5-chloro-2-methyl-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1H-indole: a 5-HT6 agonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 10131112 |
| CHEMBL ID | 364005 |
| CHEBI ID | 92829 |
| SCHEMBL ID | 1548928 |
| MeSH ID | M0528400 |
| Synonym |
|---|
| BRD-K47659338-003-01-0 |
| NCGC00161402-01 |
| 5-chloro-2-methyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1h-indole |
| CHEMBL364005 , |
| 5-chloro-2-methyl-3-(1,2,3,6-tetrahydro-pyridin-4-yl)-1h-indole |
| bdbm50171235 |
| A830276 |
| 5-chloranyl-2-methyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1h-indole |
| 54635-62-0 |
| 5-chloro-2-methyl-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1h-indole |
| emd-386088 |
| SCHEMBL1548928 |
| gtpl8428 |
| compound 18 [pmid 16055331] |
| DTXSID30436055 |
| CHEBI:92829 |
| Q260375 |
| 1h-indole, 5-chloro-2-methyl-3-(1,2,3,6-tetrahydro-4-pyridinyl)- |
| urz93y3d9j , |
| Class | Description |
|---|---|
| indoles | Any compound containing an indole skeleton. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 7.9433 | 0.1800 | 13.5574 | 39.8107 | AID1468 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 17.7828 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 28.1838 | 0.3162 | 12.7657 | 31.6228 | AID881 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 28.1838 | 0.0063 | 8.2350 | 39.8107 | AID881 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 4 | Cavia porcellus (domestic guinea pig) | IC50 (µMol) | 0.6200 | 0.0001 | 1.0076 | 8.7800 | AID254880 |
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.6600 | 0.0003 | 1.3833 | 8.4000 | AID254849 |
| 5-hydroxytryptamine receptor 1B | Homo sapiens (human) | IC50 (µMol) | 0.1100 | 0.0005 | 0.3975 | 6.5000 | AID254855 |
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | IC50 (µMol) | 0.2400 | 0.0001 | 0.8801 | 8.8500 | AID254866 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | IC50 (µMol) | 0.4500 | 0.0001 | 1.0302 | 9.0000 | AID254867 |
| 5-hydroxytryptamine receptor 1B | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.1800 | 0.0005 | 1.4835 | 7.8000 | AID254850 |
| 5-hydroxytryptamine receptor 7 | Homo sapiens (human) | IC50 (µMol) | 3.0000 | 0.0005 | 0.4546 | 4.7640 | AID254859 |
| Sodium channel protein type 1 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 0.6600 | 0.0023 | 2.8296 | 9.0000 | AID254849 |
| 5-hydroxytryptamine receptor 3A | Homo sapiens (human) | IC50 (µMol) | 0.0340 | 0.0001 | 1.0789 | 9.0000 | AID254932 |
| 5-hydroxytryptamine receptor 6 | Homo sapiens (human) | IC50 (µMol) | 0.0074 | 0.0017 | 0.8381 | 5.4200 | AID254858; AID254956 |
| Sodium channel protein type 2 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 0.6600 | 0.0000 | 3.7401 | 10.0000 | AID254849 |
| Sodium channel protein type 3 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 0.6600 | 0.0053 | 2.8085 | 9.0000 | AID254849 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| 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. |
| AID254859 | Inhibitory activity against 5-hydroxytryptamine 7 receptor in human | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | 2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists. |
| AID254867 | Inhibitory activity against 5-hydroxytryptamine 2C receptor in human | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | 2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists. |
| AID255427 | Intrinsic activity (IA) at the 5-HT6 receptor determined by measuring their cAMP production in BHK cells and compared to the effect elicited by 5-HT | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | 2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists. |
| AID254855 | Inhibitory activity against 5-hydroxytryptamine 1B receptor in calf | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | 2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists. |
| AID254849 | Inhibitory activity against 5-hydroxytryptamine 1A receptor in rat | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | 2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists. |
| AID254866 | Inhibitory activity against 5-hydroxytryptamine 2A receptor in human | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | 2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists. |
| AID254858 | Inhibitory activity against 5-hydroxytryptamine 6 receptor in human | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | 2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists. |
| AID254956 | Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | 2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists. |
| AID254850 | Inhibitory activity against 5-hydroxytryptamine 1B receptor in rat | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | 2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists. |
| AID254880 | Inhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pig | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | 2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists. |
| AID255635 | Concentration to stimulate the cAMP production in BHK cells | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | 2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists. |
| AID254932 | Inhibitory activity against 5-hydroxytryptamine 3 receptor expressed in NG 108 cells | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | 2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists. |
| AID1345170 | Human 5-HT6 receptor (5-Hydroxytryptamine receptors) | 2005 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19 | 2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 2 (8.33) | 29.6817 |
| 2010's | 18 (75.00) | 24.3611 |
| 2020's | 4 (16.67) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (12.49) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 24 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||