Assay ID | Title | Year | Journal | Article |
AID738297 | Antagonist activity at sigma 2 receptor in human MCF7 cells assessed as effect on bradykinin-triggered Ca2+ response at 10 uM pretreated for 10 mins measured every 5 secs by fluorescence analysis | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
| Investigation of σ receptors agonist/antagonist activity through N-(6-methoxytetralin-1-yl)- and N-(6-methoxynaphthalen-1-yl)alkyl derivatives of polymethylpiperidines. |
AID641927 | Inhibition of human recombinant MAOA expressed in insect cells assessed as oxidation of kynuramine substrate at 2 mM measured after additional enzyme added after 120 mins incubation | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24
| Time-dependent slowly-reversible inhibition of monoamine oxidase A by N-substituted 1,2,3,6-tetrahydropyridines. |
AID231644 | Binding affinity ratio of sigma 1 receptor to that of sigma 2 receptor | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
| 4-(tetralin-1-yl)- and 4-(naphthalen-1-yl)alkyl derivatives of 1-cyclohexylpiperazine as sigma receptor ligands with agonist sigma2 activity. |
AID765139 | Displacement of [3H](+)-pentazocine from sigma 1 receptor in rat brain homogenates after 120 mins by liquid scintillation counting | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Effect of ring-constrained phenylpropyloxyethylamines on sigma receptors. |
AID256864 | Percentage inhibition of rat C6 glioma cell proliferation mediated by sigma 1 receptor at 50 uM | 2005 | Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
| Methyl substitution on the piperidine ring of N-[omega-(6-methoxynaphthalen-1-yl)alkyl] derivatives as a probe for selective binding and activity at the sigma(1) receptor. |
AID77183 | Inhibition of electrically stimulated contractions of the isolated guinea pig badder at 30 uM. | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
| 4-(tetralin-1-yl)- and 4-(naphthalen-1-yl)alkyl derivatives of 1-cyclohexylpiperazine as sigma receptor ligands with agonist sigma2 activity. |
AID203682 | In vitro binding affinity at opioid sigma-1 receptor in guinea pig brain membranes by (+)-[3H]pentazocine displacement. | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
| 4-(tetralin-1-yl)- and 4-(naphthalen-1-yl)alkyl derivatives of 1-cyclohexylpiperazine as sigma receptor ligands with agonist sigma2 activity. |
AID641841 | Inhibition of human recombinant MAOA expressed in insect cells assessed as oxidation of kynuramine substrate at 2 mM measured after additional substrate added after 90 mins incubation | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24
| Time-dependent slowly-reversible inhibition of monoamine oxidase A by N-substituted 1,2,3,6-tetrahydropyridines. |
AID641835 | Competitive inhibition of human recombinant MAO-A assessed as dissociation constant for enzyme-inhibitor complex by Lineweaver-Burk plot analysis | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24
| Time-dependent slowly-reversible inhibition of monoamine oxidase A by N-substituted 1,2,3,6-tetrahydropyridines. |
AID738302 | Antiproliferative activity against human MCF7 cells transfected with human sigma1 receptor after 48 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
| Investigation of σ receptors agonist/antagonist activity through N-(6-methoxytetralin-1-yl)- and N-(6-methoxynaphthalen-1-yl)alkyl derivatives of polymethylpiperidines. |
AID641832 | Selectivity index, ratio of IC50 for human recombinant MAOB to IC50 for human recombinant MAOA | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24
| Time-dependent slowly-reversible inhibition of monoamine oxidase A by N-substituted 1,2,3,6-tetrahydropyridines. |
AID348122 | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane without cerebellum | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Novel 4-(4-aryl)cyclohexyl-1-(2-pyridyl)piperazines as Delta(8)-Delta(7) sterol isomerase (emopamil binding protein) selective ligands with antiproliferative activity. |
AID1420180 | Cytotoxicity against human SH-SY5Y cells at 50 uM after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
| New piperidine-based derivatives as sigma receptor ligands. Synthesis and pharmacological evaluation. |
AID348128 | Cytotoxicity against human PC3 cells assessed as LDH release at 100 uM after 24 hrs relative to untreated control | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Novel 4-(4-aryl)cyclohexyl-1-(2-pyridyl)piperazines as Delta(8)-Delta(7) sterol isomerase (emopamil binding protein) selective ligands with antiproliferative activity. |
AID641830 | Inhibition of human recombinant MAOA expressed in insect cells using kynuramine substrate after 60 mins | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24
| Time-dependent slowly-reversible inhibition of monoamine oxidase A by N-substituted 1,2,3,6-tetrahydropyridines. |
AID349266 | Displacement of [3H]ditolylguanidine from sigma 2 opioid receptor in rat brain cerebellum | 2008 | European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
| Nitrile analogs of meperidine as high affinity and selective sigma-1 receptor ligands. |
AID641922 | Competitive inhibition of human recombinant MAO-A assessed as dissociation constant for enzyme-inhibitor-substrate complex by Lineweaver-Burk plot analysis | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24
| Time-dependent slowly-reversible inhibition of monoamine oxidase A by N-substituted 1,2,3,6-tetrahydropyridines. |
AID348121 | Displacement of [3H](-)-(S)-emopamil from EBP in guinea pig liver membrane | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Novel 4-(4-aryl)cyclohexyl-1-(2-pyridyl)piperazines as Delta(8)-Delta(7) sterol isomerase (emopamil binding protein) selective ligands with antiproliferative activity. |
AID204284 | Binding affinity for sigma-1 receptor by displacing [3H]-(+) pentazocine | 2002 | Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
| N-arylalkylpiperidines as high-affinity sigma-1 and sigma-2 receptor ligands: phenylpropylamines as potential leads for selective sigma-2 agents. |
AID348123 | Displacement of [3H]-DTG from sigma 2-type opioid receptor in rat liver membrane in presence of (+)-pentazocine | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Novel 4-(4-aryl)cyclohexyl-1-(2-pyridyl)piperazines as Delta(8)-Delta(7) sterol isomerase (emopamil binding protein) selective ligands with antiproliferative activity. |
AID765138 | Displacement of [3H]di-o-tolylguanidine from sigma 2 receptor in rat brain homogenates after 120 mins by liquid scintillation counting | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Effect of ring-constrained phenylpropyloxyethylamines on sigma receptors. |
AID1420188 | Cytotoxicity against human PANC1 cells at 50 uM after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
| New piperidine-based derivatives as sigma receptor ligands. Synthesis and pharmacological evaluation. |
AID348127 | Selectivity ratio of Ki for sigma 2 receptor in rat liver membrane to Ki for EBP in guinea pig liver membrane | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Novel 4-(4-aryl)cyclohexyl-1-(2-pyridyl)piperazines as Delta(8)-Delta(7) sterol isomerase (emopamil binding protein) selective ligands with antiproliferative activity. |
AID765137 | Selectivity ratio of Ki for sigma 2 receptor in rat brain homogenates to Ki for sigma 1 receptor in rat brain homogenates | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Effect of ring-constrained phenylpropyloxyethylamines on sigma receptors. |
AID203825 | In vitro binding affinity at opioid sigma-2 receptor in rat liver membranes by [3H]-DTG displacement in the presence of 1 uM (+)-pentazocine. | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
| 4-(tetralin-1-yl)- and 4-(naphthalen-1-yl)alkyl derivatives of 1-cyclohexylpiperazine as sigma receptor ligands with agonist sigma2 activity. |
AID348126 | Selectivity ratio of Ki for sigma 1 receptor in guinea pig brain membrane without cerebellum to Ki for EBP in guinea pig liver membrane | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Novel 4-(4-aryl)cyclohexyl-1-(2-pyridyl)piperazines as Delta(8)-Delta(7) sterol isomerase (emopamil binding protein) selective ligands with antiproliferative activity. |
AID349265 | Displacement of [3H](+)-pentazocine from sigma 1 opioid receptor in rat brain cerebellum | 2008 | European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
| Nitrile analogs of meperidine as high affinity and selective sigma-1 receptor ligands. |
AID35286 | In vitro binding affinity at alpha-1 adrenergic receptor in rat cortex by [3H]prazosin displacement. | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
| 4-(tetralin-1-yl)- and 4-(naphthalen-1-yl)alkyl derivatives of 1-cyclohexylpiperazine as sigma receptor ligands with agonist sigma2 activity. |
AID738303 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
| Investigation of σ receptors agonist/antagonist activity through N-(6-methoxytetralin-1-yl)- and N-(6-methoxynaphthalen-1-yl)alkyl derivatives of polymethylpiperidines. |
AID349267 | Selectivity ratio of Ki for rat sigma 2 opioid receptor to Ki for rat sigma 1 opioid receptor | 2008 | European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
| Nitrile analogs of meperidine as high affinity and selective sigma-1 receptor ligands. |
AID641831 | Inhibition of human recombinant MAOB expressed in insect cells using benzylamine hydrochloride as substrate after 30 mins | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24
| Time-dependent slowly-reversible inhibition of monoamine oxidase A by N-substituted 1,2,3,6-tetrahydropyridines. |
AID204308 | Binding affinity for sigma-2 receptor by displacing [3H]DTG in presence of dextrallorphan | 2002 | Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
| N-arylalkylpiperidines as high-affinity sigma-1 and sigma-2 receptor ligands: phenylpropylamines as potential leads for selective sigma-2 agents. |
AID5897 | In vitro binding affinity at serotonin 5-hydroxytryptamine 3 receptor in rat cortex by [3H]granisetron displacement. | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
| 4-(tetralin-1-yl)- and 4-(naphthalen-1-yl)alkyl derivatives of 1-cyclohexylpiperazine as sigma receptor ligands with agonist sigma2 activity. |
AID348125 | Antiproliferative activity against human PC3 cells expressing EBP at 100 uM after 48 hrs by MTT assay | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Novel 4-(4-aryl)cyclohexyl-1-(2-pyridyl)piperazines as Delta(8)-Delta(7) sterol isomerase (emopamil binding protein) selective ligands with antiproliferative activity. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |