Assay ID | Title | Year | Journal | Article |
AID1346055 | Human H4 receptor (Histamine receptors) | 2004 | Biochemical pharmacology, Sep-01, Volume: 68, Issue:5
| Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist. |
AID1346107 | Human H3 receptor (Histamine receptors) | 2004 | Biochemical pharmacology, Sep-01, Volume: 68, Issue:5
| Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist. |
AID1346017 | Rat H3 receptor (Histamine receptors) | 2000 | British journal of pharmacology, Dec, Volume: 131, Issue:7
| Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain. |
AID1346107 | Human H3 receptor (Histamine receptors) | 2001 | The Biochemical journal, Apr-15, Volume: 355, Issue:Pt 2
| Genomic organization and characterization of splice variants of the human histamine H3 receptor. |
AID1346088 | Mouse H3 receptor (Histamine receptors) | 2004 | Journal of neurochemistry, Sep, Volume: 90, Issue:6
| Cloning and expression of the mouse histamine H3 receptor: evidence for multiple isoforms. |
AID1346095 | Human H2 receptor (Histamine receptors) | 2015 | Pharmacological reviews, Jul, Volume: 67, Issue:3
| International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors. |
AID1346107 | Human H3 receptor (Histamine receptors) | 2003 | The Journal of pharmacology and experimental therapeutics, Jun, Volume: 305, Issue:3
| Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects. |
AID1346017 | Rat H3 receptor (Histamine receptors) | 2003 | The Journal of pharmacology and experimental therapeutics, Jun, Volume: 305, Issue:3
| Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects. |
AID1346017 | Rat H3 receptor (Histamine receptors) | 2002 | European journal of pharmacology, Oct-18, Volume: 453, Issue:1
| Characteristics of recombinantly expressed rat and human histamine H3 receptors. |
AID1346017 | Rat H3 receptor (Histamine receptors) | 2004 | Biochemical pharmacology, Sep-01, Volume: 68, Issue:5
| Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist. |
AID1346107 | Human H3 receptor (Histamine receptors) | 2000 | British journal of pharmacology, Dec, Volume: 131, Issue:7
| Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain. |
AID1346107 | Human H3 receptor (Histamine receptors) | 2015 | Pharmacological reviews, Jul, Volume: 67, Issue:3
| International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors. |
AID1346017 | Rat H3 receptor (Histamine receptors) | 2001 | Biochemical and biophysical research communications, Jan-12, Volume: 280, Issue:1
| The rat H3 receptor: gene organization and multiple isoforms. |
AID1346107 | Human H3 receptor (Histamine receptors) | 2002 | European journal of pharmacology, Oct-18, Volume: 453, Issue:1
| Characteristics of recombinantly expressed rat and human histamine H3 receptors. |
AID1346055 | Human H4 receptor (Histamine receptors) | 2015 | Pharmacological reviews, Jul, Volume: 67, Issue:3
| International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors. |
AID1346037 | Human H1 receptor (Histamine receptors) | 2015 | Pharmacological reviews, Jul, Volume: 67, Issue:3
| International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors. |
AID1346055 | Human H4 receptor (Histamine receptors) | 2003 | The Journal of pharmacology and experimental therapeutics, Jun, Volume: 305, Issue:3
| Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects. |
AID1540200 | Inhibition of human AChE | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands. |
AID365358 | Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced response | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
AID1383056 | Binding affinity to human H3R | | | |
AID238933 | Antagonist potency against human H3 receptor in GTPgamma-S-Assay | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| 2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists. |
AID239591 | In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing human histamine H3 receptor | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. |
AID1810554 | Displacement of [3H]MSX-2 from human recombinant adenosine A2A receptor expressed in CHO cells at 1 uM by liquid scintillation counting analysis | | | |
AID365347 | Displacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cells | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
AID365345 | Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
AID365356 | Antagonist activity at human full length histamine H3 receptor expressed in HEK293 cells assessed as inhibition of (R)-alpha-methylhistamine-induced intracellular calcium release by FLIPR | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
AID1540197 | Inhibition of human histamine H3 receptor | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands. |
AID661878 | Binding affinity to human H3 receptor | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype. |
AID365357 | Antagonist activity at rat full length histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced intracellular calcium release by FLIPR | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
AID365355 | Antagonist activity at rat full length histamine H3 receptor expressed in HEK cells assessed as inhibition of forskolin-induced intracellular calcium release by SPA | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
AID365343 | Displacement of [3H]mepyramine from human histamine H1 receptor | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
AID1728998 | Agonist activity at C-terminal SmBit/mini-Gi protein-fused/N-terminal LgBit-tagged human H3R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by Nano-glo luminescence | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Structural modifications in the distal, regulatory region of histamine H |
AID725694 | Displacement of [3H]Nalpha-methylhistamine from human recombinant histamine H3 receptor expressed in HEK-293 cells | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
| Bodilisant-a novel fluorescent, highly affine histamine h3 receptor ligand. |
AID1729009 | Binding affinity to human H3R | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Structural modifications in the distal, regulatory region of histamine H |
AID597171 | Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9
| N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands. |
AID1057468 | Reversal of RAMH-induced dipsogenia in Lister Hooded rat at 3 mg/kg, po | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
| The discovery of the benzazepine class of histamine H3 receptor antagonists. |
AID236100 | Oral bioavailability in rat (dose 1-5 mg/kg i.v.) | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. |
AID365344 | Displacement of [3H]tiotidine from human histamine H2 receptor | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
AID239562 | In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing rat histamine H3 receptor | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. |
AID86456 | Antagonist potency against human histamine H3 receptor expressed in CHO cells was determined by GTPgamma-S-assay | 2004 | Journal of medicinal chemistry, May-20, Volume: 47, Issue:11
| 1-alkyl-4-acylpiperazines as a new class of imidazole-free histamine H(3) receptor antagonists. |
AID1545349 | Inhibition of human plasma butyrylcholinesterase by Ellman's method | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
| Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018). |
AID780102 | Awakening activity in rat assessed as increased wakefulness at 10 mg/kg, ip after 3 hrs | 2013 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22
| Discovery of a potent, selective, and orally bioavailable histamine H3 receptor antagonist SAR110068 for the treatment of sleep-wake disorders. |
AID1728994 | Displacement of [3H]UR-PI294 from human SP-FLAG-tagged H3R expressed in HEK293T cells measured after 60 to 120 mins by liquid scintillation counting analysis | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Structural modifications in the distal, regulatory region of histamine H |
AID86627 | In vivo effects in mice against H3 receptor on N6-methylhistamine levels in brain (following oral dosing of compound) | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
| Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(phenoxymethyl)benzyl)piperidines and related compounds. |
AID239987 | In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing rat histamine H3 receptor | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. |
AID365352 | Antagonist activity at human full length histamine H3 receptor expressed in HEK cells assessed as inhibition of [35S]gammaGTP binding relative to control | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
AID468419 | Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
| Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates. |
AID1810548 | Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells by liquid scintillation counting analysis | | | |
AID237820 | Concentration in brain of rats after 1 hr of intravenous administration | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. |
AID365349 | Displacement of [3H]LY278584 from 5HT2 receptor in rat frontal cortex | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
AID597172 | Displacement of [125I]iodoproxyfan from human full-length histamine H3 receptor expressed in HEK293 cells after 60 mins | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9
| N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands. |
AID597174 | Antagonist activity at histamine H3 receptor in po dosed 24 hrs fasted Swiss mouse brain assessed as t-MeHA level | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9
| N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands. |
AID89716 | In vitro inhibitory activity against Histamine H3 receptor for K+ evoked depolarization-induced release of [3H]histamine from synaptosomes of rat cerebral cortex | 2000 | Bioorganic & medicinal chemistry letters, Oct-16, Volume: 10, Issue:20
| Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists. |
AID1545350 | Displacement of [3H]-N-alpha-methylhistamine from human H3R expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
| Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018). |
AID86458 | Inhibition of [125I]iodoproxyfan binding to human histamine H3 receptor of CHO-K1 cells | 2001 | Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
| Different antagonist binding properties of human and rat histamine H3 receptors. |
AID1540204 | Inhibition of human BChE | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands. |
AID236517 | Clearance was observed in rat after intravenous administration of 1-5 mg/kg | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. |
AID365350 | Displacement of [3H]LY278584 from 5HT3 receptor in rat frontal cortex | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
AID1545348 | Inhibition of human acetylcholinesterase expressed in HEK 293 cells using acetylthiocholine iodide as substrate by Ellman's method | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
| Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018). |
AID1810550 | Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells by liquid scintillation counting analysis | | | |
AID1810551 | Displacement of [3H]PSB-11 from human recombinant adenosine A3 receptor expressed in CHO cells by liquid scintillation counting analysis | | | |
AID89708 | Histamine H3 receptor antagonist activity in an assay with K+ evoked depolarization-induced release of [3H]-histamine from rat synaptosomes. | 2000 | Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17
| New histamine H(3)-receptor ligands of the proxifan series: imoproxifan and other selective antagonists with high oral in vivo potency. |
AID1728993 | Inhibition of recombinant CYP3A4 (unknown origin) at 10 uM measured after 30 mins by luciferase reporter gene assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Structural modifications in the distal, regulatory region of histamine H |
AID1383054 | Inhibition of human MAO-B expressed in baculovirus infected insect cell membranes using kynuramine as substrate up to 30 mins by spectrophotometric method | | | |
AID1810555 | Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells at 1 uM by liquid scintillation counting analysis | | | |
AID1810549 | Displacement of [3H]MSX-2 from human recombinant adenosine A2A receptor expressed in CHO cells by liquid scintillation counting analysis | | | |
AID1057472 | Antagonist activity at human histamine H3 receptor expressed in CHOK1 cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
| The discovery of the benzazepine class of histamine H3 receptor antagonists. |
AID365354 | Antagonist activity at human full length histamine H3 receptor expressed in rat C6 cells assessed as inhibition of forskolin-induced cAMP release by SPA | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
AID88633 | In vivo Histamine H3 receptor antagonism, dose required to increase in N-t-methylhistamine levels in Swiss mice brains 90 min after p.o. administration | 2000 | Bioorganic & medicinal chemistry letters, Oct-16, Volume: 10, Issue:20
| Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists. |
AID1540203 | Inhibition of human MAOB | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands. |
AID1383055 | Inhibition of human MAO-A expressed in baculovirus infected insect cell membranes using kynuramine as substrate up to 30 mins by spectrophotometric method | | | |
AID1810553 | Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells at 1 uM by liquid scintillation counting analysis | | | |
AID130836 | In vivo potency on [3H]histamine level in mouse brain cortex at a dose of 3 mg/kg | 2002 | Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5
| Development of a new class of nonimidazole histamine H(3) receptor ligands with combined inhibitory histamine N-methyltransferase activity. |
AID365342 | Displacement of [3H]NAMH from histamine H3 receptor in rat cortex | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
AID86466 | Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressing CHO cells | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
| Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(phenoxymethyl)benzyl)piperidines and related compounds. |
AID131007 | Potency after oral administration in vivo in mice | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
| 4-(omega-(alkyloxy)alkyl)-1H-imidazole derivatives as histamine H(3) receptor antagonists/agonists. |
AID661879 | Selectivity ratio of Ki for human H3 receptor to Ki for rat H3 receptor | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
| Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype. |
AID237554 | Volume of distribution was observed in rat after intravenous administration of 1-5 mg/kg | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. |
AID89885 | Ratio of binding affinity of rat histamine H3 receptor to that of human histamine H3 receptor; 1:12 | 2001 | Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
| Different antagonist binding properties of human and rat histamine H3 receptors. |
AID239988 | In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing human histamine H3 receptor | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. |
AID365353 | Antagonist activity at rat full length histamine H3 receptor expressed in rat C6 cells assessed as inhibition of [35S]gammaGTP binding relative to control | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
AID1545346 | Inhibition of recombinant human MAOB expressed in baculovirus infected BTI insect cells using p-tyramine as substrate by Amplex red reagent/horseradish peroxidase coupled fluorescence assay | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
| Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018). |
AID365346 | Displacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cells | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
AID1057471 | Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
| The discovery of the benzazepine class of histamine H3 receptor antagonists. |
AID302579 | Memory enhancing effect in ip dosed adult rat by social recognition memory method | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| Synthesis, potency, and in vivo profiles of quinoline containing histamine H3 receptor inverse agonists. |
AID468415 | Displacement of [3H]iodoproxyfan from human histamine H3 receptor expressed in CHO-K1 cells | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
| Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates. |
AID131347 | Dose required to increase N-methyl-histamine levels in mouse brain cortex after perorally administration as an index of increased histaminergic neuron activity. | 2000 | Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17
| New histamine H(3)-receptor ligands of the proxifan series: imoproxifan and other selective antagonists with high oral in vivo potency. |
AID365340 | Displacement of [3H]NAMH from rat full length histamine H3 receptor expressed in rat C6 cells | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
AID1545345 | Inhibition of recombinant human MAOA expressed in baculovirus infected BTI insect cells using p-tyramine as substrate by Amplex red reagent/horseradish peroxidase coupled fluorescence assay | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
| Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018). |
AID1637854 | Reduction in food consumption in Wistar rat at 3 mg/kg, sc administered daily for 5 days relative to control | 2019 | MedChemComm, Feb-01, Volume: 10, Issue:2
| Design, synthesis, and |
AID1057470 | Binding affinity to human serum albumin | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
| The discovery of the benzazepine class of histamine H3 receptor antagonists. |
AID1728999 | Antagonist activity at C-terminal SmBit/mini-Gi protein-fused/N-terminal LgBit-tagged human H3R stably expressed in HEK293T cells assessed as inhibition of histamine-induced mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Structural modifications in the distal, regulatory region of histamine H |
AID1810556 | Displacement of [3H]PSB-11 from human recombinant adenosine A3 receptor expressed in CHO cells at 1 uM by liquid scintillation counting analysis | | | |
AID1810552 | Displacement of [3H] N-alpha methylhistamine from human recombinant histamine H3 receptor expressed in HEK293 cells measured after 90 mins | | | |
AID246007 | Tested for their ability to enhance memory in the adult rats using social recognition memory test | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. |
AID365341 | Displacement of [3H]NAMH from histamine H3 receptor in human cortex | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
AID239893 | Tested for its ability to block human histamine H3 receptor activation by the agonist R-alpha-methyl histamine in a [Ca2+] flux assay | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. |
AID89714 | In vitro binding affinity against rat histamine H3 receptor | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
| 4-(omega-(alkyloxy)alkyl)-1H-imidazole derivatives as histamine H(3) receptor antagonists/agonists. |
AID365339 | Displacement of [3H]NAMH from human full length histamine H3 receptor expressed in rat C6 cells | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
AID237264 | Half life was observed in rat after intravenous administration of 3-5 mg/kg; (n=3) | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. |
AID246006 | Lowest dose to induce CNS side effects was assessed in a general behavioral screen in rats | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. |
AID468416 | Selectivity, ratio of Ki for human histaminee H4 receptor to Ki for human histamine H3 receptor | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
| Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates. |
AID89562 | Inhibition of [125I]iodoproxyfan from rat histamine H3 receptor expressed in CHO-K1 cells | 2001 | Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
| Different antagonist binding properties of human and rat histamine H3 receptors. |
AID246008 | Tested for their ability to enhance learning in the rat pups using inhibitory avoidance acquisition model | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. |
AID365348 | Displacement of [3H]LY278584 from 5HT1 receptor in rat frontal cortex | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
AID1540202 | Inhibition of human MAOA | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands. |
AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500
| Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7
| Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | | | |
AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500
| Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500
| Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347059 | CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7
| Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7
| A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID1347151 | Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
| Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. |
AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7
| Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7
| A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID1347410 | qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library | 2019 | Cellular signalling, 08, Volume: 60 | A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening. |
AID588378 | qHTS for Inhibitors of ATXN expression: Validation | | | |
AID1798786 | Radioligand Binding Assay from Article 10.1021/jm8003625: \\The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.\\ | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |