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sibutramine (CID 5210) - Compound BioActivity Data
.
BioActivity Outcomes:
Active(19)
 
 
Inactive(353)
 
 
Inconclusive(4)
 
 
Unspecified(156)
 
 
Top Targets:
7TM GPCR Srx(31)
 
 
 
 
7TM GPCR Srsx(27)
 
 
 
p450(9)
 
 
Tryp SPc(5)
 
 
 
CAP ED(5)
 
 
 
BioAssay Types:
Screening(248)
 
 
 
Confirmatory(98)
 
 
 
 
Literature(39)
 
 
 
 
BioActivity Types:
IC50(123)
 
 
 
 
Potency(89)
 
 
 
 
EC50(2)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 492    Data Row: 532   Total Pages: 11   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103498411]
IC50 0.632DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) [AID625256, Type: other]Sodium-dependent dopamine transporter [gi:266667]
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2
[SID103498411]
IC50 0.809DRUGMATRIX: Calcium Channel Type L, Benzothiazepine radioligand binding (ligand: [3H] Diltiazem) [AID625215, Type: other]
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3
[SID103498411]
IC50 2.085DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) [AID625222, Type: other]Sodium-dependent serotonin transporter [gi:400630]
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4
[SID103498411]
IC50 2.39DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) [AID625202, Type: other]Alpha-2B adrenergic receptor [gi:27151763]
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5
[SID103498411]
IC50 2.722DRUGMATRIX: Calcium Channel Type L, Phenylalkylamine radioligand binding (ligand: [3H] (-)-Desmethoxyverapamil (D-888)) [AID625234, Type: other]
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6
[SID103498411]
IC50 5.665DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) [AID625207, Type: other]Sodium-dependent noradrenaline transporter [gi:128616]
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7
[SID103498411]
EC50 8Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay [AID547622, Type: Literature]
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8
[SID103498411]
EC50 10Cytotoxicity against BESM cells after 88 hrs by HTS assay [AID547621, Type: Literature]
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9
[SID103498411]
Antiobesity activity in high fat diet-fed C57BL/6 mouse assessed as reduction in body weight at 3 mg/kg, po daily measured up to day 137 relative to control [AID661527, Type: Literature]
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10
[SID48416537]
DSSTox (FDAMDD) FDA Maximum (Recommended) Daily Dose Database [AID1195, Type: other]
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11
[SID49732001]
Counterscreen for inhibitors of AddAB: absorbance-based bacterial cell-based high throughput screening assay to identify inhibitors of bacterial viability [AID449728, Type: screening]
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12
[SID103498411]
Reduction of cumulative food intake in over-night fasted mouse at 10 mg/kg, ip after 3 hrs relative to control [AID307533, Type: Literature]
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13
[SID103498411]
Reduction in food intake in diet-induced obese Wistar rat chronic feeding model at 6 mg/kg, po once daily after 8 days [AID443391, Type: Literature]
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14
[SID49732001]
Counterscreen for AddAB inhibitors: absorbance-based bacterial cell-based high throughput confirmation assay for inhibitors of bacterial viability [AID488956, Type: screening]
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15
[SID49732001]
HTS to Find Inhibitors of Pathogenic Pemphigus Antibodies [AID588358, Type: screening]
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16
[SID49732001]
Absorbance-based primary bacterial cell-based high throughput screening assay to identify inhibitors of AddAB recombination protein complex [AID435030, Type: screening]hypothetical protein HP1089 [Helicobacter pylori 26695] [gi:15645703]
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17
[SID49732001]
Absorbance-based bacterial cell-based high throughput confirmation assay for inhibitors of AddAB recombination protein complex [AID488942, Type: screening]hypothetical protein HP1089 [Helicobacter pylori 26695] [gi:15645703]
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18
[SID49732001]
Absorbance-based bacterial cell-based high throughput confirmation assay for inhibitors of AddAB recombination protein complex [AID488942, Type: screening]recombination protein RecB [Helicobacter pylori 26695] [gi:15646160]
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19
[SID49732001]
Absorbance-based primary bacterial cell-based high throughput screening assay to identify inhibitors of AddAB recombination protein complex [AID435030, Type: screening]recombination protein RecB [Helicobacter pylori 26695] [gi:15646160]
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20
[SID103498411]
IC50 DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) [AID625203, Type: other]Alpha-2C adrenergic receptor [gi:20141211]
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21
[SID103498411]
IC50 DRUGMATRIX: Vasopressin V1A radioligand binding (ligand: [125I] PhenylacetylTyr(Me)PheGlnAsnArgProArgTyr) [AID625233, Type: other]Vasopressin V1a receptor [gi:586197]
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22
[SID103498411]
IC50 DRUGMATRIX: Protein Serine/Threonine Kinase, p38alpha enzyme inhibition (substrate: Myelin Basic Protein) [AID625182, Type: other]Mitogen-activated protein kinase 14 [gi:2499600]
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23
[SID103498411]
IC50 DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr)) [AID625184, Type: other]Epidermal growth factor receptor [gi:2811086]
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24
[SID103498411]
IC50 DRUGMATRIX: Peptidase, Angiotensin Converting Enzyme enzyme inhibition (substrate: FAPGG) [AID625173, Type: other]Angiotensin-converting enzyme [gi:2822103]
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25
[SID103498411]
IC50 DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) [AID625163, Type: other]Mu-type opioid receptor [gi:2851402]
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26
[SID103498411]
IC50 DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) [AID625248, Type: other]Cytochrome P450 2C9 [gi:6686268]
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27
[SID103498411]
IC50 DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) [AID625192, Type: other]5-hydroxytryptamine receptor 2A [gi:543727]
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28
[SID103498411]
IC50 DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) [AID625199, Type: other]Alpha-1B adrenergic receptor [gi:543734]
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29
[SID103498411]
IC50 DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA) [AID625195, Type: other]Adenosine receptor A2a [gi:543740]
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30
[SID103498411]
IC50 DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625155, Type: other]Muscarinic acetylcholine receptor M5 [gi:543761]
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31
[SID103498411]
IC50 DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol) [AID625258, Type: other]Estrogen receptor [gi:544257]
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32
[SID103498411]
IC50 DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) [AID625269, Type: other]Histamine H1 receptor [gi:547645]
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33
[SID103498411]
IC50 DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH) [AID625149, Type: other]Melanocortin receptor 5 [gi:729996]
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34
[SID103498411]
IC50 DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) [AID625217, Type: other]5-hydroxytryptamine receptor 2B [gi:1168220]
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35
[SID103498411]
IC50 DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) [AID625200, Type: other]Alpha-1D adrenergic receptor [gi:1168243]
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36
[SID103498411]
IC50 DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) [AID625198, Type: other]Alpha-1D adrenergic receptor [gi:1168244]
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37
[SID103498411]
IC50 DRUGMATRIX: Aldose Reductase enzyme inhibition (substrate: DL-Glyceraldehyde) [AID625208, Type: other]Aldose reductase [gi:1168407]
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38
[SID103498411]
IC50 DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1) [AID625237, Type: other]C-C chemokine receptor type 2 [gi:1168965]
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39
[SID103498411]
IC50 DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) [AID625254, Type: other]D(3) dopamine receptor [gi:1169206]
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40
[SID103498411]
IC50 DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) [AID625221, Type: other]5-hydroxytryptamine receptor 6 [gi:1703010]
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41
[SID103498411]
IC50 DRUGMATRIX: Angiotensin AT2 radioligand binding (ligand: [125I] CGP-42112A) [AID625209, Type: other]Type-2 angiotensin II receptor [gi:1703214]
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42
[SID103498411]
IC50 DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC) [AID625238, Type: other]C-C chemokine receptor type 4 [gi:1705894]
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43
[SID103498411]
IC50 DRUGMATRIX: Chemokine CCR5 radioligand binding (ligand: [125I] MIP-1alpha) [AID625239, Type: other]C-C chemokine receptor type 5 [gi:1705896]
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44
[SID103498411]
IC50 DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone) [AID625255, Type: other]D(4) dopamine receptor [gi:1345939]
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45
[SID103498411]
IC50 DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) [AID625201, Type: other]Alpha-2A adrenergic receptor [gi:1351829]
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46
[SID103498411]
IC50 DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) [AID625196, Type: other]Adenosine receptor A3 [gi:1351831]
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47
[SID103498411]
IC50 DRUGMATRIX: Chemokine CXCR2 (IL-8B) radioligand binding (ligand: [125I] IL-8) [AID625241, Type: other]C-X-C chemokine receptor type 2 [gi:1352454]
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48
[SID103498411]
IC50 DRUGMATRIX: Neuropeptide Y Y2 radioligand binding (ligand: [125I] Peptide YY) [AID625157, Type: other]Neuropeptide Y receptor type 2 [gi:1352610]
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49
[SID103498411]
IC50 DRUGMATRIX: Protein Serine/Threonine Phosphatase, PPP3CA (Calcineurin, PP2B) enzyme inhibition (substrate: DiFMUP) [AID625183, Type: other]Serine/threonine-protein phosphatase 2B catalytic subunit alpha isoform [gi:1352673]
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50
[SID103498411]
IC50 DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid) [AID625244, Type: other]Prostaglandin G/H synthase 2 [gi:3915797]
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