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L 744832 (CID 6918276) - Compound BioActivity Data
.
BioActivity Outcomes:
Active(17)
 
 
Unspecified(123)
 
 
Top Targets:
7TM GPCR Srx(17)
 
 
 
7TM GPCR Srsx(15)
 
 
 
p450(8)
 
 
 
NR LBD ER(2)
 
 
STKc ERK1 2 l..(2)
 
 
BioAssay Types:
Literature(8)
 
 
 
BioActivity Types:
IC50(119)
 
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 140    Data Row: 140   Total Pages: 3   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID104242266]
IC50 0.027Inhibition of FTase [AID587820, Type: Literature]
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2
[SID104242266]
IC50 0.028DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) [AID625254, Type: other]D(3) dopamine receptor [gi:1169206]
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3
[SID104242266]
IC50 0.122DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH) [AID625149, Type: other]Melanocortin receptor 5 [gi:729996]
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4
[SID104242266]
IC50 0.157DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) [AID625253, Type: other]D(2) dopamine receptor [gi:118206]
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5
[SID104242266]
IC50 0.432DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) [AID625201, Type: other]Alpha-2A adrenergic receptor [gi:1351829]
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6
[SID104242266]
IC50 0.54DRUGMATRIX: Sodium Channel, Site 2 radioligand binding (ligand: [3H] Batrachotoxin) [AID625225, Type: other]
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7
[SID104242266]
IC50 0.7DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) [AID625249, Type: other]Cytochrome P450 2D6 [gi:84028191]
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8
[SID104242266]
IC50 0.813DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr)) [AID625185, Type: other]Tyrosine-protein kinase Fyn [gi:125370]
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9
[SID104242266]
IC50 1.609DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) [AID625227, Type: other]Substance-K receptor [gi:229462950]
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10
[SID104242266]
IC50 3DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin) [AID625251, Type: other]Cytochrome P450 3A4 [gi:116241312]
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11
[SID104242266]
IC50 3.136DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) [AID625203, Type: other]Alpha-2C adrenergic receptor [gi:20141211]
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12
[SID104242266]
IC50 3.216DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr)) [AID625184, Type: other]Epidermal growth factor receptor [gi:2811086]
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13
[SID104242266]
IC50 3.395DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH) [AID625147, Type: other]Melanocortin receptor 3 [gi:395398606]
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14
[SID104242266]
IC50 3.568DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625152, Type: other]Muscarinic acetylcholine receptor M2 [gi:113122]
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15
[SID104242266]
IC50 3.568DRUGMATRIX: Calcium Channel Type L, Benzothiazepine radioligand binding (ligand: [3H] Diltiazem) [AID625215, Type: other]
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16
[SID104242266]
IC50 4.501DRUGMATRIX: Calcium Channel Type L, Dihydropyridine radioligand binding (ligand: [3H] Nitrendipine) [AID625216, Type: other]
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17
[SID104242266]
Induction of disorganization of tubulin in human PC3 cells assessed as microtuble bundles at 75 uM after 24 hrs by immunofluorescence microscopy [AID587825, Type: Literature]
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18
[SID104242266]
IC50 75Anticancer activity against hormone-resistant human PC3 cells assessed as cell proliferation after 72 hrs by MTT assay [AID587817, Type: Literature]
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19
[SID104242266]
IC50 78Anticancer activity against hormone-resistant human DU145 cells assessed as cell proliferation after 72 hrs by MTT assay [AID587816, Type: Literature]
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20
[SID104242266]
Concentration causing regression of MMTV-v-Ras mice bearing palpable tumors [AID109686, Type: Literature]
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21
[SID104242266]
Antiproliferative activity against human PC3 cells at 10 uM after 120 hrs by MTT assay relative to DMSO [AID503311, Type: Literature]
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22
[SID104242266]
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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23
[SID104242266]
IC50 DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) [AID625200, Type: other]Alpha-1D adrenergic receptor [gi:1168243]
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24
[SID104242266]
IC50 DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) [AID625198, Type: other]Alpha-1D adrenergic receptor [gi:1168244]
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25
[SID104242266]
IC50 DRUGMATRIX: Aldose Reductase enzyme inhibition (substrate: DL-Glyceraldehyde) [AID625208, Type: other]Aldose reductase [gi:1168407]
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26
[SID104242266]
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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27
[SID104242266]
IC50 DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) [AID625196, Type: other]Adenosine receptor A3 [gi:1351831]
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28
[SID104242266]
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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29
[SID104242266]
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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30
[SID104242266]
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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31
[SID104242266]
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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32
[SID104242266]
IC50 DRUGMATRIX: Angiotensin AT2 radioligand binding (ligand: [125I] CGP-42112A) [AID625209, Type: other]Type-2 angiotensin II receptor [gi:1703214]
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33
[SID104242266]
IC50 DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC) [AID625238, Type: other]C-C chemokine receptor type 4 [gi:1705894]
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34
[SID104242266]
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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35
[SID104242266]
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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36
[SID104242266]
IC50 DRUGMATRIX: Bradykinin B2 radioligand binding (ligand: [3H] Bradykinin) [AID625213, Type: other]B2 bradykinin receptor [gi:2506481]
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37
[SID104242266]
IC50 DRUGMATRIX: Peptidase, Angiotensin Converting Enzyme enzyme inhibition (substrate: FAPGG) [AID625173, Type: other]Angiotensin-converting enzyme [gi:2822103]
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38
[SID104242266]
IC50 DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) [AID625163, Type: other]Mu-type opioid receptor [gi:2851402]
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39
[SID104242266]
IC50 DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid) [AID625244, Type: other]Prostaglandin G/H synthase 2 [gi:3915797]
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40
[SID104242266]
IC50 DRUGMATRIX: Estrogen ERbeta radioligand binding (ligand: [3H] Estradiol) [AID625259, Type: other]Estrogen receptor beta [gi:6166154]
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41
[SID104242266]
IC50 DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808) [AID625220, Type: other]5-hydroxytryptamine receptor 4 [gi:6224984]
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42
[SID104242266]
IC50 DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) [AID625248, Type: other]Cytochrome P450 2C9 [gi:6686268]
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43
[SID104242266]
IC50 DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) [AID625171, Type: other]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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44
[SID104242266]
IC50 DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4) [AID625145, Type: other]Cysteinyl leukotriene receptor 1 [gi:20138087]
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45
[SID104242266]
IC50 DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625154, Type: other]Muscarinic acetylcholine receptor M4 [gi:23503039]
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46
[SID104242266]
IC50 DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) [AID625202, Type: other]Alpha-2B adrenergic receptor [gi:27151763]
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47
[SID104242266]
DRUGMATRIX: Protein Tyrosine Phosphatase, PTPRC (CD45) enzyme inhibition (substrate: DiFMUP) [AID625188, Type: other]Receptor-type tyrosine-protein phosphatase C [gi:33112650]
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48
[SID104242266]
IC50 DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) [AID625204, Type: other]Beta-1 adrenergic receptor [gi:48429211]
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49
[SID104242266]
IC50 DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH) [AID625148, Type: other]Melanocortin receptor 4 [gi:60392672]
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50
[SID104242266]
IC50 DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) [AID625247, Type: other]Cytochrome P450 2C19 [gi:60416369]
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