AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: levosulpiride
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.29
Assay: In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D2 short form expressed in CHO cells
Drug: levosulpiride
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.06
Assay: In vitro displacement of [3H]spiperone from the cloned human dopamine receptor D3 stably expressed in CHO cells
Drug: levosulpiride
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.68
Assay: In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug: levosulpiride
Target: Myeloperoxidase (Enzyme)
Gene: MPO
UniProt: P05164 (PERM_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.12
Assay: Inhibition of recombinant MPO (unknown origin) assessed as reduction in taurine chloramine production preincubated with enzyme and taurine followed by H2O2 addition measured after 5 mins
Drug: levosulpiride
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.16
Assay: Inhibition of [3H]spiperone binding to rat striatal membrane Dopamine receptor D2
Drug: levosulpiride
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: Q95136 (DRD1_BOVIN)
Organism: Bos taurus
Activity: Ki = 4.3
Assay: In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug: levosulpiride
Target: Dopamine receptor (GPCR)
Gene: Drd1|Drd3|Drd5|Drd4|Drd2
UniProt: P18901|P19020|P25115|P30729|P61169 (DRD1_RAT|DRD3_RAT|DRD5_RAT|DRD4_RAT|DRD2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.68
Assay: Antidopamine activity in vitro by ability to displace [3H]spiperone from rat brain striatal preparations.
Drug: levosulpiride
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 = 4.82
Assay: Ability to inhibit [3H]WB-4101 binding to alpha-1 adrenergic receptor was determined in rat
Drug: levosulpiride
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 = 4.57
Assay: Ability to inhibit [3H]spiperone binding to 5-hydroxytryptamine 2 receptor determined in rat
Drug: lidocaine
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.8
Action type: BLOCKER
Drug: lidocaine
Target: Sodium channel protein type 2 subunit alpha (Ion channel)
Gene: SCN2A
UniProt: Q99250 (SCN2A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: lidocaine
Target: Sodium channel protein type 3 subunit alpha (Ion channel)
Gene: SCN3A
UniProt: Q9NY46 (SCN3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.98
Action type: BLOCKER
Assay: Modulation of human Nav1.3 in open-inactivated state assessed as inhibition of inward current after 4 mins by whole-cell electrophysiology
Drug: lidocaine
Target: Sodium channel protein type 4 subunit alpha (Ion channel)
Gene: SCN4A
UniProt: P35499 (SCN4A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.7
Action type: BLOCKER
Assay: Modulation of human Nav1.4 in open-inactivated state assessed as inhibition of inward current after 4 mins by whole-cell electrophysiology
Drug: lidocaine
Target: Sodium channel protein type 9 subunit alpha (Ion channel)
Gene: SCN9A
UniProt: Q15858 (SCN9A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.54
Action type: BLOCKER
Assay: Modulation of human Nav1.7 in open-inactivated state assessed as inhibition of inward current after 4 mins by whole-cell electrophysiology
Drug: lidocaine
Target: 5-hydroxytryptamine receptor 3A (Ion channel)
Gene: HTR3A
UniProt: P46098 (5HT3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 3.296
Drug: lidocaine
Target: Sodium channel protein type 10 subunit alpha (Ion channel)
Gene: SCN10A
UniProt: Q9Y5Y9 (SCNAA_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: lidocaine
Target: Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 (Ion channel)
Gene: HCN4
UniProt: Q9Y3Q4 (HCN4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 3.559
Drug: lidocaine
Target: Acetylcholine receptor (Ion channel)
Gene: CHRNA1|CHRNB1|CHRND
UniProt: P02708|P11230|Q07001 (ACHA_HUMAN|ACHB_HUMAN|ACHD_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.955
Drug: lidocaine
Target: Sodium channel alpha subunits; brain (Types I, II, III) (Ion channel)
Gene: Scn1a|Scn2a|Scn3a
UniProt: P04774|P04775|P08104 (SCN1A_RAT|SCN2A_RAT|SCN3A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.25
Assay: Concentration required to inhibit [3H]BTX binding to Sodium channel of rat brain
Drug: lidocaine
Target: Sodium channel protein type X alpha subunit (Ion channel)
Gene: Scn10a
UniProt: Q62968 (SCNAA_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4
Action type: BLOCKER
Drug: lidocaine
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: Scn5a
UniProt: P15389 (SCN5A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.2
Action type: BLOCKER
Drug: lidoflazine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.8
Assay: Inhibitory concentration against potassium channel HERG
Drug: lidoflazine
Target: Equilibrative nucleoside transporter 1 (Transporter)
Gene: SLC29A1
UniProt: Q99808 (S29A1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.55
Assay: Inhibition of ENT1 in human K562 cells by flow cytometric assay
Drug: lidoflazine
Target: Sodium channel alpha subunits; brain (Types I, II, III) (Ion channel)
Gene: Scn1a|Scn2a|Scn3a
UniProt: P04774|P04775|P08104 (SCN1A_RAT|SCN2A_RAT|SCN3A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.11
Assay: Inhibition of [3H]- batrachotoxin binding to sodium channel in rat neocortical membrane
Drug: limaprost
Target: Prostaglandin E2 receptor EP1 subtype (GPCR)
Gene: PTGER1
UniProt: P34995 (PE2R1_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Drug: lincomycin
Target: 50S ribosomal protein L10 (Ribosomal protein)
Gene: rpl10
UniProt: P15825 (RL10_HALMA)
Organism: Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809)
Drug: lindane
Target: Gamma-aminobutyric acid receptor subunit beta-3 (Ion channel)
Gene: GABRB3
UniProt: P28472 (GBRB3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.05
Assay: Displacement of [3H]EBOB from recombinant Homo sapiens (human) GABA beta3 receptor
Drug: lindane
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.39
Assay: Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881)
Drug: lindane
Target: Gamma-aminobutyric acid receptor subunit beta (Ion channel)
Gene: Rdl
UniProt: Q75NA5 (GBRB_MUSDO)
Organism: Musca domestica
Activity: IC50 = 7.96
Assay: Inhibition of Musca domestica (house fly) GABA receptor
Drug: lindane
Target: Gamma-aminobutyric acid receptor subunit rho-1 (Ion channel)
Gene: GABRR1
UniProt: P24046 (GBRR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.04
Assay: Displacement of [3H]EBOB from recombinant Homo sapiens (human) GABA rho1 receptor
Drug: lindane
Target: GABA-A receptor alpha-1/beta-3/gamma-2 (Ion channel)
Gene: GABRA1|GABRG2|GABRB3
UniProt: P14867|P18507|P28472 (GBRA1_HUMAN|GBRG2_HUMAN|GBRB3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.68
Assay: Displacement of [3H]EBOB from recombinant Homo sapiens (human) GABA alpha1beta3gamma2 receptor
Drug: lindane
Target: GABA-A receptor (Ion channel)
Gene: Rdl1|Rdl2|Rdl3
UniProt: H9U2V9|H9U2W0|H9U2W1 (H9U2V9_TETUR|H9U2W0_TETUR|H9U2W1_TETUR)
Organism: Tetranychus urticae
Action type: NEGATIVE ALLOSTERIC MODULATOR
Assay: Mechanism of Action; CHEMBL2364024; PROTEIN COMPLEX GROUP
Drug: lindane
Target: GABA-A receptor (Ion channel)
UniProt: E0V9W2|E0VY07|E0W492 (E0V9W2_PEDHC|E0VY07_PEDHC|E0W492_PEDHC)
Organism: Pediculus humanus subsp. corporis
Action type: NEGATIVE ALLOSTERIC MODULATOR
Assay: Mechanism of Action; CHEMBL2364025; PROTEIN COMPLEX GROUP
Drug: lindane
Target: GABA-A receptor alpha-6/beta-3/gamma-2 (Ion channel)
Gene: GABRG2|GABRB3|GABRA6
UniProt: P18507|P28472|Q16445 (GBRG2_HUMAN|GBRB3_HUMAN|GBRA6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.31
Assay: Displacement of [3H]EBOB from recombinant Homo sapiens (human) GABA alpha6beta3gamma2 receptor
Drug: lindane
Target: GABA A receptor alpha-1/beta-1/gamma-2 (Ion channel)
Gene: GABRA1|GABRB1|GABRG2
UniProt: P14867|P18505|P18507 (GBRA1_HUMAN|GBRB1_HUMAN|GBRG2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.17
Assay: Displacement of [3H]EBOB from recombinant Homo sapiens (human) GABA alpha1beta1gamma2 receptor
Drug: linezolid
Target: Amine oxidase [flavin-containing] B (Enzyme)
Gene: MAOB
UniProt: P27338 (AOFB_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.5
Drug: linezolid
Target: Amine oxidase [flavin-containing] A (Enzyme)
Gene: MAOA
UniProt: P21397 (AOFA_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.1
Assay: Inhibition of MAO-A (unknown origin) by luciferase reporter gene assay
Drug: linezolid
Target: Amine oxidase [flavin-containing] B (Enzyme)
Gene: Maob
UniProt: P19643 (AOFB_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.77
Assay: Compound was evaluated for inhibition of Mono aminoxidase B in rat primary hepatocytes
Drug: linezolid
Target: Succinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrial (Enzyme)
Gene: SDHA
UniProt: P31040 (SDHA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.09
Assay: Inhibition of SDH-A (unknown origin) by ELISA
Drug: liothyronine
Target: Thyroid hormone receptor alpha (Nuclear hormone receptor)
Gene: THRA
UniProt: P10827 (THA_HUMAN)
Organism: Homo sapiens
Activity: Kd = 10.24
Action type: AGONIST
Assay: Displacement of [125I]T3 from human TRalpha receptor
Drug: liothyronine
Target: Thyroid hormone receptor beta (Nuclear hormone receptor)
Gene: THRB
UniProt: P10828 (THB_HUMAN)
Organism: Homo sapiens
Activity: Ki = 10.1
Action type: AGONIST
Assay: Inhibitory activity against [125I]T3 binding to human TRbeta1 receptor
Drug: liothyronine
Target: Adenosine receptor A1 (GPCR)
Gene: ADORA1
UniProt: P30542 (AA1R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.62
Assay: DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX)
Drug: liothyronine
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.301
Drug: liothyronine
Target: Thyroid hormone receptor beta (Transcription factor)
Gene: Thrb
UniProt: P18113 (THB_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.74
Assay: In vitro inhibition of the bound [125I]L-T3 rat liver nuclear L-triiodothyronine receptor
Drug: liothyronine
Target: Proliferating cell nuclear antigen (Nuclear other)
Gene: PCNA
UniProt: P12004 (PCNA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.44
Assay: Inhibition of human recombinant PCNA interaction with PIP box protein N-5-carboxyfluorescein-SAVLQKKITDYFHPKK after 30 mins by fluorescence polarization assay
Drug: liothyronine
Target: THAP domain-containing protein 1 (Unclassified)
Gene: THAP1
UniProt: Q9NVV9 (THAP1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 9
Drug: liothyronine
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: EC50 = 5.15
Assay: Non-competitive inhibitory activity against recombinant Gamma-aminobutyric acid A (GABA-A) receptor
Drug: liothyronine
Target: GABA-A receptor; anion channel (Ion channel)
Gene: GABRP|GABRD|GABRA1|GABRB1|GABRG2|GABRB3|GABRA5|GABRA3|GABRA2|GABRB2|GABRA4|GABRE|GABRA6|GABRG1|GABRG3|GABRQ
UniProt: O00591|O14764|P14867|P18505|P18507|P28472|P31644|P34903|P47869|P47870|P48169|P78334|Q16445|Q8N1C3|Q99928|Q9UN88 (GBRP_HUMAN|GBRD_HUMAN|GBRA1_HUMAN|GBRB1_HUMAN|GBRG2_HUMAN|GBRB3_HUMAN|GBRA5_HUMAN|GBRA3_HUMAN|GBRA2_HUMAN|GBRB2_HUMAN|GBRA4_HUMAN|GBRE_HUMAN|GBRA6_HUMAN|GBRG1_HUMAN|GBRG3_HUMAN|GBRT_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.64
Assay: Direct channel-gating action blocked by picrotoxin
Drug: lisinopril
Target: Angiotensin-converting enzyme (Enzyme)
Gene: ACE
UniProt: P12821 (ACE_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.92
Action type: INHIBITOR
Drug: lisinopril
Target: Angiotensin-converting enzyme (Enzyme)
Gene: ACE
UniProt: P12822 (ACE_RABIT)
Organism: Oryctolagus cuniculus
Activity: Ki = 7.29
Assay: Inhibition of rabbit testis recombinant ACE C domain
Drug: lisuride
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.491
Assay: DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug: lisuride
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.538
Assay: DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug: lisuride
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.11
Assay: Affinity towards Dopamine receptor D1
Drug: lisuride
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.3
Assay: Binding affinity towards Dopamine receptor D2 by displacement of [3H]U-86170.
Drug: lisuride
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.936
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: lisuride
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.4
Assay: Binding affinity towards Serotonin 5-hydroxytryptamine 1A receptor by displacement of [3H]-(+)-8-OH-DPAT.
Drug: lisuride
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.061
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: lisuride
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.3
Action type: AGONIST
Drug: lisuride
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.259
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: lisuride
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.3
Action type: ANTAGONIST
Drug: lisuride
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.625
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: lisuride
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.77
Assay: Binding affinity towards Dopamine receptor D3 by displacement of [3H](+)-7-OH-DPAT.
Drug: lisuride
Target: D(1B) dopamine receptor (GPCR)
Gene: DRD5
UniProt: P21918 (DRD5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.5
Action type: AGONIST
Drug: lisuride
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.721
Assay: DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug: lisuride
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.991
Assay: DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug: lisuride
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.7
Action type: AGONIST
Drug: lisuride
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9
Action type: AGONIST
Drug: lisuride
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.203
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: lisuride
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.796
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: lisuride
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.3
Action type: AGONIST
Drug: lisuride
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.037
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: lisuride
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki  7.78
Drug: lisuride
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.174
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: lisuride
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.338
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug: lisuride
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.64
Drug: lisuride
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Kd = 9.52
Assay: In vitro affinity at mutant D2 receptor (S194A) in C6 (glioma) cell membranes.
Drug: lisuride
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 9.33
Drug: lisuride
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32305 (5HT7R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.3
Action type: AGONIST
Drug: lisuride
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: Htr6
UniProt: P31388 (5HT6R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.3
Action type: AGONIST
Drug: lisuride
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.489
Action type: ANTAGONIST
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: lofepramine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.699
Drug: lofepramine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.155
Action type: INHIBITOR
Drug: lofepramine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.268
Action type: INHIBITOR
Drug: lofepramine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.337
Drug: lofepramine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.7
Drug: lofepramine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7
Drug: lofepramine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.444
Drug: lofepramine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.174
Drug: lofepramine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.481
Drug: lofepramine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.886
Drug: lofepramine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.468
Drug: lofepramine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.337
Drug: lofexidine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.9
Assay: Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in HeLa cells after 30 mins
Drug: lofexidine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.17
Assay: Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2B expressed in CHO cells
Drug: lofexidine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.16
Assay: Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells
Drug: lofexidine
Target: Nischarin (Unclassified)
Gene: Nisch
UniProt: Q4G017 (NISCH_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.25
Assay: Displacement of [125I]PIC from Imidazoline-1 receptor in rat PC12 cell membrane incubated for 30 mins by gamma counting method
Drug: lofexidine
Target: Adrenergic receptor alpha-2 (GPCR)
Gene: Adra2b|Adra2c|Adra2a
UniProt: P19328|P22086|P22909 (ADA2B_RAT|ADA2C_RAT|ADA2A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.6
Assay: Binding affinity against Alpha-2 adrenergic receptor is the ability to inhibit the specific [3H]clonidine binding (0.4 nM) to rat isolated brain membranes by 50% was reported; 2.5*10e-9
Drug: lofexidine
Target: Adrenergic receptor alpha-1 (GPCR)
Gene: Adra1b|Adra1d|Adra1a
UniProt: P15823|P23944|P43140 (ADA1B_RAT|ADA1D_RAT|ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.18
Assay: Binding affinity against alpha-1 adrenergic receptor is the ability to inhibit the specific [3H]prazosin binding (0.2 nM) to rat isolated brain membranes by 50% was reported; 6.6*10e-7
Drug: lofexidine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.36
Action type: AGONIST
Assay: Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells
Drug: lomefloxacin
Target: DNA gyrase subunit A (Enzyme)
Gene: gyrA
UniProt: P43700 (GYRA_HAEIN)
Organism: Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
Activity: IC50 = 5.15
Drug: lomefloxacin
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: lomerizine
Target: Voltage-dependent N-type calcium channel subunit alpha-1B (Ion channel)
Gene: CACNA1B
UniProt: Q00975 (CAC1B_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.61
Assay: Inhibition of calcium channel Cav2.2 in IMR32 cells
Drug: lonazolac
Target: Prostaglandin E synthase (Enzyme)
Gene: PTGES
UniProt: O14684 (PTGES_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.35
Assay: Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as inhibition of PGE2 formation from PGH2 after 15 mins by RP-HPLC analysis