Assay ID | Title | Year | Journal | Article |
AID1337900 | Analgesic activity in Swiss CD1 mouse assessed reduction in formalin-induced inflammatory pain by measuring reduction in time spent in licking or biting formalin injected hind paw at 3 mg/kg, ip pretreated for 30 mins followed by formalin injection measur | | | |
AID4418 | Compound was tested for inhibition constant against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes. | 1998 | Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
| Functional characteristics of a series of N4-substituted 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazines as 5-HT1A receptor ligands. Structure-activity relationships. |
AID192922 | Ability to counteract the 8-OH-DPAT (1 mg/kg sc)-induced Hypothermia in rats (n=4) and evaluated for the decrease in body temperature (degrees Celsius) at 0.1(micro mol/kg) | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
| Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635. |
AID481374 | Half life in human liver microsomes at 1 uM after 20 mins | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
| The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists. |
AID597359 | Octanol-water partition coefficient, log D of the compound at pH 7.4 by HPLC analysis | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID1830042 | Displacement of [3H]5-CT from human recombinant 5-HT7A receptor expressed in HEK cells by radioligand completion assay | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
| Activity of |
AID597306 | Inhibition of adrenergic Alpha-2C receptor at 10 uM | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID17425 | Biodistribution of the [11C]-radiolabeled compound in rat cerebellum | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| Development of fluorine-18-labeled 5-HT1A antagonists. |
AID239801 | Binding affinity for alpha 1d adrenoceptor | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
| Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses. |
AID79314 | Ability to antagonize the 8-OH-DPAT-induced contractions of a strip of guinea pig ileum tissue | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
| Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635. |
AID17427 | Biodistribution of the [11C]-radiolabeled compound in rat cortex | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| Development of fluorine-18-labeled 5-HT1A antagonists. |
AID597314 | Inhibition of 5HT1A receptor | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID1601988 | Induction of hypothermia in CD-1 mouse assessed as change in body temperature at 0.1 mg/kg, sc measured after 30 mins by thermometric method (Rvb <= 0.4 deg C) | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
AID726708 | Ratio of drug level in brain to plasma at steady state in rat at 1000 ng/g after 5 hrs | 2013 | Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
| Discovery of novel α₁-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands. |
AID510389 | Displacement [3H]prazosin of human recombinant Alpha-1B adrenergic receptor expressed in CHO cells by rapid filtration technique | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
| 1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors. |
AID1713196 | Inhibition of 8-OH-DPAT-induced hypothermia in Swiss albino mouse assessed as change in rectal body temperature at 0.3 mg/kg, sc pretreated with compound for 45 mins followed by 8-OH-DPAT challenge and measured after 45 min by thermometer (Rvb = -1.3 degr | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
| Synthesis and biological investigation of new equatorial (β) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile. |
AID1517951 | Induction of hypothermia in CD-1 mouse assessed as change in body temperature at 0.1 mg/kg, ip measured after 120 mins by thermometric method (Rvb = -0.1 to 0.3 deg C) | | | |
AID597302 | Inhibition of adrenergic beta3 receptor at 10 uM | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID1713195 | Inhibition of 8-OH-DPAT-induced hypothermia in Swiss albino mouse assessed as change in rectal body temperature at 0.3 mg/kg, sc pretreated with compound for 45 mins followed by 8-OH-DPAT challenge and measured after 30 min by thermometer (Rvb = -1.7 degr | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
| Synthesis and biological investigation of new equatorial (β) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile. |
AID37309 | Binding affinity against rat cortical alpha-1 adrenergic receptor labeled with [3H]prazosin radioligand | 2004 | Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
| Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines. |
AID726716 | Efflux ratio of apparent permeability from basolateral to apical side over apical to basolateral side in human Caco2 cells at 1 to 20 uM | 2013 | Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
| Discovery of novel α₁-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands. |
AID1593196 | Displacement of [3H]Prazosin from human recombinant alpha 1B adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay | | | |
AID1365313 | In-vivo 5-HT1A receptor antagonist activity in Swiss albino mouse assessed as reduction in 8-OH-DPAT-stimulated induction of lower lip retraction by measuring lower lip retraction score at 0.3 mg/kg, ip dosed 15 mins before test (Rvb = 2.875 +/- 0.08183 N | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
| New 5-HT |
AID3922 | Binding affinity at human 5-hydroxytryptamine 1A receptor by inhibition of [3H]8-OH-DPAT binding in Chinese hamster ovary cell line | 2002 | Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
| Improvement in the selectivity and metabolic stability of the serotonin 5-HT(1A) ligand, S 15535: a series of cis- and trans-2-(arylcycloalkylamine) 1-indanols. |
AID17429 | Biodistribution of the [11C]-radiolabeled compound in rat hippocampus | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| Development of fluorine-18-labeled 5-HT1A antagonists. |
AID239800 | Binding affinity for alpha 1b adrenoceptor | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
| Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses. |
AID193028 | Ability to counteract the 8-OH-DPAT (1 mg/kg sc)-induced Hypothermia in rats (n=4) and evaluated for the decrease in body temperature (degrees Celsius) at 10(micro mol/kg) | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
| Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635. |
AID481370 | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
| The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists. |
AID309503 | Effect on 8-OH-DPAT-induced lower lip retraction in Wistar rat at 0.1 mg/kg | 2007 | Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22
| The influence of modifications in imide fragment structure on 5-HT(1A) and 5-HT(7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl)piperazines. |
AID597310 | Inhibition of dopamine D4 receptor | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID1517941 | Induction of hypothermia in CD-1 mouse assessed as change in body temperature at 0.1 mg/kg, ip measured after 60 mins by thermometric method (Rvb = -0.2 to 0.5 deg C) | | | |
AID597320 | Inhibition of adrenergic alpha2B receptor at 10 uM | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID226695 | In vitro affinity against 5-HT1B/1D receptor using [3H]5-HT in calf striatum | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
| Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635. |
AID17428 | Biodistribution of the [11C]-radiolabeled compound in rat cortex co-injected with 50 nM of WAY 100635. | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| Development of fluorine-18-labeled 5-HT1A antagonists. |
AID1555769 | Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1B expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counter | 2019 | European journal of medicinal chemistry, Aug-15, Volume: 176 | 1,3-Dioxane as a scaffold for potent and selective 5-HT |
AID510388 | Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
| 1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors. |
AID6432 | Receptor-linked G protein activation at 5-hydroxytryptamine receptor was determined by measuring the stimulation of [35S]GTP-gamma-S, binding (Experiment 1) | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| Development of fluorine-18-labeled 5-HT1A antagonists. |
AID309481 | Decrease in body temperature in Swiss Albino mouse at 0.1 mg/kg after 90 mins | 2007 | Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22
| The influence of modifications in imide fragment structure on 5-HT(1A) and 5-HT(7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl)piperazines. |
AID481372 | Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as maximal blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
| The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists. |
AID87452 | Percent increase in the Forskolin-Stimulated cAMP formation, in HeLa cells transfected with the 5-HT 1A receptor at 1 uM concentration | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants. |
AID231744 | Ratio of biodistribution of compound at cortex and cerebellum-1 in rat with 200 nmol of WAY 100635 | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| Development of fluorine-18-labeled 5-HT1A antagonists. |
AID1854976 | Binding affinity to 5-HT1A receptor (unknown origin) assessed as dissociation constant | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
| Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors. |
AID87447 | Effect (1 uM) on Forskolin-Stimulated cAMP formation, in HeLa cells transfected with the 5-HT 1A receptor | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants. |
AID597282 | Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 EBNA cells after 1 hr by liquid scintillation counting | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID17431 | Biodistribution of the [11C]-radiolabeled compound in rat hypothalamus | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| Development of fluorine-18-labeled 5-HT1A antagonists. |
AID1517936 | Induction of hypothermia in CD-1 mouse assessed as change in body temperature at 0.1 mg/kg, ip measured after 30 mins by thermometric method (Rvb = -0.2 to 0.4 deg C) | | | |
AID1830038 | Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
| Activity of |
AID3884 | Agonist efficacy of [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor compared to 5-HT | 2002 | Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
| Improvement in the selectivity and metabolic stability of the serotonin 5-HT(1A) ligand, S 15535: a series of cis- and trans-2-(arylcycloalkylamine) 1-indanols. |
AID597303 | Inhibition of adrenergic beta2 receptor at 10 uM | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID204533 | Binding affinity against serotonin transporter in rat cortical tissues using radioligand [3H]paroxetine | 2004 | Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
| Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines. |
AID408276 | Displacement of [3H]WAY100635 from human recombinant 5HT1A receptor | 2008 | Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
| Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists. |
AID3752 | In vitro affinity against 5-hydroxytryptamine 1A receptor using [3H]-8-OH-DPAT in rat hippocampus | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
| Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635. |
AID204069 | Inhibition concentration against [3H]5-HT uptake by human serotonin transporter in JAR cells | 2004 | Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
| Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines. |
AID17430 | Biodistribution of the [11C]-radiolabeled compound in rat hippocampus co-injected with 50 nM of WAY 100635. | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| Development of fluorine-18-labeled 5-HT1A antagonists. |
AID1854984 | Binding affinity to D4 receptor (unknown origin) assessed as dissociation constant | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
| Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors. |
AID17426 | Biodistribution of the [11C]-radiolabeled compound in rat cerebellum co-injected with 50 nM of WAY 100635. | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| Development of fluorine-18-labeled 5-HT1A antagonists. |
AID597309 | Inhibition of adrenergic Alpha-1D receptor | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID1704732 | Antagonist activity at human 5HT1A receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux at 10 uM incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 | | | |
AID1365297 | Inhibition of 8-OH-DPAT-induced hypothermia in Swiss albino mouse at 0.1 mg/kg, ip measured after 120 mins post dose co-treated with 8-OH-DPAT | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
| New 5-HT |
AID3758 | In vitro binding affinity to 5-hydroxytryptamine 1A receptor using [125I](R)-(+)-trans-8-OH-PIPAT as radioligand in rat hippocampal homogenate | 1994 | Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26
| Derivatives of 4-(2'-methoxyphenyl)-1-[2'-(N-2"-pyridinyl-p-iodobenzamido)ethyl]pipera zine (p-MPPI) as 5-HT1A ligands. |
AID597305 | Inhibition of 5HT5A receptor at 10 uM | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID1854988 | Displacement of [3H]-8-OH-DPAT from Sprague-Dawley rat hippocampal membrane 5HT1A receptor | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
| Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors. |
AID510402 | Antagonist activity at human cloned 5HT1A receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced [34S]GTPgammaS binding by liquid scintillation counting | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
| 1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors. |
AID597321 | Inhibition of adrenergic alpha2A receptor at 10 uM | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID4140 | Antagonistic activity at postsynaptic 5-hydroxytryptamine 1A receptor was measured by its ability to inhibit hypothermia elicited by s.c. administration of 8-OH-DPAT in rat | 2002 | Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
| Improvement in the selectivity and metabolic stability of the serotonin 5-HT(1A) ligand, S 15535: a series of cis- and trans-2-(arylcycloalkylamine) 1-indanols. |
AID193027 | Ability to counteract the 8-OH-DPAT (1 mg/kg sc)-induced Hypothermia in rats (n=4) and evaluated for the decrease in body temperature (degrees Celsius) at 1.0(micro mol/kg) | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
| Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635. |
AID597307 | Inhibition of 5HT1D receptor at 10 uM | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID1517946 | Induction of hypothermia in CD-1 mouse assessed as change in body temperature at 0.1 mg/kg, ip measured after 90 mins by thermometric method (Rvb = -0.3 to 0.3 deg C) | | | |
AID1593199 | Antagonist activity at cloned human 5-HT1A receptor transfected in human HeLa cell membranes preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 30 mins by liquid scintillation counting | | | |
AID87448 | Effect on Forskolin-Stimulated cAMP formation, in HeLa cells transfected with the 5-HT 1A receptor at 1 uM concentration | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants. |
AID3510 | Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor | 2004 | Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
| Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines. |
AID510390 | Displacement [3H]prazosin of human recombinant Alpha-1D adrenergic receptor expressed in CHO cells by rapid filtration technique | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
| 1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors. |
AID17432 | Biodistribution of the [11C]-radiolabeled compound in rat hypothalamus co-injected with 50 nM of WAY 100635. | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| Development of fluorine-18-labeled 5-HT1A antagonists. |
AID3772 | Inhibitory activity against 5-hydroxytryptamine 1A receptor of rat hippocampal homogenates | 1994 | Journal of medicinal chemistry, May-13, Volume: 37, Issue:10
| Synthesis and evaluation of 4-(2'-methoxyphenyl)-1-[2'-[N-(2"-pyridinyl)-p- iodobenzamido]ethyl]piperazine (p-MPPI): a new iodinated 5-HT1A ligand. |
AID1337901 | Analgesic activity in Swiss CD1 mouse assessed reduction in formalin-induced inflammatory pain by measuring reduction in time spent in licking or biting formalin injected hind paw at 3 mg/kg, ip pretreated for 30 mins followed by formalin injection measur | | | |
AID422848 | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
| Synthesis, potency, and in vivo evaluation of 2-piperazin-1-ylquinoline analogues as dual serotonin reuptake inhibitors and serotonin 5-HT1A receptor antagonists. |
AID239799 | Binding affinity for alpha 1a adrenoceptor | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
| Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses. |
AID597284 | Inhibition of 5HT2A receptor at 10 uM | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID597301 | Inhibition of dopamine D2 receptor at 10 uM | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID597308 | Inhibition of 5HT1B receptor at 10 uM | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID3547 | Agonistic effect against 5-hydroxytryptamine 1A receptor using [35S]GTP-gamma-S as radioligand in CHO cells relative to 5-HT | 2004 | Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
| Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines. |
AID3803 | Binding affinity against human 5-hydroxytryptamine 1A receptor in CHO cells labeled with [3H]8-OH-DPAT radioligand | 2004 | Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
| Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines. |
AID87450 | Percent increase in the Forskolin-Stimulated cAMP formation, in HeLa cells transfected with the 5-HT 1A receptor [compound (1 uM)] | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants. |
AID231742 | Ratio of biodistribution of compound at Hippocampus and cerebellum-1 in rat with 200 nmol of WAY 100635 | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| Development of fluorine-18-labeled 5-HT1A antagonists. |
AID309471 | Decrease in body temperature in Swiss Albino mouse at 0.1 mg/kg after 30 mins | 2007 | Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22
| The influence of modifications in imide fragment structure on 5-HT(1A) and 5-HT(7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl)piperazines. |
AID3524 | Agonistic efficacy was evaluated by adenylyl cyclase assay in CHO cells stably expressing the human 5-HT1A receptor | 1998 | Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
| Functional characteristics of a series of N4-substituted 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazines as 5-HT1A receptor ligands. Structure-activity relationships. |
AID1830041 | Displacement of [3H]LSD from human recombinant 5-HT2A receptor expressed in HEK cells by radioligand completion assay relative to control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
| Activity of |
AID231558 | Ratio of biodistribution of compound at Hippocampus and cerebellum-1 in rat | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| Development of fluorine-18-labeled 5-HT1A antagonists. |
AID309486 | Decrease in body temperature in Swiss Albino mouse at 0.1 mg/kg after 120 mins | 2007 | Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22
| The influence of modifications in imide fragment structure on 5-HT(1A) and 5-HT(7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl)piperazines. |
AID597285 | Inhibition of 5HT2C receptor at 10 uM | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID441123 | Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HEK293 cells after 120 mins | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Synthesis and characterization of environment-sensitive fluorescent ligands for human 5-HT1A receptors with 1-arylpiperazine structure. |
AID597304 | Inhibition of adrenergic beta1 receptor at 10 uM | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID339528 | Displacement of [3H]paroxetine from rat cortical 5HTT reuptake site | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
| Studies toward the discovery of the next generation of antidepressants. Part 6: Dual 5-HT1A receptor and serotonin transporter affinity within a class of arylpiperazinyl-cyclohexyl indole derivatives. |
AID597319 | Inhibition of sigma 1 receptor at 10 uM | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID1555768 | Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting | 2019 | European journal of medicinal chemistry, Aug-15, Volume: 176 | 1,3-Dioxane as a scaffold for potent and selective 5-HT |
AID221108 | Time-dependent effect on 8-OH-DPAT-induced hypothermia (change in body temperature) after 60 min, in mice at 1 mg/kg dose | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants. |
AID1365310 | In-vivo 5-HT1A receptor agonist activity in Swiss albino mouse assessed as induction of lower lip retraction by measuring lower lip retraction score at 0.3 mg/kg, ip dosed 15 mins before test (Rvb = 0.0 +/- 0.0 No_unit) | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
| New 5-HT |
AID1713194 | Inhibition of 8-OH-DPAT-induced hypothermia in Swiss albino mouse assessed as change in rectal body temperature at 0.3 mg/kg, sc pretreated with compound for 45 mins followed by 8-OH-DPAT challenge and measured after 15 min by thermometer (Rvb = -1.8 degr | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
| Synthesis and biological investigation of new equatorial (β) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile. |
AID1409504 | Antagonist activity at serotonin 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics. |
AID597315 | Inhibition of 5HT1B receptor | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID1830039 | Displacement of [3H]LSD from human recombinant 5-HT2C receptor expressed in HEK cells by radioligand completion assay relative to control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
| Activity of |
AID3882 | Antagonistic efficacy was evaluated by adenylyl cyclase assay in CHO cells stably expressing the human 5-HT1A receptor | 1998 | Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
| Functional characteristics of a series of N4-substituted 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazines as 5-HT1A receptor ligands. Structure-activity relationships. |
AID510394 | Selectivity for human recombinant adrenergic Alpha-1B receptor over human recombinant adrenergic alpha1A receptor | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
| 1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors. |
AID231743 | Ratio of biodistribution of compound at cortex and cerebellum-1 in rat | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| Development of fluorine-18-labeled 5-HT1A antagonists. |
AID339531 | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
| Studies toward the discovery of the next generation of antidepressants. Part 6: Dual 5-HT1A receptor and serotonin transporter affinity within a class of arylpiperazinyl-cyclohexyl indole derivatives. |
AID1593197 | Displacement of [3H]Prazosin from human recombinant alpha 1D adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay | | | |
AID1555772 | Agonist activity at human recombinant 5HT1A receptor expressed in human HeLa cells assessed as increase in [35S]GTPgammaS binding incubated for 20 mins by liquid scintillation counter | 2019 | European journal of medicinal chemistry, Aug-15, Volume: 176 | 1,3-Dioxane as a scaffold for potent and selective 5-HT |
AID597317 | Inhibition of sigma 2 receptor at 10 uM | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID1409503 | Antagonist activity at serotonin 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux at 10 uM after 15 mins by calcium 4-dye based FLIPR assay relative to control | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics. |
AID597283 | Inhibition of 5HT1E receptor at 10 uM | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID4398 | Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes. | 1998 | Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
| Functional characteristics of a series of N4-substituted 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazines as 5-HT1A receptor ligands. Structure-activity relationships. |
AID1601994 | Induction of hypothermia in CD-1 mouse assessed as change in body temperature at 0.1 mg/kg, sc measured after 60 mins by thermometric method (Rvb = 0.1 deg C) | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
AID1555770 | Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1D expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counter | 2019 | European journal of medicinal chemistry, Aug-15, Volume: 176 | 1,3-Dioxane as a scaffold for potent and selective 5-HT |
AID597318 | Inhibition of SERT at 10 uM | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID597313 | Inhibition of adrenergic alpha1A receptor | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID1602006 | Induction of hypothermia in CD-1 mouse assessed as change in body temperature at 0.1 mg/kg, sc measured after 120 mins by thermometric method (Rvb = -0.1 to 0.1 deg C) | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
AID510393 | Selectivity for human recombinant adrenergic Alpha-1B receptor over human recombinant adrenergic alpha1D receptor | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
| 1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors. |
AID1602000 | Induction of hypothermia in CD-1 mouse assessed as change in body temperature at -0.1 to 0.1 mg/kg, sc measured after 90 mins by thermometric method (Rvb = -0.1 to 0.1 deg C) | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
AID221103 | Time-dependent effect on 8-OH-DPAT-induced hypothermia (change in body temperature) after 30 min, in mice at 1 mg/kg dose | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants. |
AID1593195 | Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay | | | |
AID597311 | Inhibition of adrenergic Alpha-1B receptor | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID408280 | Intrinsic activity at human recombinant 5HT1A receptor expressed in HEK293 cells by [35S]GTPgammaS binding relative to 5 hydroxytryptamine | 2008 | Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
| Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists. |
AID4198 | In vitro binding affinity for 5-hydroxytryptamine 1A receptor was determined by measuring specific inhibition of [125I]-binding to rat hippocampal membrane preparations | 1998 | Journal of medicinal chemistry, Jan-15, Volume: 41, Issue:2
| Isoindol-1-one analogues of 4-(2'-methoxyphenyl)-1-[2'-[N-(2"-pyridyl)-p-iodobenzamido]ethyl]pipera zine (p-MPPI) as 5-HT1A receptor ligands. |
AID6433 | Receptor-linked G protein activation at 5-hydroxytryptamine receptor was determined by measuring the stimulation of [35S]GTP-gamma-S, binding (Experiment 2) | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| Development of fluorine-18-labeled 5-HT1A antagonists. |
AID1555771 | Displacement of [3H]8-OH-DPAT from human cloned 5HT-1AR transfected in HeLa cells incubated for 30 mins by liquid scintillation counter | 2019 | European journal of medicinal chemistry, Aug-15, Volume: 176 | 1,3-Dioxane as a scaffold for potent and selective 5-HT |
AID3513 | Effective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cells | 2004 | Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
| Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines. |
AID597312 | Inhibition of 5HT7 receptor | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID1830043 | Displacement of [3H]8-OH-DAPT from human recombinant 5-HT1A receptor expressed in COS7 cells measured after 60 to 90 mins by radioligand completion assay relative to control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
| Activity of |
AID726771 | Apparent permeability across apical to basolateral side in human Caco2 cells at 1 to 20 uM by LC-MS/MS analysis | 2013 | Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
| Discovery of novel α₁-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands. |
AID597286 | Inhibition of 5HT3 receptor at 10 uM | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID4326 | Inhibition of binding of [125I]8-OH-PIPAT ligand to 5-hydroxytryptamine 1A receptor of rat hippocampal homogenates | 1994 | Journal of medicinal chemistry, May-13, Volume: 37, Issue:10
| Synthesis and evaluation of 4-(2'-methoxyphenyl)-1-[2'-[N-(2"-pyridinyl)-p- iodobenzamido]ethyl]piperazine (p-MPPI): a new iodinated 5-HT1A ligand. |
AID309476 | Decrease in body temperature in Swiss Albino mouse at 0.1 mg/kg after 60 mins | 2007 | Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22
| The influence of modifications in imide fragment structure on 5-HT(1A) and 5-HT(7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl)piperazines. |
AID221098 | Time-dependent effect on 8-OH-DPAT-induced hypothermia (change in body temperature) after 15 min, in mice at 1 mg/kg dose | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants. |
AID1593198 | Displacement of [3H]-8-OH-DPAT from human recombinant 5-HT1A receptor expressed in human HeLa cells incubated for 30 mins by radioligand competition binding assay | | | |
AID1713201 | Effect on 8-OH-DPAT-induced lower lip retraction in Wistar rat at 0.2 mg/kg, sc pretreated with compound for 45 mins followed by 8-OH-DPAT challenge and measured after 15 mins (Rvb = 2.7 to 2.8 No_unit) | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
| Synthesis and biological investigation of new equatorial (β) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile. |
AID221164 | In vitro oral metabolic bioavailability after incubation with hepatic microsomes. | 2002 | Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
| Improvement in the selectivity and metabolic stability of the serotonin 5-HT(1A) ligand, S 15535: a series of cis- and trans-2-(arylcycloalkylamine) 1-indanols. |
AID726714 | Unbound fraction in rat plasma at 1000 ng/g after 5 hrs by equilibrium dialysis method | 2013 | Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
| Discovery of novel α₁-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands. |
AID481373 | Half life in rat liver microsomes at 1 uM after 20 mins | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
| The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists. |
AID408275 | Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor | 2008 | Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
| Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists. |
AID726709 | Ratio of drug level in brain to plasma in rat at 1 hr | 2013 | Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
| Discovery of novel α₁-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands. |
AID481371 | Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
| The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists. |
AID510392 | Selectivity for human recombinant adrenergic alpha1A receptor over human recombinant adrenergic Alpha-1D receptor | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
| 1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors. |
AID1393526 | Antagonist activity at human 5-HT1AR expressed in HEK293 cells assessed as inhibition of 8-OH-DPAT-induced calcium flux by fluorimetric method | | | |
AID3836 | In vitro inhibition of [3H]- 8-OH-DPAT binding to cloned cell line containing human 5-hydroxytryptamine 1A receptor | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| Development of fluorine-18-labeled 5-HT1A antagonists. |
AID1713197 | Inhibition of 8-OH-DPAT-induced hypothermia in Swiss albino mouse assessed as change in rectal body temperature at 0.3 mg/kg, sc pretreated with compound for 45 mins followed by 8-OH-DPAT challenge and measured after 60 min by thermometer (Rvb = -1.3 degr | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
| Synthesis and biological investigation of new equatorial (β) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile. |
AID597287 | Inhibition of 5HT6 receptor at 10 uM | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID3540 | Agonistic effect against 5-hydroxytryptamine 1A receptor using cAMP as radioligand relative to 5-HT in inhibiting forskolin-stimulated adenylate cyclase activity in CHO cells | 2004 | Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
| Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines. |
AID726710 | Unbound fraction in rat brain at 1000 ng/g after 5 hrs by equilibrium dialysis method | 2013 | Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
| Discovery of novel α₁-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands. |
AID197200 | Evaluated for the inhibition of footshock-evoked ultrasonic vocalization in rats after administration of 8-OH-DPAT (0.1 mg/kg sc) alone or in combination with WAY-100635 | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
| Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635. |
AID1704733 | Antagonist activity at human 5HT1A receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based | | | |
AID309496 | Effect on lower lip retraction in Wistar rat at 0.1 mg/kg | 2007 | Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22
| The influence of modifications in imide fragment structure on 5-HT(1A) and 5-HT(7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl)piperazines. |
AID510395 | Selectivity for human recombinant adrenergic alpha1 receptor over human cloned 5HT1A receptor | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
| 1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors. |
AID1713200 | Effect on 8-OH-DPAT-induced lower lip retraction in Wistar rat at 0.1 mg/kg, sc pretreated with compound for 45 mins followed by 8-OH-DPAT challenge and measured after 15 mins (Rvb = 2.7 to 2.8 No_unit) | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
| Synthesis and biological investigation of new equatorial (β) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile. |
AID510391 | Displacement [3H]8-OH-DPAT of human cloned 5HT1A receptor expressed in human HeLa cells by rapid filtration technique | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
| 1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors. |
AID1347154 | Primary screen GU AMC 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. |
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. |
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. |
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. |
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. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID588378 | qHTS for Inhibitors of ATXN expression: Validation | | | |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | | | |
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. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
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. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
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. |
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. |
AID624215 | Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1A | 1998 | European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3
| Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study. |
AID624215 | Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1A | 1998 | Naunyn-Schmiedeberg's archives of pharmacology, Mar, Volume: 357, Issue:3
| Labelling of recombinant human and native rat serotonin 5-HT1A receptors by a novel, selective radioligand, [3H]-S 15535: definition of its binding profile using agonists, antagonists and inverse agonists. |
AID1345814 | Human D4 receptor (Dopamine receptors) | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
| Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto |
AID1345615 | Human 5-HT1A receptor (5-Hydroxytryptamine receptors) | 1998 | Naunyn-Schmiedeberg's archives of pharmacology, Mar, Volume: 357, Issue:3
| Labelling of recombinant human and native rat serotonin 5-HT1A receptors by a novel, selective radioligand, [3H]-S 15535: definition of its binding profile using agonists, antagonists and inverse agonists. |
AID1345615 | Human 5-HT1A receptor (5-Hydroxytryptamine receptors) | 1998 | European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3
| Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study. |
AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 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. |
AID624215 | Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1A | 1997 | Life sciences, , Volume: 60, Issue:9
| Pharmacological characterization of recombinant human 5-hydroxytryptamine1A receptors using a novel antagonist radioligand, [3H]WAY-100635. |
AID1345615 | Human 5-HT1A receptor (5-Hydroxytryptamine receptors) | 1997 | Life sciences, , Volume: 60, Issue:9
| Pharmacological characterization of recombinant human 5-hydroxytryptamine1A receptors using a novel antagonist radioligand, [3H]WAY-100635. |
AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6
| A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
AID493017 | Wombat Data for BeliefDocking | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
| Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |