ronacaleret: a calcium-sensing receptor antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 10345214 |
| CHEMBL ID | 1198855 |
| SCHEMBL ID | 3737849 |
| MeSH ID | M0561836 |
| Synonym |
|---|
| sb-751689 |
| CHEMBL1198855 , |
| ronacaleret |
| bdbm50346036 |
| ronacaleret [inn] |
| unii-dih95yp7j3 |
| dih95yp7j3 , |
| sb 751689 |
| benzenepropanoic acid, 3-(((2r)-3-((2-(2,3-dihydro-1h-inden-2-yl)-1,1-dimethylethyl)amino)-2-hydroxypropyl)oxy)-4,5-difluoro- |
| 3-(3-(((2r)-3-((2-(2,3-dihydro-1h-inden-2-yl)-1,1-dimethylethyl)amino)-2-hydroxypropyl)oxy)-4,5-difluorophenyl)propanoic acid |
| SCHEMBL3737849 |
| gtpl9473 |
| 3-[3-[(2r)-3-[[1-(2,3-dihydro-1h-inden-2-yl)-2-methylpropan-2-yl]amino]-2-hydroxypropoxy]-4,5-difluorophenyl]propanoic acid |
| DB05255 |
| DTXSID60892347 |
| Q27276413 |
Ronacaleret is an orally-active calcium-sensing receptor (CaSR) antagonist. It has the potential for therapeutic utility in the stimulation of PTH release.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Ronacaleret is an orally-active calcium-sensing receptor (CaSR) antagonist that has the potential for therapeutic utility in the stimulation of PTH release, notably as a bone anabolic agent comparable to recombinant human PTH(1-34) (rhPTH(1-34)). " | ( Characterization of the effect of chronic administration of a calcium-sensing receptor antagonist, ronacaleret, on renal calcium excretion and serum calcium in postmenopausal women. Caltabiano, S; Desjardins, JP; Dollery, CT; Favus, MJ; Fitzpatrick, LA; Hossain, M; Kumar, R; Kurtinecz, MT, 2013) | 2.05 |
| "Ronacaleret is an orally administered calcium-sensing receptor antagonist that stimulates endogenous parathyroid hormone release from the parathyroid glands." | ( Ronacaleret, a calcium-sensing receptor antagonist, increases trabecular but not cortical bone in postmenopausal women. Cicconetti, G; Dabrowski, CE; Engelke, K; Fitzpatrick, LA; Fuerst, T; Genant, HK; Gordon, DN, 2012) | 2.54 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Extracellular calcium-sensing receptor | Homo sapiens (human) | IC50 (µMol) | 0.1460 | 0.0000 | 0.0416 | 0.1460 | AID600276 |
| Extracellular calcium-sensing receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.3200 | 0.3200 | 0.4367 | 0.5300 | AID600275 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| phosphatidylinositol phospholipase C activity | Extracellular calcium-sensing receptor | Homo sapiens (human) |
| G protein-coupled receptor activity | Extracellular calcium-sensing receptor | Homo sapiens (human) |
| integrin binding | Extracellular calcium-sensing receptor | Homo sapiens (human) |
| calcium ion binding | Extracellular calcium-sensing receptor | Homo sapiens (human) |
| protein binding | Extracellular calcium-sensing receptor | Homo sapiens (human) |
| amino acid binding | Extracellular calcium-sensing receptor | Homo sapiens (human) |
| protein kinase binding | Extracellular calcium-sensing receptor | Homo sapiens (human) |
| protein homodimerization activity | Extracellular calcium-sensing receptor | Homo sapiens (human) |
| transmembrane transporter binding | Extracellular calcium-sensing receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| plasma membrane | Extracellular calcium-sensing receptor | Homo sapiens (human) |
| cell surface | Extracellular calcium-sensing receptor | Homo sapiens (human) |
| basolateral plasma membrane | Extracellular calcium-sensing receptor | Homo sapiens (human) |
| apical plasma membrane | Extracellular calcium-sensing receptor | Homo sapiens (human) |
| neuronal cell body | Extracellular calcium-sensing receptor | Homo sapiens (human) |
| axon terminus | Extracellular calcium-sensing receptor | Homo sapiens (human) |
| plasma membrane | Extracellular calcium-sensing receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID600202 | Oral bioavailability in Sprague-Dawley rat at 10 mg/kg | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12 | The discovery of novel calcium sensing receptor negative allosteric modulators. |
| AID600276 | Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12 | The discovery of novel calcium sensing receptor negative allosteric modulators. |
| AID600201 | Cmax in Sprague-Dawley rat at 10 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12 | The discovery of novel calcium sensing receptor negative allosteric modulators. |
| AID600277 | Inhibition of human ERG at 10 uM by whole cell voltage clamp technique | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12 | The discovery of novel calcium sensing receptor negative allosteric modulators. |
| AID600200 | Increase in PTH (1-84) release response in Sprague-Dawley rat at 10 mg/kg, po by PTH ELISA | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12 | The discovery of novel calcium sensing receptor negative allosteric modulators. |
| AID600279 | Intrinsic clearance in rat liver microsomes assessed per mg of protein | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12 | The discovery of novel calcium sensing receptor negative allosteric modulators. |
| AID600280 | Lipophilicity, log D of the compound | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12 | The discovery of novel calcium sensing receptor negative allosteric modulators. |
| AID600275 | Negative allosteric modulator activity at rat calcium sensing receptor expressed in HEK cells | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12 | The discovery of novel calcium sensing receptor negative allosteric modulators. |
| AID600278 | Intrinsic clearance in human liver microsomes assessed per mg of protein | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12 | The discovery of novel calcium sensing receptor negative allosteric modulators. |
| AID1346721 | Human CaS receptor (Calcium-sensing receptor) | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12 | The discovery of novel calcium sensing receptor negative allosteric modulators. |
| [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 | 1 (8.33) | 29.6817 |
| 2010's | 10 (83.33) | 24.3611 |
| 2020's | 1 (8.33) | 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 (23.40) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 5 (41.67%) | 5.53% |
| Reviews | 1 (8.33%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 6 (50.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||