AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: zotepine
Target: 5-hydroxytryptamine receptor 3A (Ion channel)
Gene: HTR3A
UniProt: P46098 (5HT3A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.326
Drug: zotepine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.301
Drug: zotepine
Target: 5-hydroxytryptamine receptor 5A (GPCR)
Gene: HTR5A
UniProt: P47898 (5HT5A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.538
Drug: zotepine
Target: 5-hydroxytryptamine receptor 1E (GPCR)
Gene: HTR1E
UniProt: P28566 (5HT1E_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.5
Action type: ANTAGONIST
Drug: zotepine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32305 (5HT7R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.8
Action type: ANTAGONIST
Drug: zotepine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: Htr6
UniProt: P31388 (5HT6R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.9
Action type: ANTAGONIST
Drug: zuclopenthixol
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Drug: zuclopenthixol
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.77
Assay: Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug: zuclopenthixol
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Drug: zuclopenthixol
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Drug: zuclopenthixol
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Drug: ziconotide
Target: Voltage-dependent N-type calcium channel subunit alpha-1B (Ion channel)
Gene: CACNA1B
UniProt: Q00975 (CAC1B_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: ziconotide
Target: Voltage-dependent N-type calcium channel subunit alpha-1B (Ion channel)
Gene: Cacna1b
UniProt: Q02294 (CAC1B_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 10.3
Action type: BLOCKER
Drug: ziconotide
Target: Voltage-dependent P/Q-type calcium channel subunit alpha-1A (Ion channel)
Gene: Cacna1a
UniProt: P54282 (CAC1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.3
Action type: BLOCKER
Drug: zotarolimus
Target: Peptidyl-prolyl cis-trans isomerase FKBP1A (Enzyme)
Gene: FKBP1A
UniProt: P62942 (FKB1A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.55
Action type: INHIBITOR
Drug: zotarolimus
Target: Serine/threonine-protein kinase mTOR (Kinase)
Gene: MTOR
UniProt: P42345 (MTOR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.48
Assay: Inhibitory activity against FKBP12
Drug: eledoisin
Target: Substance-P receptor (GPCR)
Gene: TACR1
UniProt: P25103 (NK1R_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.6
Action type: AGONIST
Drug: eledoisin
Target: Neuromedin-K receptor (GPCR)
Gene: TACR3
UniProt: P29371 (NK3R_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 9.66
Assay: Agonist activity at NK3R (unknown origin) transfected in CHO cells assessed as calcium influx at 10 mM
Drug: gonadorelin
Target: Gonadotropin-releasing hormone receptor (GPCR)
Gene: GNRHR
UniProt: P30968 (GNRHR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8
Action type: AGONIST
Assay: The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
Drug: gonadorelin
Target: Gonadotropin-releasing hormone receptor (GPCR)
Gene: Gnrhr
UniProt: P30969 (GNRHR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.7
Assay: Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
Drug: gonadorelin
Target: Lutropin-choriogonadotropic hormone receptor (GPCR)
Gene: Lhcgr
UniProt: P16235 (LSHR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.9
Drug: lypressin
Target: Vasopressin receptor (GPCR)
Gene: AVPR2|AVPR1A|AVPR1B
UniProt: P30518|P37288|P47901 (V2R_HUMAN|V1AR_HUMAN|V1BR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action; CHEMBL2363078; PROTEIN FAMILY
Drug: mifamurtide
Target: Nucleotide-binding oligomerization domain-containing protein 2 (Cytosolic other)
Gene: NOD2
UniProt: Q9HC29 (NOD2_HUMAN)
Organism: Homo sapiens
Action type: ACTIVATOR
Assay: Mechanism of Action
Drug: suramin
Target: NAD-dependent protein deacetylase sirtuin-1 (Enzyme)
Gene: SIRT1
UniProt: Q96EB6 (SIR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.52
Assay: Inhibition of recombinant SIRT1 using ZMAL substrate after 4 hrs by homogeneous fluorescence assay
Drug: suramin
Target: P2Y purinoceptor 6 (GPCR)
Gene: P2RY6
UniProt: Q15077 (P2RY6_HUMAN)
Organism: Homo sapiens
Activity: Kb = 4
Action type: ANTAGONIST
Drug: suramin
Target: P2Y purinoceptor 1 (GPCR)
Gene: P2RY1
UniProt: P47900 (P2RY1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.3
Action type: ANTAGONIST
Drug: suramin
Target: NAD-dependent protein deacetylase sirtuin-2 (Enzyme)
Gene: SIRT2
UniProt: Q8IXJ6 (SIR2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.96
Assay: Inhibition of recombinant SIRT2 using ZMAL substrate after 4 hrs by homogeneous fluorescence assay
Drug: suramin
Target: P2Y purinoceptor 2 (GPCR)
Gene: P2RY2
UniProt: P41231 (P2RY2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.3
Action type: ANTAGONIST
Drug: suramin
Target: P2Y purinoceptor 11 (GPCR)
Gene: P2RY11
UniProt: Q96G91 (P2Y11_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Action type: ANTAGONIST
Drug: suramin
Target: Protein arginine N-methyltransferase 1 (Enzyme)
Gene: PRMT1
UniProt: Q99873 (ANM1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.27
Assay: Inhibition of His6x-tagged PRMT1-mediated protein arginine methylation expressed in Escherichia coli BL21 (DE3) using H4(1-20) and [14C]-SAM by scintillation counting
Drug: suramin
Target: P2Y purinoceptor 13 (GPCR)
Gene: P2RY13
UniProt: Q9BPV8 (P2Y13_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.6
Action type: ANTAGONIST
Drug: suramin
Target: Reverse transcriptase/RNaseH (Enzyme)
Gene: pol
UniProt: Q72547 (Q72547_9HIV1)
Organism: Human immunodeficiency virus 1
Activity: IC50 = 5.03
Assay: Inhibition of purified HIV-1 reverse transcriptase
Drug: suramin
Target: DNA-dependent protein kinase catalytic subunit (Kinase)
Gene: PRKDC
UniProt: P78527 (PRKDC_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.77
Assay: Inhibitory activity against DNA-DNA dependent protein kinase (DNA-PK)
Drug: suramin
Target: RmtA (Enzyme)
Gene: rmtA
UniProt: Q5VLE3 (Q5VLE3_EMEND)
Organism: Emericella nidulans
Activity: IC50 = 5.23
Assay: Inhibition of Aspergillus nidulans recombinant GST-RmtA expressed in BL21 cells
Drug: suramin
Target: P2X purinoceptor 4 (Ion channel)
Gene: P2RX4
UniProt: Q99571 (P2RX4_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.749
Drug: suramin
Target: ATP-dependent 6-phosphofructokinase (Kinase)
Gene: pfk
UniProt: O15648 (PFKA_TRYBB)
Organism: Trypanosoma brucei brucei
Activity: IC50 = 5.52
Assay: Inhibition of Trypanosoma brucei PFK-mediated ADP production using ATP/fructose-6-phosphate as substrate by luciferase based luminescence assay
Drug: suramin
Target: Protein kinase C (PKC) (Kinase)
Gene: PRKD3|PRKCG|PRKCB|PRKCA|PRKCH|PRKCI|PRKCE|PRKCQ|PRKCZ|PRKCD|PRKD1
UniProt: O94806|P05129|P05771|P17252|P24723|P41743|Q02156|Q04759|Q05513|Q05655|Q15139 (KPCD3_HUMAN|KPCG_HUMAN|KPCB_HUMAN|KPCA_HUMAN|KPCL_HUMAN|KPCI_HUMAN|KPCE_HUMAN|KPCT_HUMAN|KPCZ_HUMAN|KPCD_HUMAN|KPCD1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.54
Assay: Inhibition of Protein kinase C (PKC)
Drug: suramin
Target: P2X purinoceptor 3 (Ion channel)
Gene: P2RX3
UniProt: P56373 (P2RX3_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.963
Drug: suramin
Target: NAD-dependent protein deacylase sirtuin-5, mitochondrial (Enzyme)
Gene: SIRT5
UniProt: Q9NXA8 (SIR5_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.85
Assay: Inhibition of human Sirt5 deacetylation activity using FKRGVL-acetylLys-EYGVKV as substrate after 60 mins by glutamate dehydrogenase-coupled assay
Drug: suramin
Target: Nucleoside triphosphate diphosphohydrolase 3 (Enzyme)
Gene: Entpd3
UniProt: Q80Z26 (Q80Z26_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.9
Assay: Inhibition of rat recombinant NTPDase3 expressed in CHO cells
Drug: suramin
Target: Ectonucleoside triphosphate diphosphohydrolase 2 (Enzyme)
Gene: Entpd2
UniProt: O35795 (ENTP2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.18
Assay: Inhibition of rat recombinant NTPDase2 expressed in CHO cells
Drug: suramin
Target: P2X purinoceptor 3 (Unclassified)
Gene: P2rx3
UniProt: P49654 (P2RX3_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.52
Action type: ANTAGONIST
Drug: suramin
Target: P2X purinoceptor 2 (Unclassified)
Gene: P2rx2
UniProt: P49653 (P2RX2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.98
Action type: ANTAGONIST
Drug: suramin
Target: P2X purinoceptor 1 (Unclassified)
Gene: P2rx1
UniProt: P47824 (P2RX1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6
Action type: ANTAGONIST
Drug: suramin
Target: P2X purinoceptor 5 (Unclassified)
Gene: P2rx5
UniProt: P51578 (P2RX5_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.4
Action type: ANTAGONIST
Drug: suramin
Target: Signal transducer and activator of transcription 1-alpha/beta (Unclassified)
Gene: STAT1
UniProt: P42224 (STAT1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.04
Assay: Inhibition of 5-carboxyfluorescein-GpYDKPHVL-OH binding to STAT1 (unknown origin) pre-incubated for 1 hr before fluorescent-labelled peptide addition by fluorescence polarization assay
Drug: suramin
Target: Signal transducer and activator of transcription 5A (Unclassified)
Gene: STAT5A
UniProt: P42229 (STA5A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.03
Assay: Inhibition of 5-carboxyfluorescein-GpYLVLDKW-OH binding to C-terminal 6x-His-tagged and an N-terminal maltose-binding protein-tagged STAT5A SH2 domain (137 to 507 residues) (unknown origin) expressed in Escherichia coli Rosetta BL21 DE3 pre-incubated for 1 hr before fluorescent-labelled peptide addition by fluorescence polarization assay
Drug: suramin
Target: Signal transducer and activator of transcription 5B (Unclassified)
Gene: STAT5B
UniProt: P51692 (STA5B_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.98
Assay: Inhibition of 5-carboxyfluorescein-GpYLVLDKW-OH binding to STAT5B SH2 domain (unknown origin) pre-incubated for 1 hr before fluorescent-labelled peptide addition by fluorescence polarization assay
Drug: triptorelin
Target: Gonadotropin-releasing hormone receptor (GPCR)
Gene: GNRHR
UniProt: P30968 (GNRHR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 9.025
Action type: AGONIST
Drug: triptorelin
Target: Gonadotropin-releasing hormone receptor (GPCR)
Gene: Gnrhr
UniProt: P30969 (GNRHR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.8
Action type: AGONIST
Drug: doxacurium
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Drug: doxacurium
Target: Neuronal acetylcholine receptor subunit alpha-2 (Ion channel)
Gene: CHRNA2
UniProt: Q15822 (ACHA2_HUMAN)
Organism: Homo sapiens
Drug: doxacurium
Target: Acetylcholine receptor (Ion channel)
Gene: CHRNA1|CHRNB1|CHRND
UniProt: P02708|P11230|Q07001 (ACHA_HUMAN|ACHB_HUMAN|ACHD_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Drug: histrelin
Target: Gonadotropin-releasing hormone receptor (GPCR)
Gene: GNRHR
UniProt: P30968 (GNRHR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action; CHEMBL1855; SINGLE PROTEIN
Drug: caspofungin
Target: Beta-1,3-glucan synthase catalytic subunit 1 (Enzyme)
Gene: GSC1
UniProt: O13428 (O13428_CANAX)
Organism: Candida albicans
Activity: IC50 = 8.89
Action type: INHIBITOR
Drug: caspofungin
Target: 1,3-beta-glucan synthase catalytic subunit FksP (Enzyme)
UniProt: Q4WLT4 (Q4WLT4_ASPFU)
Organism: Neosartorya fumigata (strain ATCC MYA-4609 / Af293 / CBS 101355 / FGSC A1100)
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2364674; SINGLE PROTEIN
Drug: caspofungin
Target: 1,3-beta-D-glucan synthase catalytic subunit (Unclassified)
Gene: CaFKS1
UniProt: O13383 (O13383_CANAX)
Organism: Candida albicans
Activity: IC50 = 9.62
Assay: Inhibition of wild type Candida albicans MY1055 1,3-beta-D-glucan synthase using UDP[6,3H]-glucose as substrate after 60 mins by liquid scintillation counting analysis
Drug: calcitonin (salmon synthetic)
Target: Amylin receptor AMY1 (GPCR)
Gene: CALCR|RAMP1
UniProt: P30988|O60894 (CALCR_HUMAN|RAMP1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.65
Action type: AGONIST
Assay: IC50 values for peptides in competition for 125I-labeled salmon CT binding to COS-7 cells cotransfected with 100 ng of hCTR and 100 ng of RAMP.
Drug: calcitonin (salmon synthetic)
Target: Amylin receptor AMY2 (GPCR)
Gene: CALCR|RAMP2
UniProt: P30988|O60895 (CALCR_HUMAN|RAMP2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.873
Action type: AGONIST
Assay: IC50 values for peptides in competition for 125I-labeled salmon CT binding to COS-7 cells cotransfected with 100 ng of hCTR and 100 ng of RAMP.
Drug: calcitonin (salmon synthetic)
Target: Amylin receptor AMY3 (GPCR)
Gene: CALCR|RAMP3
UniProt: P30988|O60896 (CALCR_HUMAN|RAMP3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.499
Action type: AGONIST
Assay: IC50 values for peptides in competition for 125I-labeled salmon CT binding to COS-7 cells cotransfected with 100 ng of hCTR and 100 ng of RAMP.
Drug: calcitonin (salmon synthetic)
Target: Calcitonin receptor (GPCR)
Gene: CALCR
UniProt: P30988 (CALCR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 11.086
Action type: AGONIST
Assay: Mechanism of Action
Drug: desirudin
Target: Prothrombin (Enzyme)
Gene: F2
UniProt: P00734 (THRB_HUMAN)
Organism: Homo sapiens
Activity: Ki = 12.7
Action type: INHIBITOR
Drug: glucagon
Target: Glucagon-like peptide 1 receptor (GPCR)
Gene: GLP1R
UniProt: P43220 (GLP1R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7
Action type: AGONIST
Drug: glucagon
Target: Glucagon receptor (GPCR)
Gene: GCGR
UniProt: P47871 (GLR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 9
Action type: AGONIST
Drug: glucagon
Target: Glucagon receptor (GPCR)
Gene: Gcgr
UniProt: P30082 (GLR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.82
Assay: Compound was tested for its ability to displace [125I]glucagon from the glucagon receptor
Drug: glucagon
Target: Adenylate cyclase (Enzyme)
Gene: Adcy1|Adcy3|Adcy2|Adcy4|Adcy8|Adcy6|Adcy5
UniProt: D4A3N4|P21932|P26769|P26770|P40146|Q03343|Q04400|Q8CFM9 (D4A3N4_RAT|ADCY3_RAT|ADCY2_RAT|ADCY4_RAT|ADCY8_RAT|ADCY6_RAT|ADCY5_RAT|Q8CFM9_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 8.23
Assay: Adenylate cyclase activity measured as 50% inhibitory concentration
Drug: glucagon
Target: Glucagon-like peptide 1 receptor (GPCR)
Gene: GLP1R
UniProt: F8V479 (F8V479_MACFA)
Organism: Macaca fascicularis
Activity: EC50 = 10.51
Assay: Agonist activity at monkey GLP1R expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
Drug: glucagon
Target: Glucagon-like peptide 1 receptor (GPCR)
Gene: Glp1r
UniProt: O35659 (GLP1R_MOUSE)
Organism: Mus musculus
Activity: EC50 = 10.36
Assay: Agonist activity at mouse GLP-1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
Drug: lepirudin
Target: Prothrombin (Enzyme)
Gene: F2
UniProt: P00734 (THRB_HUMAN)
Organism: Homo sapiens
Activity: Ki = 13
Action type: INHIBITOR
Drug: somatostatin
Target: Mu-type opioid receptor (GPCR)
Gene: Oprm1
UniProt: P33535 (OPRM_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.22
Assay: Inhibition of binding of [3H]-naloxone to Opioid receptor mu 1 of rat brain membranes
Drug: somatostatin
Target: Delta-type opioid receptor (GPCR)
Gene: Oprd1
UniProt: P33533 (OPRD_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.7
Assay: Inhibition of [3H]-DPDPE binding to Opioid receptor delta 1 of rat brain membranes
Drug: somatostatin
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: somatostatin
Target: Somatostatin receptor type 3 (GPCR)
Gene: Sstr3
UniProt: P30935 (SSR3_MOUSE)
Organism: Mus musculus
Activity: IC50 = 10.1
Assay: Tested for inhibition of radioligand binding to cloned somatostatin receptor mSSTR3
Drug: somatostatin
Target: Somatostatin receptor type 5 (GPCR)
Gene: Sstr5
UniProt: P30938 (SSR5_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 9.07
Assay: Tested for inhibition of radioligand binding to cloned somatostatin receptor rSSTR5
Drug: somatostatin
Target: Somatostatin receptor (GPCR)
Gene: Sstr5|Sstr1|Sstr2|Sstr3|Sstr4
UniProt: O08858|P30873|P30875|P30935|P49660 (SSR5_MOUSE|SSR1_MOUSE|SSR2_MOUSE|SSR3_MOUSE|SSR4_MOUSE)
Organism: Mus musculus
Activity: IC50 = 5.89
Assay: Compound was tested for its binding affinity against somatostatin receptors on AtT-20 cells
Drug: somatostatin
Target: Somatostatin receptor (GPCR)
Gene: Sstr1|Sstr2|Sstr3|Sstr4|Sstr5
UniProt: P28646|P30680|P30936|P30937|P30938 (SSR1_RAT|SSR2_RAT|SSR3_RAT|SSR4_RAT|SSR5_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 9.7
Assay: Compound was tested for its potency to displace 3-[125I]- - Tyr11-SRIF-14 from somatostatin receptor on membranes of rat cerebral cortex
Drug: somatostatin
Target: Somatostatin receptor type 2 (GPCR)
Gene: SSTR2
UniProt: P30874 (SSR2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 10.46
Action type: AGONIST
Assay: Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-2) subtype
Drug: somatostatin
Target: Somatostatin receptor type 3 (GPCR)
Gene: SSTR3
UniProt: P32745 (SSR3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 10
Action type: AGONIST
Assay: Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype
Drug: somatostatin
Target: Somatostatin receptor type 5 (GPCR)
Gene: SSTR5
UniProt: P35346 (SSR5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.85
Action type: AGONIST
Assay: Inhibition of human sst5 receptor expressed in CHO cells
Drug: somatostatin
Target: Somatostatin receptor type 4 (GPCR)
Gene: SSTR4
UniProt: P31391 (SSR4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.23
Action type: AGONIST
Assay: Inhibition of human sst4 receptor expressed in CHO cells
Drug: somatostatin
Target: Somatostatin receptor type 1 (GPCR)
Gene: SSTR1
UniProt: P30872 (SSR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.54
Action type: AGONIST
Assay: Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-1) subtype
Drug: pyrantel
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: O96529 (O96529_MELIC)
Organism: Meloidogyne incognita
Drug: atosiban
Target: Vasopressin V1a receptor (GPCR)
Gene: AVPR1A
UniProt: P37288 (V1AR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.82
Assay: Binding affinity to human vasopressin V1a receptor
Drug: atosiban
Target: Vasopressin V1b receptor (GPCR)
Gene: AVPR1B
UniProt: P47901 (V1BR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.36
Assay: Binding affinity to human vasopressin V1b receptor
Drug: atosiban
Target: Vasopressin V2 receptor (GPCR)
Gene: AVPR2
UniProt: P30518 (V2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.48
Assay: Binding affinity to human vasopressin V2 receptor
Drug: atosiban
Target: Oxytocin receptor (GPCR)
Gene: Oxtr
UniProt: P70536 (OXYR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.4
Drug: atosiban
Target: Oxytocin receptor (GPCR)
Gene: OXTR
UniProt: P30559 (OXYR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.96
Action type: ANTAGONIST
Assay: Binding affinity to human oxytocin receptor
Drug: oxybuprocaine
Target: Sodium channel protein type 10 subunit alpha (Ion channel)
Gene: SCN10A
UniProt: Q9Y5Y9 (SCNAA_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: oxybuprocaine
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 = 5.54
Action type: BLOCKER
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: benzethonium
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.934
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: benzethonium
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.051
Assay: DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole)
Drug: benzethonium
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.888
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: benzethonium
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.046
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: benzethonium
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.432
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: benzethonium
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.269
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: benzethonium
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.532
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: benzethonium
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.004
Assay: DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: benzethonium
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.69
Assay: DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: benzethonium
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.092
Assay: DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: benzethonium
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.444
Assay: DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: benzethonium
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.018
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: benzethonium
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.545
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: benzethonium
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.965
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: benzethonium
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P22303 (ACES_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.649
Assay: DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine)