Assay ID | Title | Year | Journal | Article |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347159 | Primary screen GU Rhodamine 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. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 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. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID616659 | Lipophilicity, log D of the compound | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| Novel and highly potent histamine H3 receptor ligands. Part 1: withdrawing of hERG activity. |
AID302569 | Clearance in rat at 1 mg/kg, iv | 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. |
AID302562 | Antagonist activity at human histamine H3 receptor expressed with Galphaq/i5 in HEL239 cells assessed as reduction of RAMH-induced intracellular calcium | 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. |
AID290795 | Binding affinity to human histamine H3 receptor | 2007 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
| A new class of histamine H3 receptor antagonists derived from ligand based design. |
AID616658 | Displacement of [125I]Iodoproxyfan from human recombinant histamine H3 receptor by Competitive binding assay | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| Novel and highly potent histamine H3 receptor ligands. Part 1: withdrawing of hERG activity. |
AID253633 | Area under plasma concentration curve of the compound upon p.o. dose of 1 mg/kg in rats | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
| Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency. |
AID302575 | Protein binding in dog plasma | 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. |
AID622483 | Displacement of [3H]-NAMH from human histamine H3 receptor expressed in CHO cells | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
| Synthesis and structure-activity relationships of 4,5-fused pyridazinones as histamine H₃ receptor antagonists. |
AID483431 | Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells | 2010 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
| In vitro studies on a class of quinoline containing histamine H3 antagonists. |
AID236518 | Clearance was observed in monkey 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. |
AID389212 | Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
| Synthesis and evaluation of structurally constrained quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists. |
AID237276 | Half life was observed in monkey 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. |
AID622486 | Displacement of [3H]-NAMH from rat histamine H3 receptor expressed in CHO cells | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
| Synthesis and structure-activity relationships of 4,5-fused pyridazinones as histamine H₃ receptor antagonists. |
AID341508 | Displacement of [3H]RAMH from human histamine H3 receptor expressed in CHO cells | 2008 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15
| Refinement of histamine H3 ligands pharmacophore model leads to a new class of potent and selective naphthalene inverse agonists. |
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. |
AID305748 | Displacement of [3H]N-alpha-methylhistamine from human cloned histamine H3 receptor expressed in C6 cells | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| 4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration. |
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. |
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. |
AID302572 | Ratio of drug level in brain to blood in mouse at 1 mg/kg, ip | 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. |
AID86612 | Binding potency was determined by displacement of [3H]N-alpha-methyl histamine from cloned human histamine H3 receptor expressed in C6 cells | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
| A new class of potent non-imidazole H(3) antagonists: 2-aminoethylbenzofurans. |
AID611518 | Displacement of [3H]NAMH from rat histamine H3 receptor expressed in CHO cells | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
AID692497 | Oral bioavailability in monkey at 1 mg/kg | 2011 | Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1
| Histamine H3 receptor as a drug discovery target. |
AID611517 | Displacement of [3H]NAMH from human histamine H3 receptor expressed in CHO cells | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
AID302560 | Displacement of [3H]-N-alpha methyl histamine from human H3 receptor expressed in C6 cells | 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. |
AID302574 | Ratio of drug level in brain to blood in rat at 1 mg/kg, iv | 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. |
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. |
AID780100 | Awakening activity in rat assessed as increased wakefulness at 10 mg/kg, po after 3 to 4 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. |
AID89863 | Binding potency was determined by displacement of [3H]N-alpha-methyl histamine from histamine H3 receptor of rat cortical membranes | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
| A new class of potent non-imidazole H(3) antagonists: 2-aminoethylbenzofurans. |
AID237553 | Volume of distribution was observed in dog 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. |
AID305753 | Clearance in rat brain at 1 mg/kg, iv | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| 4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration. |
AID305750 | Half life in rat at 1 mg/kg, iv | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| 4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration. |
AID236516 | Clearance was observed in dog 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. |
AID599203 | Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
| Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists. |
AID302563 | Antagonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as inhibition of RAMH-stimulated [35S]GTP-gamma-S binding | 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. |
AID244036 | Inhibition of CYP1A2 at 20 uM assessed by effect on rate of oxidation of phenacetin O-deethylation upon incubation with human liver microsomes | 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. |
AID253632 | Area under plasma concentration curve of the compound upon i.v. dose of 1 mg/kg in rats | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
| Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency. |
AID599205 | Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
| Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists. |
AID611522 | Bioavailability in fasted Sprague-Dawley rat at 1 mg/kg, iv after 6 to 24 hrs by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
AID305754 | Cmax in rat at 1 mg/kg, po | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| 4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration. |
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. |
AID244034 | Inhibition of CYP3A4 at 2 uM assessed by effect on rate of oxidation of terfenadine hydroxylation upon incubation with human liver microsomes | 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. |
AID244057 | Inhibition of CYP2D6 at 20 uM assessed by effect on rate of oxidation of dextromethorphan O-demethylation upon incubation with human liver microsomes | 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. |
AID692495 | Oral bioavailability in rat at 1 mg/kg | 2011 | Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1
| Histamine H3 receptor as a drug discovery target. |
AID237263 | Half life was observed in dog 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. |
AID305749 | Displacement of [3H]N-alpha-methylhistamine from histamine H3 receptor in rat cortical membranes | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| 4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration. |
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. |
AID236099 | Bioavailability in dog (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. |
AID305757 | Oral bioavailability in rat at 1 mg/kg | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| 4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration. |
AID302578 | Protein binding in rat plasma | 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. |
AID305756 | AUC (0 to infinity) in rat at 1 mg/kg, po | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| 4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration. |
AID616657 | Displacement of [3H]dofetilide from human recombinant ERG by Competitive binding assay | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| Novel and highly potent histamine H3 receptor ligands. Part 1: withdrawing of hERG activity. |
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. |
AID302564 | Antagonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as inhibition of RAMH-stimulated [35S]GTP-gamma-S binding | 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. |
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. |
AID244029 | Inhibition of CYP2A6 at 2 uM, assessed by effect on rate of oxidation of coumarin 7-hydroxylation upon incubation with human liver microsomes | 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. |
AID692496 | Oral bioavailability in dog at 1 mg/kg | 2011 | Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1
| Histamine H3 receptor as a drug discovery target. |
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. |
AID305752 | AUC (0 to infinity) in rat at 1 mg/kg, iv | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| 4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration. |
AID421582 | Displacement of [3H]N-alpha methyl histamine from human cloned histamine H3 receptor expressed in C6 cells | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
| Design of a new histamine H3 receptor antagonist chemotype: (3aR,6aR)-5-alkyl-1-aryl-octahydropyrrolo[3,4-b]pyrroles, synthesis, and structure-activity relationships. |
AID244037 | Inhibition of CYP2C9 at 20 uM assessed by its effect on rate of oxidation of Tolbutamide hydroxylation upon incubation with human liver microsomes | 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. |
AID421583 | Displacement of [3H]N-alpha methyl histamine from rat cortical membrane histamine H3 receptor | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
| Design of a new histamine H3 receptor antagonist chemotype: (3aR,6aR)-5-alkyl-1-aryl-octahydropyrrolo[3,4-b]pyrroles, synthesis, and structure-activity relationships. |
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. |
AID302573 | Drug level in rat brain at 1 mg/kg, iv | 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. |
AID302567 | Half life in rat at 1 mg/kg, iv | 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. |
AID302570 | Oral bioavailability in rat at 1 mg/kg | 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. |
AID244033 | Inhibition of CYP2C9 at 2 uM assessed by effect on rate of oxidation of Tolbutamide hydroxylation upon incubation with human liver microsomes | 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. |
AID244032 | Inhibition of CYP2A6 at 20 uM assessed by effect on rate of oxidation of coumarin 7-hydroxylation upon incubation with human liver microsomes | 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. |
AID611525 | Ratio of drug uptake in brain to plasma of fasted Sprague-Dawley rat at 1 mg/kg, iv after 6 to 24 hrs by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
AID89566 | Binding potency was determined by displacement of [3H]N-alpha-methyl histamine from histamine H3 receptor of rat cortical membranes | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
| A new class of potent non-imidazole H(3) antagonists: 2-aminoethylbenzofurans. |
AID305758 | Ratio of drug level in brain to plasma in rat at 5 mg/kg, iv | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| 4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration. |
AID302577 | Protein binding in monkey plasma | 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. |
AID237555 | Volume of distribution was observed in monkey 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. |
AID305755 | Half life in rat at 1 mg/kg, po | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| 4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration. |
AID302571 | Drug level in mouse brain at 1 mg/kg, ip | 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. |
AID302566 | Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding | 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. |
AID692493 | Binding affinity to rat cortical histamine H3 receptor | 2011 | Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1
| Histamine H3 receptor as a drug discovery target. |
AID244047 | Inhibition of CYP2E1 at 20 uM assessed by effect on rate of oxidation of chlorzoxazone 6-hydroxylation upon incubation with human liver microsomes | 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. |
AID611520 | Terminal half life in fasted Sprague-Dawley rat at 1 mg/kg, iv after 6 to 24 hrs by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
AID302561 | Displacement of [3H]-N-alpha methyl histamine from rat H3 receptor expressed in C6 cells | 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. |
AID86462 | Binding potency was determined by displacement of [3H]N-alpha-methyl histamine from cloned human histamine H3 receptor expressed in C6 cells | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
| A new class of potent non-imidazole H(3) antagonists: 2-aminoethylbenzofurans. |
AID244052 | Inhibition of CYP2C19 at 2 uM assessed by effect on rate of oxidation of S-mephenytoin 4'-hydroxylation upon incubation with human liver microsomes | 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. |
AID253550 | Oral bioavailability in rat (dose 1 mg/kg) | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
| Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency. |
AID254441 | In vitro binding affinity for human histamine H3 receptor using [3H]N-alpha-methylhistamine | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
| Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency. |
AID780098 | Awakening activity in rat assessed as decrease of theta rhythm at 10 mg/kg, po after 3 to 4 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. |
AID244056 | Inhibition of CYP2C19 at 20 uM assessed by effect on rate of oxidation of S-mephenytoin 4'-hydroxylation upon incubation with human liver microsomes | 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. |
AID244031 | Inhibition of CYP1A2 at 2 uM assessed by effect on rate of oxidation of phenacetin O-deethylation upon incubation with human liver microsomes | 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. |
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. |
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. |
AID244053 | Inhibition of CYP2D6 at 2 uM assessed by effect on rate of oxidation of dextromethorphan O-demethylation upon incubation with human liver microsomes | 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. |
AID236104 | Oral bioavailability in monkey (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. |
AID244044 | Inhibition of CYP2E1 at 2 uM assessed by effect on rate of oxidation of chlorzoxazone 6-hydroxylation upon incubation with human liver microsomes | 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. |
AID692494 | Binding affinity to human histamine H3 receptor | 2011 | Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1
| Histamine H3 receptor as a drug discovery target. |
AID253709 | Maximum plasma concentration upon p.o. dose of 1 mg/kg in rats | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
| Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency. |
AID611521 | Systemic clearance in fasted Sprague-Dawley rat at 1 mg/kg, iv after 6 to 24 hrs by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
AID302565 | Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding | 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. |
AID302576 | Protein binding in human plasma | 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. |
AID253809 | Terminal half life upon i.v. dose of 1 mg/kg in rats | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
| Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency. |
AID254439 | In vitro binding affinity for rat histamine H3 receptor using [3H]N-alpha-methylhistamine | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
| Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency. |
AID244038 | Inhibition of CYP3A4 at 20 uM assessed by effect on rate of oxidation of terfenadine hydroxylation upon incubation with human liver microsomes | 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. |
AID305751 | Volume of distribution in rat at terminal phase at 1 mg/kg, iv | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| 4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration. |
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. |
AID253810 | Terminal half life upon p.o. dose of 1 mg/kg in rats | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
| Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency. |
AID483430 | Displacement of [3H]N-alpha-methylhistamine from rat cloned histamine H3 receptor | 2010 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
| In vitro studies on a class of quinoline containing histamine H3 antagonists. |
AID302568 | Volume of distribution in rat at 1 mg/kg, iv | 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. |
AID375418 | Binding affinity to histamine H3 receptor | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
| 5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity. |
AID253576 | Plasma clearance upon i.v. dose of 1 mg/kg in rats | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
| Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency. |
AID483429 | Displacement of [3H]N-alpha-methylhistamine from human cloned histamine H3 receptor | 2010 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
| In vitro studies on a class of quinoline containing histamine H3 antagonists. |
AID483432 | Selectivity ratio of Ki for human cloned histamine H3 receptor over Ki for human ERG | 2010 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
| In vitro studies on a class of quinoline containing histamine H3 antagonists. |
AID1346037 | Human H1 receptor (Histamine receptors) | 2005 | The Journal of pharmacology and experimental therapeutics, Apr, Volume: 313, Issue:1
| Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties. |
AID1346017 | Rat H3 receptor (Histamine receptors) | 2005 | The Journal of pharmacology and experimental therapeutics, Apr, Volume: 313, Issue:1
| Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties. |
AID1346095 | Human H2 receptor (Histamine receptors) | 2005 | The Journal of pharmacology and experimental therapeutics, Apr, Volume: 313, Issue:1
| Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties. |
AID1346107 | Human H3 receptor (Histamine receptors) | 2005 | The Journal of pharmacology and experimental therapeutics, Apr, Volume: 313, Issue:1
| Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |