: IC50 = 5.29
Action type: INHIBITOR
Drug: norfloxacin
Target: DNA topoisomerase 4 subunit A (Enzyme)
Gene: parC
UniProt: P0C1U9 (PARC_STAAU)
Organism: Staphylococcus aureus
Activity: IC50 = 5.46
Assay: Inhibition of topoisomerase 4 decatenation in Staphylococcus aureus ATCC 29213
Drug: norfloxacin
Target: DNA gyrase subunit A (Enzyme)
Gene: gyrA
UniProt: P9WG47 (GYRA_MYCTU)
Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv)
Activity: IC50 = 4.28
Assay: Inhibition of DNA supercoiling activity of wild type Mycobacterium tuberculosis DNA gyrase A
Drug: norfloxacin
Target: DNA gyrase subunit A (Enzyme)
Gene: gyrA
UniProt: P0AES4 (GYRA_ECOLI)
Organism: Escherichia coli (strain K12)
Activity: IC50 = 6.05
Action type: INHIBITOR
Drug: norfloxacin
Target: Gamma-aminobutyric acid receptor subunit alpha-4 (Ion channel)
Gene: GABRA4
UniProt: P48169 (GBRA4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.29
Drug: norfloxacin
Target: Gamma-aminobutyric acid receptor subunit alpha-6 (Ion channel)
Gene: GABRA6
UniProt: Q16445 (GBRA6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.29
Drug: norfloxacin
Target: DNA topoisomerase 2-beta (Enzyme)
Gene: TOP2B
UniProt: Q02880 (TOP2B_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.22
Drug: norfloxacin
Target: Multidrug and toxin extrusion protein 1 (Transporter)
Gene: SLC47A1
UniProt: Q96FL8 (S47A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.75
Assay: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Drug: norfloxacin
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: IC50 = 7.7
Assay: Inhibition of [3H]muscimol binding to GABA A receptor 4-biphenylacetic acid at 10 e-4 M
Drug: norfloxacin
Target: Multidrug resistance protein mdtK (Unclassified)
Gene: mdtK
UniProt: P37340 (MDTK_ECOLI)
Organism: Escherichia coli (strain K12)
Activity: Kd = 4.01
Assay: Binding affinity to Escherichia coli K-12 multidrug efflux protein YdhE expressed in Escherichia coli AG100AX in presence of 0.02% DDM surfactant by fluorescence polarization assay
Drug: norgestimate
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Drug: norgestimate
Target: Short transient receptor potential channel 3 (Ion channel)
Gene: TRPC3
UniProt: Q13507 (TRPC3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.52
Action type: BLOCKER
Assay: Norgestimate-induced inhibition of hTRPC3-mediated Ca2+ entry in transfected CHO cells stimulated with the OAG diacylglycerol analog.
Drug: norgestimate
Target: Short transient receptor potential channel 6 (Ion channel)
Gene: TRPC6
UniProt: Q9Y210 (TRPC6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.28
Action type: BLOCKER
Assay: Norgestimate-induced inhibition of hTRPC6-mediated Ca2+ entry in transfected HEK-FITR cells stimulated with the OAG diacylglycerol analog.
Drug: nortriptyline
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.57
Assay: DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug: nortriptyline
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.59
Drug: nortriptyline
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.561
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: nortriptyline
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.34
Action type: INHIBITOR
Drug: nortriptyline
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.36
Action type: INHIBITOR
Drug: nortriptyline
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.509
Drug: nortriptyline
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.356
Drug: nortriptyline
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.066
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: nortriptyline
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8
Drug: nortriptyline
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.67
Assay: Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug: nortriptyline
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.26
Drug: nortriptyline
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7
Drug: nortriptyline
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.215
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: nortriptyline
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.033
Drug: nortriptyline
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.639
Assay: DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug: nortriptyline
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.398
Drug: nortriptyline
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.959
Drug: nortriptyline
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.301
Drug: nortriptyline
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.076
Drug: nortriptyline
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.013
Drug: nortriptyline
Target: Aldehyde oxidase (Enzyme)
Gene: AOX1
UniProt: Q06278 (AOXA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.071
Drug: nortriptyline
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.523
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: nortriptyline
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.921
Drug: nortriptyline
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: Km = 6.225
Drug: nortriptyline
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.91
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: nortriptyline
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: nortriptyline
Target: Proto-oncogene tyrosine-protein kinase receptor Ret (Kinase)
Gene: RET
UniProt: P07949 (RET_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.82
Drug: nortriptyline
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.943
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: nortriptyline
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.837
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug: nortriptyline
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 10.4
Assay: Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
Drug: nortriptyline
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.73
Drug: nortriptyline
Target: Histamine H1 receptor (GPCR)
Gene: Hrh1
UniProt: P31390 (HRH1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 10.3
Assay: Compound tested for its inhibitory activity against Histamine H1 receptor
Drug: nortriptyline
Target: ATP-sensitive inward rectifier potassium channel 10 (Ion channel)
Gene: KCNJ10
UniProt: P78508 (KCJ10_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.796
Action type: BLOCKER
Assay: inhibition at +30 mV
Drug: noscapine
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.087
Assay: DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: noscapine
Target: Cytochrome P450 2C19 (Enzyme)
Gene: CYP2C19
UniProt: P33261 (CP2CJ_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.398
Assay: DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: noscapine
Target: Solute carrier family 22 member 2 (Transporter)
Gene: SLC22A2
UniProt: O15244 (S22A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.59
Assay: Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Drug: noscapine
Target: Multidrug and toxin extrusion protein 1 (Transporter)
Gene: SLC47A1
UniProt: Q96FL8 (S47A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.46
Assay: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Drug: novobiocin
Target: ATP-binding cassette sub-family G member 2 (Transporter)
Gene: ABCG2
UniProt: Q9UNQ0 (ABCG2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.18
Assay: Inhibition of ABCG2 in human mitoxantrone-resistant MCF7 cells by Hoechst 33342 assay
Drug: novobiocin
Target: DNA gyrase subunit B (Enzyme)
Gene: gyrB
UniProt: P0AES6 (GYRB_ECOLI)
Organism: Escherichia coli (strain K12)
Activity: IC50 = 6.81
Assay: Inhibition of Escherichia coli JM109 DNA gyrase subunit B assessed as ATP hydrolysis by ATPase assay
Drug: novobiocin
Target: DNA gyrase subunit B (Enzyme)
Gene: gyrB
UniProt: P0A4L9 (GYRB_STRPN)
Organism: Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4)
Activity: IC50 = 7.43
Assay: Inhibition of Streptococcus pneumoniae SP-3 gyrB by enzyme coupled phosphate assay
Drug: novobiocin
Target: ParE (Enzyme)
Gene: parE
UniProt: Q7X1P7 (Q7X1P7_STREE)
Organism: Streptococcus pneumoniae
Activity: IC50 = 5.69
Assay: Inhibition of Streptococcus pneumoniae SP-3 parE after 30 mins
Drug: novobiocin
Target: DNA gyrase subunit B (Enzyme)
Gene: gyrB
UniProt: C3SLN2 (C3SLN2_ECOLX)
Organism: Escherichia coli
Activity: Kd = 7.55
Assay: Binding affinity to Escherichia coli GyrB
Drug: novobiocin
Target: DNA gyrase (Enzyme)
Gene: gyrA|gyrB
UniProt: P0AES4|P0AES6 (GYRA_ECOLI|GYRB_ECOLI)
Organism: Escherichia coli (strain K12)
Activity: IC50 = 7
Assay: Inhibition of reconstituted Escherichia coli DNA gyrase subunit AB assessed as reduction of DNA supercoiling activity using pBR322 DNA substrate
Drug: novobiocin
Target: DNA gyrase (Enzyme)
Gene: gyrB|gyrA
UniProt: Q5HK03|Q5HK04 (GYRB_STAEQ|GYRA_STAEQ)
Organism: Staphylococcus epidermidis (strain ATCC 35984 / RP62A)
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2331040; PROTEIN COMPLEX
Drug: novobiocin
Target: DNA gyrase subunit B (Enzyme)
Gene: gyrB
UniProt: P0C559 (GYRB_MYCSM)
Organism: Mycobacterium smegmatis
Activity: IC50 = 6.7
Assay: Inhibition of Mycobacterium smegmatis GyrB ATPase activity expressed in Escherichia coli BL21 (DE3) after 2 hrs
Drug: novobiocin
Target: DNA gyrase subunit B (Enzyme)
Gene: gyrB
UniProt: P0A0K8 (GYRB_STAAU)
Organism: Staphylococcus aureus
Activity: IC50 = 6.9
Drug: novobiocin
Target: DNULL gyrase subunit B (Enzyme)
Gene: gyrB
UniProt: A0QNE0 (GYRB_MYCS2)
Organism: Mycolicibacterium smegmatis
Activity: IC50 = 7.34
Assay: Inhibition of Mycobacterium smegmatis 155 6His-tagged DNA gyrase B catalytic domain ATPase activity expressed in Escherichia coli BL21 (DE3) pLysS cells assessed as inorganic phosphate release after 120 mins in presence of ATP by malachite green dye based assay
Drug: novobiocin
Target: DNULL gyrase subunit B (Enzyme)
Gene: gyrB
UniProt: C3SLN3 (C3SLN3_ECOLX)
Organism: Escherichia coli
Activity: Ki = 8.15
Assay: Inhibition of Escherichia coli H560 DNA gyrase B ATPase activity after 30 mins by ammonium molybdate/malachite green-based phosphate detection assay
Drug: buphenine
Target: Adrenergic receptor alpha-1 (GPCR)
Gene: ADRA1D|ADRA1A|ADRA1B
UniProt: P25100|P35348|P35368 (ADA1D_HUMAN|ADA1A_HUMAN|ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.21
Assay: In vitro blocking activity against alpha adrenergic receptor, isolated from rabbit aortic strip
Drug: octreotide
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki  7.921
Drug: octreotide
Target: Somatostatin receptor type 2 (GPCR)
Gene: SSTR2
UniProt: P30874 (SSR2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 10.699
Action type: AGONIST
Drug: octreotide
Target: Somatostatin receptor type 3 (GPCR)
Gene: SSTR3
UniProt: P32745 (SSR3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.3
Action type: AGONIST
Drug: octreotide
Target: Somatostatin receptor type 5 (GPCR)
Gene: SSTR5
UniProt: P35346 (SSR5_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.523
Action type: AGONIST
Drug: octreotide
Target: Somatostatin receptor type 2 (GPCR)
Gene: Sstr2
UniProt: P30875 (SSR2_MOUSE)
Organism: Mus musculus
Activity: IC50 = 9.55
Assay: Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR2b
Drug: octreotide
Target: Somatostatin receptor type 3 (GPCR)
Gene: Sstr3
UniProt: P30935 (SSR3_MOUSE)
Organism: Mus musculus
Activity: IC50 = 8.52
Assay: Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3
Drug: octreotide
Target: Somatostatin receptor type 4 (GPCR)
Gene: SSTR4
UniProt: P31391 (SSR4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.4
Action type: AGONIST
Assay: Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
Drug: octreotide
Target: Somatostatin receptor type 5 (GPCR)
Gene: Sstr5
UniProt: P30938 (SSR5_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.98
Assay: Tested for inhibition of radioligand binding to cloned somatostatin receptor rSSTR5
Drug: octreotide
Target: Somatostatin receptor type 1 (GPCR)
Gene: SSTR1
UniProt: P30872 (SSR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.65
Action type: AGONIST
Assay: Displacement of [125I]-somatostatin from human sst1 receptor after 2 hrs by beta scintillation counting analysis
Drug: octreotide
Target: Somatostatin receptor type 2 (GPCR)
Gene: Sstr2
UniProt: P30680 (SSR2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.7
Action type: AGONIST
Drug: octreotide
Target: Somatostatin receptor type 3 (GPCR)
Gene: Sstr3
UniProt: P30936 (SSR3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.8
Action type: AGONIST
Drug: octreotide
Target: Somatostatin receptor type 5 (GPCR)
Gene: Sstr5
UniProt: O08858 (SSR5_MOUSE)
Organism: Mus musculus
Activity: Ki = 9.9
Action type: AGONIST
Drug: ofloxacin
Target: Gamma-aminobutyric acid receptor subunit alpha-2 (Ion channel)
Gene: GABRA2
UniProt: P47869 (GBRA2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.23
Drug: ofloxacin
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.54
Drug: ofloxacin
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.41
Drug: ofloxacin
Target: DNA gyrase subunit A (Enzyme)
Gene: gyrA
UniProt: P0AES4 (GYRA_ECOLI)
Organism: Escherichia coli (strain K12)
Activity: IC50 = 5.28
Action type: INHIBITOR
Drug: ofloxacin
Target: DNA gyrase subunit B (Enzyme)
Gene: gyrB
UniProt: P0AES7 (GYRB_ECO57)
Organism: Escherichia coli O157:H7
Drug: ofloxacin
Target: Histamine H3 receptor (GPCR)
Gene: HRH3
UniProt: Q9Y5N1 (HRH3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.55
Drug: ofloxacin
Target: Gag-Pro-Pol polyprotein (Polyprotein)
Gene: gag-pro-pol
UniProt: P03362 (POL_HTL1A)
Organism: Human T-cell leukemia virus 1 (strain Japan ATK-1 subtype A)
Activity: IC50 = 4.82