Page last updated: 2024-12-10
obelin
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
obelin: calcium-sensitive photoprotein obtained from the hydroid Obelia geniculata [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 5311377 |
| CHEMBL ID | 251541 |
| MeSH ID | M0056027 |
Synonyms (12)
| Synonym |
|---|
| gtpl2030 |
| obelin |
| CHEMBL251541 , |
| [(3r,4ar,10ar)-6-methoxy-1-methyl-3,4,4a,5,10,10a-hexahydro-2h-benzo[g]quinolin-3-yl]-[4-(4-nitrophenyl)piperazin-1-yl]methanone |
| sra880 |
| bdbm50423297 |
| sra880 free base |
| 187218-90-2 (free base) |
| ((3r,4ar,10ar)-6-methoxy-1-methyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinolin-3-yl)(4-(4-nitrophenyl)piperazin-1-yl)methanone |
| Q27088869 |
| 187218-90-2 |
| AKOS040749558 |
Research Excerpts
Overview
Obelin is a photoprotein that emits light by Ca2+-binding.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Obelin is a photoprotein that emits light by Ca2+-binding. " | ( Use of proZZ-obelin fusion protein in bioluminescent immunoassay. Frank, LA; Illarionova, VA; Vysotski, ES, 1996) | 2.11 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " The octapeptide-obelin fusion protein retained the bioluminescence properties of the native protein, and was subsequently used to generate dose-response curves for the free octapeptide." | ( Genetically engineered obelin as a bioluminescent label in an assay for a peptide. Daunert, S; Lewis, JC; Matveev, SV, 1999) | 0.95 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (10)
Activation Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Beta-1 adrenergic receptor | Homo sapiens (human) | Kd | 0.2239 | 0.0001 | 0.8039 | 10.0000 | AID308062 |
| D(4) dopamine receptor | Homo sapiens (human) | Kd | 0.0050 | 0.0002 | 0.0032 | 0.0050 | AID308060; AID418527 |
| 5-hydroxytryptamine receptor 1D | Homo sapiens (human) | Kd | 0.1122 | 0.0794 | 0.0958 | 0.1122 | AID308061 |
| Somatostatin receptor type 1 | Rattus norvegicus (Norway rat) | Kd | 0.0007 | 0.0007 | 0.0007 | 0.0007 | AID308078 |
| Somatostatin receptor type 2 | Rattus norvegicus (Norway rat) | Kd | 7.7625 | 7.7625 | 7.7625 | 7.7625 | AID308079 |
| Somatostatin receptor type 1 | Homo sapiens (human) | Kd | 0.0102 | 0.0102 | 2.2901 | 4.5700 | AID308055 |
| Somatostatin receptor type 2 | Homo sapiens (human) | Kd | 36.3078 | 0.0008 | 0.0008 | 0.0008 | AID308056 |
| Somatostatin receptor type 4 | Homo sapiens (human) | Kd | 15.1356 | 8.9130 | 8.9130 | 8.9130 | AID308058 |
| Somatostatin receptor type 3 | Homo sapiens (human) | Kd | 8.7096 | 0.5250 | 4.6173 | 8.7096 | AID308057 |
| Somatostatin receptor type 5 | Homo sapiens (human) | Kd | 1.7783 | 0.0076 | 0.8929 | 1.7783 | AID308059 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (67)
Molecular Functions (23)
Ceullar Components (15)
Bioassays (20)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1346384 | Human SST1 receptor (Somatostatin receptors) | 2004 | Neuroscience letters, May-06, Volume: 361, Issue:1-3 | SRA880, in vitro characterization of the first non-peptide somatostatin sst(1) receptor antagonist. |
| AID308053 | Displacement of [125I]SRIF14 from sst1 receptor in rat brain cortex membrane | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists. |
| AID308058 | Binding affinity to human recombinant sst4 receptor | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists. |
| AID308055 | Binding affinity to human recombinant sst1 receptor | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists. |
| AID308082 | Oral bioavailability in rat at 10 mg/kg | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | SAR of the arylpiperazine moiety of obeline somatostatin sst1 receptor antagonists. |
| AID308061 | Binding affinity to human 5HT1D receptor | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists. |
| AID308054 | Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists. |
| AID418527 | Binding affinity to dopamine D4 receptor | 2009 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5 | Discovery of novel non-peptidic beta-alanine piperazine amide derivatives and their optimization to achiral, easily accessible, potent and selective somatostatin sst1 receptor antagonists. |
| AID308063 | Antagonist activity at human recombinant sst1 receptor assessed as blockade of SRIF14-induced inhibition of forskolin stimulated adenylate cyclase activity | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists. |
| AID308062 | Binding affinity to human adrenergic beta-1 receptor | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists. |
| AID308079 | Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | SAR of the arylpiperazine moiety of obeline somatostatin sst1 receptor antagonists. |
| AID308080 | Selectivity for rat sst1 receptor over rat sst2 receptor | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | SAR of the arylpiperazine moiety of obeline somatostatin sst1 receptor antagonists. |
| AID308083 | Clearance in rat at 10 mg/kg, po | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | SAR of the arylpiperazine moiety of obeline somatostatin sst1 receptor antagonists. |
| AID308084 | Volume of distribution at steady state in rat at 10 mg/kg, po | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | SAR of the arylpiperazine moiety of obeline somatostatin sst1 receptor antagonists. |
| AID308059 | Binding affinity to human recombinant sst5 receptor | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists. |
| AID308057 | Binding affinity to human recombinant sst3 receptor | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists. |
| AID308060 | Binding affinity to human dopamine D4 receptor | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists. |
| AID308056 | Binding affinity to human recombinant sst2 receptor | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists. |
| AID308078 | Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | SAR of the arylpiperazine moiety of obeline somatostatin sst1 receptor antagonists. |
| AID308085 | Ratio of drug level in brain to plasma in rat at 10 to 100 mg/kg, po after 90 mins | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | SAR of the arylpiperazine moiety of obeline somatostatin sst1 receptor antagonists. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (86)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 18 (20.93) | 18.7374 |
| 1990's | 15 (17.44) | 18.2507 |
| 2000's | 29 (33.72) | 29.6817 |
| 2010's | 19 (22.09) | 24.3611 |
| 2020's | 5 (5.81) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 26.73
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 (26.73) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 3 (3.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 97 (97.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||