SM 130686: a growth hormone secretagogue; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 9804743 |
| CHEMBL ID | 360227 |
| SCHEMBL ID | 6376444 |
| MeSH ID | M0410496 |
| Synonym |
|---|
| (s)-3-(2-chloro-phenyl)-1-(2-diethylamino-ethyl)-3-hydroxy-2-oxo-4-trifluoromethyl-2,3-dihydro-1h-indole-6-carboxylic acid amide |
| bdbm50151162 |
| CHEMBL360227 , |
| gtpl5866 |
| (3r)-3-(2-chlorophenyl)-1-(2-diethylaminoethyl)-3-hydroxy-2-oxo-4-(trifluoromethyl)indole-6-carboxamide |
| sm 130686 |
| SCHEMBL6376444 |
| 1h-indole-6-carboxamide, 3-(2-chlorophenyl)-1-(2-(diethylamino)ethyl)-2,3-dihydro-3-hydroxy-2-oxo-4-(trifluoromethyl)-, (3s)- |
| 259666-71-2 |
| unii-1gh34i6261 |
| 1GH34I6261 , |
| sm-130686 free base |
| Q27895838 |
| ysspgxcffitnce-oaqylsrusa-n |
| DTXSID501027155 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Compound 37S showed a good pharmacokinetic profile in rats with 28% oral bioavailability at 10 mg/kg and excellent in vivo activity as evidenced by a significant weight gain after 4 days of oral administration at 10 mg/kg twice a day." | ( Oxindole derivatives as orally active potent growth hormone secretagogues. Hourai, S; Hume, WE; Kumagai, K; Nagamine, J; Nagata, R; Noguchi, H; Okazaki, K; Seki, H; Taiji, M; Tokunaga, T; Ueki, Y; Umezome, T, 2001) | 0.31 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Growth hormone secretagogue receptor type 1 | Homo sapiens (human) | IC50 (µMol) | 0.0016 | 0.0004 | 0.5892 | 6.0000 | AID242191; AID242565 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| growth hormone secretagogue receptor activity | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| G protein-coupled receptor activity | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| growth hormone-releasing hormone receptor activity | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| peptide hormone binding | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| plasma membrane | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| cell surface | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| neuron projection | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| membrane raft | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| synaptic membrane | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| Schaffer collateral - CA1 synapse | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| postsynapse | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| glutamatergic synapse | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| plasma membrane | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID242191 | Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin | 2004 | Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17 | Identification of structurally diverse growth hormone secretagogue agonists by virtual screening and structure-activity relationship analysis of 2-formylaminoacetamide derivatives. |
| AID242565 | Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation | 2005 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7 | Structure-activity relationships of the oxindole growth hormone secretagogues. |
| AID1346009 | Human ghrelin receptor (Ghrelin receptor) | 2001 | Journal of medicinal chemistry, Dec-20, Volume: 44, Issue:26 | Oxindole derivatives as orally active potent growth hormone secretagogues. |
| AID1346009 | Human ghrelin receptor (Ghrelin receptor) | 2009 | Molecular pharmacology, Jan, Volume: 75, Issue:1 | Overlapping binding site for the endogenous agonist, small-molecule agonists, and ago-allosteric modulators on the ghrelin receptor. |
| [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 | 9 (100.00) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (0.00) | 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 moderate demand-to-supply ratio for research on this compound.
| This Compound (19.68) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 2 (22.22%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 7 (77.78%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||