| Assay ID | Title | Year | Journal | Article |
|---|
| 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. |
| AID591533 | Half life in CD rat at 3 mg/kg, po and 1 mg/kg, iv | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID687268 | Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging | 2012 | Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20
| Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists. |
| AID687271 | Antagonist activity at human adrenergic alpha1B receptor expressed in rat fibroblasts by by plate-based calcium imaging | 2012 | Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20
| Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists. |
| AID591515 | Binding affinity to human adrenergic Alpha-1B receptor expressed in rat intact fibroblasts | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID1331191 | Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay | 2016 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
| The discovery of quinoline based single-ligand human H |
| AID687266 | Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay | 2012 | Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20
| Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists. |
| AID591575 | Antiallergic rhinitis activity in conscious guinea pig assessed as duration of inhibition of histamine-induced nasal congestion at 0.1 to 1 mg/ml administered intranasally | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID1331184 | Antagonist activity at adrenergic alpha1A receptor (unknown origin) expressed in Rat1 cells assessed as inhibition of phenylephrine-induced Ca2+ flux preincubated for 30 mins followed by phenylephrine addition by Fluo-4-AM-dye based FLIPR assay | 2016 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
| The discovery of quinoline based single-ligand human H |
| AID591534 | Half life in Beagle dog at 3 mg/kg, po and 1 mg/kg, iv | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID687270 | Lipophilicity, log D of compound at pH 7.4 | 2012 | Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20
| Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists. |
| AID687267 | Antagonist activity at human H3 receptor expressed in CHO cells assessed as inhibition of histamine-induced GTPgamma[S] binding by scintillation proximity assay | 2012 | Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20
| Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists. |
| AID591574 | Time dependent inhibition of CYP2D6 | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591524 | Metabolic stability in human hepatocytes | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591522 | Cardiotoxicity in rabbit heart assessed as induction of QT interval prolongation | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591536 | Liver blood flow in CD rat at 3 mg/kg, po and 1 mg/kg, iv | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591567 | Ratio of drug level in brain to blood in CD rat at 1 mg/kg, iv | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591518 | Displacement of labeled dofetilide human ERG | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID1331187 | Displacement of [3H]-dofetilide from human ERG expressed in CHOK1 cell membranes incubated for 4 hrs in dark by luminescent assay | 2016 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
| The discovery of quinoline based single-ligand human H |
| AID591569 | Inhibition of CYP1A2 | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591573 | Time dependent inhibition of CYP3A4 | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591565 | Unchanged drug level in Beagle dog urine at 3 mg/kg, po and 1 mg/kg, iv after 24 hrs | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591526 | Metabolic stability in dog liver microsomes | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID687274 | Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay | 2012 | Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20
| Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists. |
| AID591562 | Oral bioavailability in CD rat at 3 mg/kg | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID1331189 | Antagonist activity at human Histamine H1 receptor expressed in CHO cells preincubated for 30 mins prior to histamine addition followed by subsequent washout and histamine challenge at 270 mins by Fluo-4 dye based FLIPR assay relative to azelastine | 2016 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
| The discovery of quinoline based single-ligand human H |
| AID591516 | Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID1331188 | Antagonist activity at human Histamine H1 receptor expressed in CHO cells preincubated for 30 mins prior to histamine addition followed by subsequent washout and histamine challenge at 90 mins by Fluo-4 dye based FLIPR assay relative to azelastine | 2016 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
| The discovery of quinoline based single-ligand human H |
| AID1331186 | Lipophilicity, logD of compound at pH 7.4 | 2016 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
| The discovery of quinoline based single-ligand human H |
| AID591517 | Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM incubated for 30 mins measured after washout followed by repeat histamine chal | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591571 | Inhibition of CYP2C19 | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591572 | Inhibition of CYP3A4 | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591528 | Clearance in Beagle dog at 3 mg/kg, po and 1 mg/kg, iv | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591520 | Binding affinity to human histamine H4 receptor | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID1331182 | Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay | 2016 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
| The discovery of quinoline based single-ligand human H |
| AID591563 | Oral bioavailability in Beagle dog at 3 mg/kg | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591513 | Antagonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as inhibition of histamine-induced GTP-gammaS binding | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591531 | Volume of distribution at steady state in Beagle dog at 3 mg/kg, po and 1 mg/kg, iv | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591521 | Inhibition of human ERG by patch clamp assay | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID692513 | Binding affinity to human histamine H1 receptor | 2011 | Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1
| Histamine H3 receptor as a drug discovery target. |
| AID687269 | Displacement of [3H]dofetilide from human ERG | 2012 | Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20
| Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists. |
| AID591514 | Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591537 | Liver blood flow in Beagle dog at 3 mg/kg, po and 1 mg/kg, iv | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591525 | Metabolic stability in rat liver microsomes | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591527 | Clearance in CD rat at 3 mg/kg, po and 1 mg/kg, iv | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591568 | Inhibition of CYP2D6 | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591530 | Volume of distribution at steady state in CD rat at 3 mg/kg, po and 1 mg/kg, iv | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591570 | Inhibition of CYP2C9 | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591519 | Binding affinity to human histamine H2 receptor | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID591512 | Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| AID1331185 | Antagonist activity at adrenergic alpha1B receptor (unknown origin) expressed in Rat1 cells assessed as inhibition of phenylephrine-induced Ca2+ flux preincubated for 30 mins followed by phenylephrine addition by Fluo-4-AM-dye based FLIPR assay | 2016 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
| The discovery of quinoline based single-ligand human H |
| AID1331183 | Antagonist activity at human Histamine H3 receptor expressed in CHO cell membranes assessed as inhibition of histamine-induced [35S]GTPgammaS binding after 2 to 6 hrs by scintillation proximity assay | 2016 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
| The discovery of quinoline based single-ligand human H |
| AID591523 | Metabolic stability in human liver microsomes | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |