LG 100754: retinoic acid receptors antagonist & agonist; a mixed function retinoid whose activity is dimer-selective; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 6442223 |
| CHEMBL ID | 109581 |
| SCHEMBL ID | 502043 |
| MeSH ID | M0266282 |
| Synonym |
|---|
| bdbm50052589 |
| (2e,4e,6z)-3-methyl-7-(5,5,8,8-tetramethyl-3-propoxy-5,6,7,8-tetrahydro-naphthalen-2-yl)-octa-2,4,6-trienoic acid |
| lg754 |
| (2e,4e,6z)-3-methyl-7-(5,5,8,8-tetramethyl-3-propoxy-6, 7-dihydronaphthalen-2-yl)octa-2,4,6-trienoic acid |
| gtpl2814 |
| lg100754 |
| (2e,4e,6z)-3-methyl-7-(5,5,8,8-tetramethyl-3-propoxy-5,6,7,8-tetrahydronaphthalen-2-yl)octa-2,4,6-trienoic acid |
| cd 3159 |
| CHEMBL109581 , |
| 2,4,6-octatrienoic acid, 3-methyl-7-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-3-propoxy-2-naphthalenyl)-, (2e,4e,6z)- |
| 180713-37-5 |
| lgd 100754 |
| lg 100754 |
| (2e,4e,6z)-3-methyl-7-(5,5,8,8-tetramethyl-3-propoxy-6,7-dihydronaphthalen-2-yl)octa-2,4,6-trienoic acid |
| SCHEMBL502043 |
| (2e,4e,6z)-3-methyl-7-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-3-propoxy-3-naphthalenyl)-2,4,6-octatrienoic acid |
| AKOS024457822 |
| HY-108523 |
| Q27080268 |
| (2e,4e,6z)-3-methyl-7-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-3-propoxy-3-naphthalenyl)-2,4,6-octatrienoicacid |
| CS-0029091 |
| F82159 |
| MS-26692 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Retinoic acid receptor alpha | Homo sapiens (human) | Ki | 1.7910 | 0.0010 | 0.9485 | 6.5000 | AID200136 |
| Retinoic acid receptor beta | Homo sapiens (human) | Ki | 2.5870 | 0.0007 | 1.5673 | 9.9010 | AID198220 |
| Retinoic acid receptor gamma | Homo sapiens (human) | Ki | 6.0940 | 0.0000 | 1.9975 | 10.0000 | AID198735 |
| Retinoic acid receptor RXR-alpha | Homo sapiens (human) | Ki | 0.0080 | 0.0004 | 0.5692 | 7.6320 | AID199495 |
| Retinoic acid receptor RXR-beta | Homo sapiens (human) | Ki | 0.0090 | 0.0005 | 0.1592 | 0.8810 | AID199784 |
| Retinoic acid receptor RXR-gamma | Homo sapiens (human) | Ki | 0.0140 | 0.0014 | 0.1526 | 1.0000 | AID199944 |
| [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) |
|---|---|---|---|---|---|---|---|
| Retinoic acid receptor alpha | Homo sapiens (human) | EC50 (µMol) | 0.0040 | 0.0002 | 0.1790 | 2.5119 | AID200109 |
| Retinoic acid receptor beta | Homo sapiens (human) | EC50 (µMol) | 0.0100 | 0.0003 | 0.2311 | 6.9000 | AID198202 |
| Retinoic acid receptor gamma | Homo sapiens (human) | EC50 (µMol) | 0.1920 | 0.0002 | 0.0613 | 0.6480 | AID198714 |
| Retinoic acid receptor RXR-alpha | Homo sapiens (human) | EC50 (µMol) | 0.0020 | 0.0001 | 0.3427 | 9.1000 | AID199478 |
| Retinoic acid receptor RXR-beta | Homo sapiens (human) | EC50 (µMol) | 0.0130 | 0.0008 | 0.5254 | 5.2000 | AID199782 |
| Retinoic acid receptor RXR-gamma | Homo sapiens (human) | EC50 (µMol) | 0.0040 | 0.0001 | 0.2380 | 1.2250 | AID199942 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID198735 | Inhibition of [3H]ATRA binding to Retinoic acid receptor RAR gamma | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Identification of the first retinoid X, receptor homodimer antagonist. |
| AID199944 | Inhibition of [3H]targretin binding to Retinoid X receptor RXR gamma | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Identification of the first retinoid X, receptor homodimer antagonist. |
| AID200136 | Inhibition of [3H]ATRA binding to Retinoic acid receptor RAR alpha | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Identification of the first retinoid X, receptor homodimer antagonist. |
| AID199495 | Inhibition of [3H]targretin binding to Retinoid X receptor RXR alpha | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Identification of the first retinoid X, receptor homodimer antagonist. |
| AID198220 | Inhibition of [3H]ATRA binding to Retinoic acid receptor RAR beta | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Identification of the first retinoid X, receptor homodimer antagonist. |
| AID199784 | Inhibition of [3H]-Targretin binding to Retinoid X receptor RXR beta | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Identification of the first retinoid X, receptor homodimer antagonist. |
| AID199782 | Transcriptional activation of Retinoid X receptor RXR beta | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Identification of the first retinoid X, receptor homodimer antagonist. |
| AID198714 | Transcriptional activation of Retinoic acid receptor RAR gamma | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Identification of the first retinoid X, receptor homodimer antagonist. |
| AID199942 | Transcriptional activation of Retinoid X receptor RXR gamma | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Identification of the first retinoid X, receptor homodimer antagonist. |
| AID198202 | Transcriptional activation of Retinoic acid receptor RAR beta | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Identification of the first retinoid X, receptor homodimer antagonist. |
| AID200109 | Transcriptional activation of Retinoic acid receptor RAR alpha | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Identification of the first retinoid X, receptor homodimer antagonist. |
| AID199478 | Transcriptional ativation of Retinoid X receptor RXR alpha | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Identification of the first retinoid X, receptor homodimer antagonist. |
| AID1346743 | Human Retinoid X receptor-beta (2B. Retinoid X receptors) | 2001 | Molecular endocrinology (Baltimore, Md.), Aug, Volume: 15, Issue:8 | The rexinoid LG100754 is a novel RXR:PPARgamma agonist and decreases glucose levels in vivo. |
| AID1346800 | Human Peroxisome proliferator-activated receptor-gamma (1C. Peroxisome proliferator-activated receptors) | 2001 | Molecular endocrinology (Baltimore, Md.), Aug, Volume: 15, Issue:8 | The rexinoid LG100754 is a novel RXR:PPARgamma agonist and decreases glucose levels in vivo. |
| AID1346800 | Human Peroxisome proliferator-activated receptor-gamma (1C. Peroxisome proliferator-activated receptors) | 2002 | The Journal of biological chemistry, Apr-12, Volume: 277, Issue:15 | The antidiabetic agent LG100754 sensitizes cells to low concentrations of peroxisome proliferator-activated receptor gamma ligands. |
| AID1346743 | Human Retinoid X receptor-beta (2B. Retinoid X receptors) | 1996 | Nature, Oct-03, Volume: 383, Issue:6599 | Activation of specific RXR heterodimers by an antagonist of RXR homodimers. |
| AID1346768 | Human Retinoid X receptor-alpha (2B. Retinoid X receptors) | 2001 | Molecular endocrinology (Baltimore, Md.), Aug, Volume: 15, Issue:8 | The rexinoid LG100754 is a novel RXR:PPARgamma agonist and decreases glucose levels in vivo. |
| AID1346743 | Human Retinoid X receptor-beta (2B. Retinoid X receptors) | 2002 | The Journal of biological chemistry, Apr-12, Volume: 277, Issue:15 | The antidiabetic agent LG100754 sensitizes cells to low concentrations of peroxisome proliferator-activated receptor gamma ligands. |
| [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 | 4 (33.33) | 18.2507 |
| 2000's | 5 (41.67) | 29.6817 |
| 2010's | 3 (25.00) | 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 (16.96) 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 | 12 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||