| Assay ID | Title | Year | Journal | Article |
|---|
| AID1626461 | Antidepressant activity in Sprague-Dawley rat assessed as reduction in immobility time at 3 mg/kg, ip adminstered 60 mins prior to testing measured for 5 mins by forced swimming test | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| N1-Azinylsulfonyl-1H-indoles: 5-HT6 Receptor Antagonists with Procognitive and Antidepressant-Like Properties. |
| AID1568829 | Antagonist activity at recombinant human 5HT6 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as reduction in serotonin-induced calcium mobilization flux preincubated for 30 mins followed by serotonin addition in presence of coe | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Synthesis and computer-aided SAR studies for derivatives of phenoxyalkyl-1,3,5-triazine as the new potent ligands for serotonin receptors 5-HT |
| AID647186 | Plasma clearance in rat at 1 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3
| Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT₆ receptor antagonist showing activity in rat social recognition test. |
| AID1556435 | Metabolic stability in rat liver microsomes assessed as half life incubated for 20 to 60 mins in presence of metabolic phase 1 cofactors by HPLC-LC/MS analysis | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | 2-Aminoimidazole-based antagonists of the 5-HT |
| AID1705924 | Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay | | | |
| AID1351479 | Displacement of [3H]-Raclopride from human dopamine D2L receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting method | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Novel non-sulfonamide 5-HT |
| AID763551 | Antagonist activity at 5-HT6 receptor (unknown origin) | 2013 | Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15
| Synthesis of substituted diphenyl sulfones and their structure-activity relationship with the antagonism of 5-НТ6 receptors. |
| AID1730198 | Inverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Imidazopyridine-Based 5-HT |
| AID647185 | Half life in rat at 1 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3
| Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT₆ receptor antagonist showing activity in rat social recognition test. |
| AID647188 | Oral bioavailability in rat at 5 mg/kg at 24 hrs | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3
| Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT₆ receptor antagonist showing activity in rat social recognition test. |
| AID1154620 | Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
| Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT₆ and dopamine D₂ receptor ligands. |
| AID1626443 | Cognitive enhancing effect in Sprague-Dawley rat assessed as reversal of PCP induced memory deficit at 0.3 to 1 mg/kg, ip administered 1 hour and 15 mins before familiarization phase by novel object recognition test | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| N1-Azinylsulfonyl-1H-indoles: 5-HT6 Receptor Antagonists with Procognitive and Antidepressant-Like Properties. |
| AID1730193 | Stability in pH 1 buffer assessed as compound decomposition after 1 hr | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Imidazopyridine-Based 5-HT |
| AID482331 | Binding affinity to 5HT6 receptor | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14
| (3-Phenylsulfonylcycloalkano[e and d]pyrazolo[1,5-a]pyrimidin-2-yl)amines: potent and selective antagonists of the serotonin 5-HT6 receptor. |
| AID1626453 | Antianxietic activity in ip dosed Wistar rat assessed as increase in number of licks accepted measured for 5 mins by Vogel conflict drinking test | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| N1-Azinylsulfonyl-1H-indoles: 5-HT6 Receptor Antagonists with Procognitive and Antidepressant-Like Properties. |
| AID1178357 | Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| Serotonin 5-HT6 receptor antagonists for the treatment of cognitive deficiency in Alzheimer's disease. |
| AID1730221 | Effect on neurite growth in human NG108-15 cells expressing GFP-tagged 5-HT6 receptor assessed as neurite length at 1 uM incubated for 24 hrs by epifluorescence microscopy (Rvb = 37.20 +/- 1.53 micrometer) | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Imidazopyridine-Based 5-HT |
| AID1626455 | Displacement of [3H]Lu AE60157 from rat brain 5-HT6 receptor | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| N1-Azinylsulfonyl-1H-indoles: 5-HT6 Receptor Antagonists with Procognitive and Antidepressant-Like Properties. |
| AID1351478 | Displacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by microbeta counting method | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Novel non-sulfonamide 5-HT |
| AID1784792 | Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay | | | |
| AID1730222 | Toxicity in mouse C8-D1A astrocytes assessed as reduction in cell viability at 0.25 uM by MTT assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Imidazopyridine-Based 5-HT |
| AID1784793 | Antagonist activity at GFP-tagged 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in neurite growth at 1 uM after 24 hrs | | | |
| AID1705923 | Inverse agonist activity at recombinant human 5HT6 receptor expressed in 1321N1 cells assessed as inhibition of 5CT-induced cAMP production measured after 30 mins by TR-FRET assay | | | |
| AID1784760 | Antagonist activity at human 5-HT6 receptor expressed in 1321N1 cells assessed as inhibition of 5-CT induced cAMP production incubated for 30 mins | | | |
| AID1730223 | Toxicity in mouse C8-D1A astrocytes assessed as reduction in cell viability by MTT assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Imidazopyridine-Based 5-HT |
| AID1351474 | Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Novel non-sulfonamide 5-HT |
| AID1351475 | Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Novel non-sulfonamide 5-HT |
| AID1730201 | Displacement of [3H]-8-OH-DPAT from human 5HT2A expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Imidazopyridine-Based 5-HT |
| AID1823829 | Antagonist activity at human 5-HT6 receptor expressed in human recombinant CHO-K1 cells co-expressing G protein alpha16 incubated for 1 hr by cellular aequorin-based functional assay | | | |
| AID1690399 | Antagonist activity at recombinant human Ga16-coupled 5HT2A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 15 to 30 mins followed by serotonin addition and measured for 30 to 60 secs by | 2020 | European journal of medicinal chemistry, Apr-01, Volume: 191 | Multifunctional 6-fluoro-3-[3-(pyrrolidin-1-yl)propyl]-1,2-benzoxazoles targeting behavioral and psychological symptoms of dementia (BPSD). |
| AID599941 | Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12
| Identification of a novel series of 3-piperidinyl-5-sulfonylindazoles as potent 5-HT6 ligands. |
| AID1705934 | Glio-protective activity against 6-OHDA-induced cell death in mouse C8D1A astrocytes at 0.25 uM preincubated for 24 hrs followed by 6-OHDA stimulation for 24 hrs by MTT assay | | | |
| AID1626448 | Toxicity in Sprague-Dawley rat assessed as effect on locomotory activity at 0.3 to 3 mg/kg, ip measured for 5 mins by open field test | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| N1-Azinylsulfonyl-1H-indoles: 5-HT6 Receptor Antagonists with Procognitive and Antidepressant-Like Properties. |
| AID1784761 | Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method | | | |
| AID1626446 | Antidepressant activity in Sprague-Dawley rat assessed as increase in climbing time at 3 mg/kg, ip adminstered 60 mins prior to testing measured for 5 mins by forced swimming test | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| N1-Azinylsulfonyl-1H-indoles: 5-HT6 Receptor Antagonists with Procognitive and Antidepressant-Like Properties. |
| AID1730202 | Displacement of [3H]-5-CT from human 5HT7b expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Imidazopyridine-Based 5-HT |
| AID1730196 | Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Imidazopyridine-Based 5-HT |
| AID1351506 | Binding affinity to 5HT6R (unknown origin) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Novel non-sulfonamide 5-HT |
| AID1730203 | Displacement of [3H]-raclopride from human D2L expressed in CHO-K1 cell membranes incubated for 1 hr by micro-beta plate reader based analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Imidazopyridine-Based 5-HT |
| AID1441516 | Antagonist activity at 5-HT6 receptor (unknown origin) | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
| Discovery and Development of 1-[(2-Bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole Dimesylate Monohydrate (SUVN-502): A Novel, Potent, Selective and Orally Active Serotonin 6 (5-HT |
| AID1568823 | Agonist activity at recombinant human 5HT6 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as increase in calcium mobilization and measured for 60 secs in presence of coelenterazine by luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Synthesis and computer-aided SAR studies for derivatives of phenoxyalkyl-1,3,5-triazine as the new potent ligands for serotonin receptors 5-HT |
| AID1351501 | Reversal of PCP-induced cognitive impairment in Sprague-Dawley rat assessed as reduction in time spent exploring novel object over familiar object at 0.3 to 1 mg/kg, po administered 120 mins before familiarization phase measured for 3 mins post familiariz | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Novel non-sulfonamide 5-HT |
| AID1351481 | Inverse agonist activity at GFP-tagged 5-HT6R (unknown origin) transfected in NG108-15 cells assessed as reduction in Cdk5-mediated cell differentiation by measuring neurites length at 1 uM after 24 hrs by paraformaldehyde-based epifluorescence microscopy | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Novel non-sulfonamide 5-HT |
| AID647189 | Ratio of drug uptake in brain to plasma in rat at 5 mg/kg, po | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3
| Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT₆ receptor antagonist showing activity in rat social recognition test. |
| AID1916468 | Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constant | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Chemical update on the potential for serotonin 5-HT |
| AID1154622 | Antagonist activity at human 5-HT6 receptor expressed in CHO cells assessed as reduction in serotonin-induced cAMP accumulation after 30 mins by HTRF assay | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
| Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT₆ and dopamine D₂ receptor ligands. |
| AID1705935 | Glio-protective activity against 6-OHDA-induced cell death in mouse C8D1A astrocytes at 0.25 uM preincubated for 24 hrs followed by 6-OHDA stimulation for 24 hrs by LDH assay | | | |
| AID1730200 | Displacement of [3H]-8-OH-DPAT from human 5HT1A expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2
| Imidazopyridine-Based 5-HT |
| AID1626454 | Antianxietic activity in ip dosed Wistar rat assessed as increase in number of shocks accepted measured for 5 mins by Vogel conflict drinking test | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6
| N1-Azinylsulfonyl-1H-indoles: 5-HT6 Receptor Antagonists with Procognitive and Antidepressant-Like Properties. |
| AID1178360 | Oral bioavailability in rat | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| Serotonin 5-HT6 receptor antagonists for the treatment of cognitive deficiency in Alzheimer's disease. |
| AID1497625 | Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
| Pyrroloquinoline scaffold-based 5-HT |
| AID1556434 | Metabolic stability in rat liver microsomes assessed as intrinsic clearance incubated for 20 to 60 mins in presence of metabolic phase 1 cofactors by HPLC-LC/MS analysis | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | 2-Aminoimidazole-based antagonists of the 5-HT |
| AID647187 | Volume of distribution in rat at 1 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3
| Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT₆ receptor antagonist showing activity in rat social recognition test. |
| AID1351476 | Displacement of [3H]-8-OH-DPAT from human 5HT1AR expressed in HEK293 cell membranes after 1 hr by microbeta counting method | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Novel non-sulfonamide 5-HT |
| AID1351477 | Displacement of [3H]-Ketanserin from human 5HT2AR expressed in CHO-K1 cell membranes after 1.5 hrs by microbeta counting method | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Novel non-sulfonamide 5-HT |
| 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. |
| AID1347157 | Confirmatory screen GU Rhodamine qHTS for Zika virus inhibitors qHTS | 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. |
| AID1347161 | Confirmatory 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. |
| 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. |
| AID1347169 | Tertiary RLuc qRT-PCR qHTS assay 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. |
| 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. |
| AID1345170 | Human 5-HT6 receptor (5-Hydroxytryptamine receptors) | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
| Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT₆ and dopamine D₂ receptor ligands. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |