AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: cilostazol
Target: cGMP-inhibited 3',5'-cyclic phosphodiesterase A (Enzyme)
Gene: PDE3A
UniProt: Q14432 (PDE3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.7
Action type: INHIBITOR
Drug: cilostazol
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5
Assay: DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: cilostazol
Target: cGMP-inhibited 3',5'-cyclic phosphodiesterase B (Enzyme)
Gene: PDE3B
UniProt: Q13370 (PDE3B_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.42
Action type: INHIBITOR
Drug: cimetidine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.155
Drug: cimetidine
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.14
Action type: ANTAGONIST
Drug: cimetidine
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P47747 (HRH2_CAVPO)
Organism: Cavia porcellus
Activity: Kd = 6.58
Assay: In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
Drug: cimetidine
Target: Multidrug and toxin extrusion protein 1 (Transporter)
Gene: SLC47A1
UniProt: Q96FL8 (S47A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.92
Assay: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Drug: cimetidine
Target: Multidrug and toxin extrusion protein 2 (Transporter)
Gene: SLC47A2
UniProt: Q86VL8 (S47A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.1
Action type: INHIBITOR
Drug: cimetidine
Target: Histamine H2 receptor (GPCR)
Gene: Hrh2
UniProt: P25102 (HRH2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.9
Action type: ANTAGONIST
Drug: cinacalcet
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.3
Assay: Inhibition Assay: Incubations were conducted in 96 well microtiter plates based on a method described by BD Biosciences. To the first well in each row, a NADPH regenerating system and test compound was added. In the second well and all remaining wells, NADPH regenerating system and acetonitrile (final concentration of 2%) was added. The final assay concentration of the NADPH regenerating system was 8.2 uM NADP+, 0.41 mM glucose-6-phosphate, 0.41 mM magnesium chloride hexahydrate and 0.4 U/ml glucose-6-phosphate dehydrogenase and 0.01 mg/mL control insect cell membrane protein. The test compound solution was serially diluted 1:3 through the eighth wells.The final concentration of the test compounds were in the range 100 uM to 45.7 nM in the eight rows. Wells 9 and 10 contained no test compound (only NADPH regenerating system and enzyme/substrate mix) and wells 11 and 12 were used as controls for background fluorescence (enzyme and substrate were added after the reaction was te
Drug: cinacalcet
Target: Glycine receptor subunit alpha-1 (Ion channel)
Gene: GLRA1
UniProt: P23415 (GLRA1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.49
Drug: cinacalcet
Target: Extracellular calcium-sensing receptor (GPCR)
Gene: CASR
UniProt: P41180 (CASR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.7
Action type: POSITIVE ALLOSTERIC MODULATOR
Assay: Positive allosteric modulation of calcium sensing receptor by cell based assay
Drug: cinacalcet
Target: Metabotropic glutamate receptor 5 (GPCR)
Gene: Grm5
UniProt: P31424 (GRM5_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.35
Action type: ALLOSTERIC MODULATOR
Drug: cinalukast
Target: Cysteinyl leukotriene receptor 1 (GPCR)
Gene: CYSLTR1
UniProt: Q2NNR5 (CLTR1_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 8.19
Assay: Binding affinity towards Cysteinyl leukotriene D4 receptor (cysLT1) was measured by the displacement of [3H]LTD4 radioligand
Drug: cinalukast
Target: Cysteinyl leukotriene receptor 1 (GPCR)
Gene: CYSLTR1
UniProt: Q9Y271 (CLTR1_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Assay: Mechanism of Action
Drug: cinnarizine
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.035
Assay: DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine)
Drug: cinnarizine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.587
Assay: DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
Drug: cinnarizine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.777
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: cinnarizine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.77
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: cinnarizine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.237
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: cinnarizine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.552
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: cinnarizine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.208
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
Drug: cinnarizine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.987
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: cinnarizine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.333
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: cinnarizine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.99
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: cinnarizine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.066
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: cinnarizine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.064
Assay: DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug: cinnarizine
Target: Histamine H4 receptor (GPCR)
Gene: HRH4
UniProt: Q9H3N8 (HRH4_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.849
Drug: cinnarizine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.218
Assay: DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: cinnarizine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.79
Assay: DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: cinnarizine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.292
Assay: DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: cinnarizine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.264
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: cinnarizine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.022
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: cinnarizine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.885
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: cinnarizine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.242
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: cinnarizine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.299
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: cinnarizine
Target: Membrane-associated progesterone receptor component 1 (Membrane receptor)
Gene: Pgrmc1
UniProt: P70580 (PGRC1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.793
Assay: DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
Drug: cinnarizine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.72
Drug: cinnarizine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.97
Drug: cinnarizine
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 = 6.36
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: cinoxacin
Target: Carbonic anhydrase 2 (Enzyme)
Gene: CA2
UniProt: P00918 (CAH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.08
Drug: cinoxacin
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: ciprofibrate
Target: Peroxisome proliferator-activated receptor alpha (Nuclear hormone receptor)
Gene: PPARA
UniProt: Q07869 (PPARA_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.05
Action type: AGONIST
Assay: Transactivation of GAL4-fused PPARalpha LBD expressed in HepG2 cells after 20 hrs by luminescence assay
Drug: ciprofloxacin
Target: DNA topoisomerase 4 subunit A (Enzyme)
Gene: parC
UniProt: P0AFI2 (PARC_ECOLI)
Organism: Escherichia coli (strain K12)
Activity: IC50 = 5.602
Drug: ciprofloxacin
Target: DNA topoisomerase 4 subunit A (Enzyme)
Gene: parC
UniProt: Q45066 (PARC_BACSU)
Organism: Bacillus subtilis (strain 168)
Activity: IC50 = 5.658
Drug: ciprofloxacin
Target: DNA topoisomerase 4 subunit A (Enzyme)
Gene: parC
UniProt: P0C1U9 (PARC_STAAU)
Organism: Staphylococcus aureus
Activity: IC50 = 6
Action type: INHIBITOR
Drug: ciprofloxacin
Target: DNA gyrase subunit A (Enzyme)
Gene: gyrA
UniProt: P9WG47 (GYRA_MYCTU)
Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv)
Activity: IC50 = 6.2
Drug: ciprofloxacin
Target: DNA gyrase subunit A (Enzyme)
Gene: gyrA
UniProt: P0AES4 (GYRA_ECOLI)
Organism: Escherichia coli (strain K12)
Activity: IC50 = 5.75
Action type: INHIBITOR
Drug: ciprofloxacin
Target: Histamine H3 receptor (GPCR)
Gene: Hrh3
UniProt: Q9QYN8 (HRH3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.18
Drug: ciprofloxacin
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 = 6.39
Assay: Inhibition of [3H]muscimol binding to GABA A receptor 4-biphenylacetic acid at 10 e-4 M
Drug: ciprofloxacin
Target: DNA topoisomerase II (Enzyme)
Gene: TOP2A|TOP2B
UniProt: P11388|Q02880 (TOP2A_HUMAN|TOP2B_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.52
Assay: Inhibitory activity against HeLa cell Topoisomerase II
Drug: ciprofloxacin
Target: Multidrug resistance protein mdtK (Unclassified)
Gene: mdtK
UniProt: P37340 (MDTK_ECOLI)
Organism: Escherichia coli (strain K12)
Activity: Kd = 4.04
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: cisapride
Target: 5-hydroxytryptamine receptor 4 (GPCR)
Gene: HTR4
UniProt: O70528 (5HT4R_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 7.84
Assay: Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
Drug: cisapride
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.77
Assay: Binding affinity to dopamine receptor D1
Drug: cisapride
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.64
Assay: Binding affinity to dopamine receptor D2
Drug: cisapride
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.177
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: cisapride
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.379
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: cisapride
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.19
Assay: Inhibition of human ERG in MCF7 cells
Drug: cisapride
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.523
Assay: DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin)
Drug: cisapride
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.69
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: cisapride
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.1
Assay: Binding affinity to human serotonin 5-HT1A receptor
Drug: cisapride
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.96
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: cisapride
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.15
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: cisapride
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.396
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: cisapride
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.7
Drug: cisapride
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.281
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: cisapride
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.31
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: cisapride
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.947
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: cisapride
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.155
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: cisapride
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.31
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: cisapride
Target: 3-hydroxy-3-methylglutaryl-coenzyme A reductase (Enzyme)
Gene: HMGCR
UniProt: P04035 (HMDH_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.472
Assay: DRUGMATRIX: HMG-CoA Reductase enzyme inhibition (substrate: [14C]HMG-CoA)
Drug: cisapride
Target: 5-hydroxytryptamine receptor 4 (GPCR)
Gene: HTR4
UniProt: Q13639 (5HT4R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.54
Action type: AGONIST
Assay: Binding affinity towards Serotonin 5-hydroxytryptamine 4 receptor
Drug: cisapride
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.063
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: cisapride
Target: Membrane-associated progesterone receptor component 1 (Membrane receptor)
Gene: Pgrmc1
UniProt: P70580 (PGRC1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.963
Assay: DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
Drug: cisapride
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.52
Assay: The ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brain
Drug: cisapride
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.64
Assay: Affinity towards Dopamine receptor D2 in rat striatum using [3H]spiperone as radioligand
Drug: cisapride
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32304 (5HT7R_MOUSE)
Organism: Mus musculus
Activity: Ki = 5.8
Action type: AGONIST
Drug: cisapride
Target: D(1A) dopamine receptor (GPCR)
Gene: Drd1
UniProt: P18901 (DRD1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.77
Assay: The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
Drug: cisapride
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: Adra2a
UniProt: P22909 (ADA2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.52
Assay: Compound was evaluated for the binding affinity at Alpha adrenergic receptor
Drug: cisapride
Target: 5-hydroxytryptamine receptor 4 (GPCR)
Gene: Htr4
UniProt: Q62758 (5HT4R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8
Action type: AGONIST
Drug: cisapride
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: Q75Z89 (5HT2A_BOVIN)
Organism: Bos taurus
Activity: Ki = 8.14
Assay: Compound was evaluated for the binding affinity at 5- HT2 receptor
Drug: cisapride
Target: Serotonin 3 (5-HT3) receptor (Ion channel)
Gene: Htr3a|Htr3b
UniProt: P35563|Q9JJ16 (5HT3A_RAT|5HT3B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.02
Assay: Inhibition of [3H]GR-65630 binding to rat cortical membrane serotonin 5-hydroxytryptamine 3 receptor
Drug: cisapride
Target: Serotonin 3 (5-HT3) receptor (Ion channel)
Gene: HTR3E|HTR3B|HTR3A|HTR3D|HTR3C
UniProt: A5X5Y0|O95264|P46098|Q70Z44|Q8WXA8 (5HT3E_HUMAN|5HT3B_HUMAN|5HT3A_HUMAN|5HT3D_HUMAN|5HT3C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.82
Assay: Compound was tested for 5-hydroxytryptamine 3 receptor binding affinity
Drug: cisapride
Target: Serotonin 1 (5-HT1) receptor (GPCR)
Gene: Htr1a|Htr1b|Htr1d|Htr1f
UniProt: P19327|P28564|P28565|P30940 (5HT1A_RAT|5HT1B_RAT|5HT1D_RAT|5HT1F_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.35
Assay: Inhibitory activity against 5-hydroxytryptamine 1 receptor by 3H ligand binding experiments.
Drug: cisapride
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 = 5.35
Assay: The ability to inhibit [3H]rauwolscine binding to alpha-2 adrenergic receptor in rat cortex
Drug: cisapride
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 = 8.21
Assay: The ability to inhibit [3H]ketanserin binding to 5-hydroxytryptamine 2 receptor in rat whole brain
Drug: cisapride
Target: 5-hydroxytryptamine receptor 4 (GPCR)
Gene: Htr4
UniProt: P97288 (5HT4R_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.5
Action type: AGONIST
Drug: cisatracurium
Target: Acetylcholine receptor (Ion channel)
Gene: CHRNA1|CHRNB1|CHRND
UniProt: P02708|P11230|Q07001 (ACHA_HUMAN|ACHB_HUMAN|ACHD_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8
Action type: ANTAGONIST
Drug: citalopram
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.777
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: citalopram
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.4
Drug: citalopram
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.935
Action type: INHIBITOR
Drug: citalopram
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.21
Assay: In vitro binding affinity against human norepinephrine transporter in human embryonic kidney cell line by using [3H]-nisoxatine radioligand
Drug: citalopram
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.191
Drug: citalopram
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.931
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: citalopram
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.21
Drug: citalopram
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.456
Drug: citalopram
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.875
Drug: citalopram
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.78
Assay: In vitro binding affinity against human dopamine transporter in dog kidney cell line by using [125I]RTI-55 radioligand
Drug: citalopram
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.148
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: citalopram
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.73
Assay: Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Drug: citalopram
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.74
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: citalopram
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.76