AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: clonidine
Target: Nischarin (Membrane receptor)
Gene: NISCH
UniProt: Q9Y2I1 (NISCH_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.05
Assay: Displacement of [3H]-clonidine from bovine imidazoline receptor I-1
Drug: clonidine
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.65
Assay: Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Drug: clonidine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.99
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: clonidine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: Kd = 6.59
Assay: The compound was tested for alpha-adrenergic activity against Alpha-1 adrenergic receptor from rat aorta.
Drug: clonidine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: Adra2b
UniProt: P19328 (ADA2B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.08
Assay: Compound was tested in vitro for binding affinity against Alpha-2B adrenergic receptor from cloned rat RNG receptor transfected into Chinese hamster ovary (CHO) cells
Drug: clonidine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: Adra1d
UniProt: P23944 (ADA1D_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.9
Action type: AGONIST
Drug: clonidine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.27
Drug: clonidine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: Adra2a
UniProt: P22909 (ADA2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.41
Assay: Binding affinity towards alpha-2D adrenergic receptor
Drug: clonidine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P18130 (ADA1A_BOVIN)
Organism: Bos taurus
Activity: EC50 = 7.05
Assay: Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug: clonidine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: Q28838 (ADA2A_BOVIN)
Organism: Bos taurus
Activity: IC50 = 8.7
Assay: Concentration necessary to achieve half maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor at 1 uM
Drug: clonidine
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: B0FL73 (B0FL73_CAVPO)
Organism: Cavia porcellus
Activity: Kd = 4.4
Assay: The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
Drug: clonidine
Target: Nischarin (Unclassified)
Gene: Nisch
UniProt: Q4G017 (NISCH_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.95
Assay: Binding affinity to I1 imidazoline binding site in Rattus norvegicus (rat) PC12 cells
Drug: clonidine
Target: Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 1 (Ion channel)
Gene: Hcn1
UniProt: O88704 (HCN1_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4.4
Action type: BLOCKER
Drug: clonidine
Target: Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 2 (Ion channel)
Gene: Hcn2
UniProt: O88703 (HCN2_MOUSE)
Organism: Mus musculus
Activity: IC50 = 5.1
Action type: BLOCKER
Drug: clonidine
Target: Solute carrier family 22 member 2 (Transporter)
Gene: SLC22A2
UniProt: O15244 (S22A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.796
Drug: clonidine
Target: Multidrug and toxin extrusion protein 1 (Transporter)
Gene: SLC47A1
UniProt: Q96FL8 (S47A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.48
Assay: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Drug: clonidine
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 = 8.82
Assay: In vitro binding affinity was measured as the inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor of rat cortical membranes
Drug: clonidine
Target: Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 (Ion channel)
Gene: Hcn4
UniProt: O70507 (HCN4_MOUSE)
Organism: Mus musculus
Activity: IC50 = 5
Action type: BLOCKER
Drug: clonidine
Target: Alpha-1B adrenergic receptor (GPCR)
UniProt: G3HDX1 (G3HDX1_CRIGR)
Organism: Cricetulus griseus
Activity: EC50 = 7.08
Assay: Agonist activity at hamster recombinant alpha-1B receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug: clonixin
Target: Dihydroorotate dehydrogenase (quinone), mitochondrial (Enzyme)
Gene: DHODH
UniProt: Q02127 (PYRD_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.89
Assay: Inhibition of human recombinant DHODH
Drug: cloperastine
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.83
Assay: Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
Drug: clopidogrel
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.524
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: clopidogrel
Target: P2Y purinoceptor 12 (GPCR)
Gene: P2RY12
UniProt: Q9H244 (P2Y12_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.9
Action type: ANTAGONIST
Drug: clopidogrel
Target: Cytochrome P450 2B6 (Enzyme)
Gene: CYP2B6
UniProt: P20813 (CP2B6_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.3
Drug: clorazepate
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 = 7.47
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: clorazepate
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
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: clorazepate
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
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: clorazepate
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
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: clorprenaline
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.825
Assay: DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug: clorprenaline
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.863
Assay: DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug: clotiapine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.31
Drug: clotiapine
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.36
Assay: In vitro binding affinity against Dopamine D2 receptor in rat striatal tissue.
Drug: clotiapine
Target: D(1A) dopamine receptor (GPCR)
Gene: Drd1
UniProt: P18901 (DRD1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.85
Assay: In vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
Drug: clotiapine
Target: Muscarinic acetylcholine receptor (GPCR)
Gene: Chrm1|Chrm3|Chrm4|Chrm5|Chrm2
UniProt: P08482|P08483|P08485|P08911|P10980 (ACM1_RAT|ACM3_RAT|ACM4_RAT|ACM5_RAT|ACM2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.87
Assay: In vitro binding affinity against Muscarinic acetylcholine receptors in rat brain.
Drug: clotiapine
Target: Serotonin 2 (5-HT2) receptor (GPCR)
Gene: Htr2c|Htr2a|Htr2b
UniProt: P08909|P14842|P30994 (5HT2C_RAT|5HT2A_RAT|5HT2B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.23
Assay: Binding affinity against serotonin 5-hydroxytryptamine 2 receptor
Drug: clotrimazole
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.186
Assay: DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug: clotrimazole
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.379
Assay: DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid)
Drug: clotrimazole
Target: Nuclear receptor subfamily 1 group I member 3 (Nuclear hormone receptor)
Gene: NR1I3
UniProt: Q14994 (NR1I3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.16
Action type: ANTAGONIST
Drug: clotrimazole
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.136
Assay: DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine)
Drug: clotrimazole
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.346
Assay: DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug: clotrimazole
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.391
Assay: DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
Drug: clotrimazole
Target: Adenosine receptor A2a (GPCR)
Gene: ADORA2A
UniProt: P29274 (AA2AR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.147
Assay: DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA)
Drug: clotrimazole
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.351
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: clotrimazole
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.52
Assay: Inhibition of human ERG
Drug: clotrimazole
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.699
Drug: clotrimazole
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.174
Drug: clotrimazole
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.514
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: clotrimazole
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.104
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: clotrimazole
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.995
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
Drug: clotrimazole
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.497
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: clotrimazole
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.132
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: clotrimazole
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.12
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: clotrimazole
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.235
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: clotrimazole
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.429
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: clotrimazole
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.046
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: clotrimazole
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.466
Assay: DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug: clotrimazole
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.294
Assay: DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug: clotrimazole
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.781
Assay: DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: clotrimazole
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.287
Assay: DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: clotrimazole
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.677
Assay: DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: clotrimazole
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.785
Assay: DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: clotrimazole
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.829
Assay: DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
Drug: clotrimazole
Target: Beta-3 adrenergic receptor (GPCR)
Gene: ADRB3
UniProt: P13945 (ADRB3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.267
Assay: DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug: clotrimazole
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.353
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: clotrimazole
Target: Adenosine receptor A1 (GPCR)
Gene: ADORA1
UniProt: P30542 (AA1R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.106
Assay: DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX)
Drug: clotrimazole
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.571
Assay: DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
Drug: clotrimazole
Target: Intermediate conductance calcium-activated potassium channel protein 4 (Ion channel)
Gene: KCNN4
UniProt: O15554 (KCNN4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.15
Assay: Inhibition of human cloned IK1 expressed in african green monkey COS7 cells by whole cell patch clamp assay
Drug: clotrimazole
Target: Nuclear receptor subfamily 1 group I member 2 (Nuclear hormone receptor)
Gene: NR1I2
UniProt: O75469 (NR1I2_HUMAN)
Organism: Homo sapiens
Drug: clotrimazole
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.156
Assay: DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug: clotrimazole
Target: Carbonic anhydrase 2 (Enzyme)
Gene: CA2
UniProt: P00918 (CAH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.521
Assay: DRUGMATRIX: Carbonic Anhydrase II enzyme inhibition (substrate: 4-Nitrophenyl acetate (4-NPA))
Drug: clotrimazole
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.132
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: clotrimazole
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.598
Assay: DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine)
Drug: clotrimazole
Target: Lanosterol 14-alpha demethylase (Enzyme)
Gene: ERG11
UniProt: P10613 (CP51_CANAL)
Organism: Candida albicans (strain SC5314 / ATCC MYA-2876)
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL1780; SINGLE PROTEIN
Drug: clotrimazole
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.756
Assay: DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole)
Drug: clotrimazole
Target: Beta-lactamase (Enzyme)
Gene: ampC
UniProt: P00811 (AMPC_ECOLI)
Organism: Escherichia coli (strain K12)
Activity: IC50 = 4.7
Assay: Compound was tested for the inhibition of beta-lactamase
Drug: clotrimazole
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P22303 (ACES_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.712
Assay: DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine)
Drug: clotrimazole
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.796
Assay: DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: clotrimazole
Target: Platelet-activating factor receptor (GPCR)
Gene: PTAFR
UniProt: P25105 (PTAFR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.645
Assay: DRUGMATRIX: Platelet Activating Factor (PAF) radioligand binding (ligand: [3H] PAF)
Drug: clotrimazole
Target: Aromatase (Enzyme)
Gene: CYP19A1
UniProt: P11511 (CP19A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.74
Assay: Inhibition of human placental microsome CYP19
Drug: clotrimazole
Target: Cysteinyl leukotriene receptor 1 (GPCR)
Gene: CYSLTR1
UniProt: Q9Y271 (CLTR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.78
Assay: DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4)
Drug: clotrimazole
Target: Epidermal growth factor receptor (Kinase)
Gene: EGFR
UniProt: P00533 (EGFR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.159
Assay: DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: clotrimazole
Target: Vasopressin V2 receptor (GPCR)
Gene: AVPR2
UniProt: P30518 (V2R_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.6
Assay: Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
Drug: clotrimazole
Target: Substance-P receptor (GPCR)
Gene: TACR1
UniProt: P25103 (NK1R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.058
Assay: DRUGMATRIX: Tachykinin NK1 radioligand binding (ligand: [3H] Substance P)
Drug: clotrimazole
Target: Steroid 17-alpha-hydroxylase/17,20 lyase (Enzyme)
Gene: CYP17A1
UniProt: P05093 (CP17A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.089
Drug: clotrimazole
Target: Potassium voltage-gated channel subfamily A member 3 (Ion channel)
Gene: KCNA3
UniProt: P22001 (KCNA3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.22
Assay: Inhibition of cloned Kv1.3 channel expressed in mammalian cells by whole cell patch clamp assay
Drug: clotrimazole
Target: Cytochrome P450 2C19 (Enzyme)
Gene: CYP2C19
UniProt: P33261 (CP2CJ_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.796
Assay: DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: clotrimazole
Target: Tyrosine-protein kinase Fyn (Kinase)
Gene: FYN
UniProt: P06241 (FYN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.497
Assay: DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: clotrimazole
Target: Receptor tyrosine-protein kinase erbB-2 (Kinase)
Gene: ERBB2
UniProt: P04626 (ERBB2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.178
Assay: DRUGMATRIX: Protein Tyrosine Kinase, ERBB2 (HER2) enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: clotrimazole
Target: Thromboxane-A synthase (Enzyme)
Gene: TBXAS1
UniProt: P24557 (THAS_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.854
Assay: DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2)
Drug: clotrimazole
Target: Bile acid receptor (Nuclear hormone receptor)
Gene: NR1H4
UniProt: Q96RI1 (NR1H4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.49
Assay: Antagonist activity at human GTS-tagged FXR after 20 mins by TR-FRET assay
Drug: clotrimazole
Target: Lanosterol 14-alpha demethylase (Enzyme)
Gene: CYP51A1
UniProt: Q16850 (CP51A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.89
Assay: Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay
Drug: clotrimazole
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.92
Assay: Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
Drug: clotrimazole
Target: Substance-K receptor (GPCR)
Gene: TACR2
UniProt: P21452 (NK2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.471
Assay: DRUGMATRIX: Tachykinin NK2  radioligand binding (ligand: [3H] SR-48968)
Drug: clotrimazole
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.112
Assay: DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
Drug: clotrimazole
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.906
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug: clotrimazole
Target: C-C chemokine receptor type 4 (GPCR)
Gene: CCR4
UniProt: P51679 (CCR4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.8
Assay: Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
Drug: clotrimazole
Target: Cysteinyl leukotriene receptor 1 (GPCR)
Gene: CYSLTR1
UniProt: Q2NNR5 (CLTR1_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 4.78
Assay: DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4)
Drug: clotrimazole
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: Ki = 5.942
Assay: DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
Drug: clotrimazole
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.58
Drug: clotrimazole
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.75
Drug: clotrimazole
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