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lg 100567

Description

ALRT 1550: ALRT1550 is (2E,4E,6E)-isomer; LG100567 is (2E,4E,6Z)-isomer; structure given in first source [MeSH]

Cross-References

ID SourceID
PubMed CID5287705
CHEMBL ID89241
SCHEMBL ID6049839
SCHEMBL ID6049845
MeSH IDM0264448

Synonyms (28)

Synonym
CHEMBL89241 ,
bdbm50052033
(2e,4e,6e)-7-(3,5-di-tert-butyl-phenyl)-3-methyl-octa-2,4,6-trienoic acid
alrt 1550
gtpl2740
7-(3,5-ditert-butylphenyl)-3-methylocta-2,4,6-trienoic acid
1NQ7
(2e,4e,6e)-7-(3,5-ditert-butylphenyl)-3-methylocta-2,4,6-trienoic acid
178600-20-9
SCHEMBL6049839
SCHEMBL6049845
lg 100567
h62aoa2iyf ,
3-methyl-7-(3,5-di-t-butylphenyl)octatrienoic acid, 2e,4e,6e
2,4,6-octatrienoic acid, 7-(3,5-bis(1,1-dimethylethyl)phenyl)-3-methyl-, (2e,4e,6e)-
lg100567
unii-h62aoa2iyf
alrt-1550
lg-100567
7-(3,5-di-tert-butylphenyl)-3-methylocta-2,4,6-trienoic acid
alrt1550
lgd-1550
(2e,4e,6e)-7-(3,5-di-tert-butylphenyl)-3-methylocta-2,4,6-trienoic acid
Q27074412
lgd-1550 = alrt-1550
BL177434
2,4,6-octatrienoic acid, 7-[3,5-bis(1,1-dimethylethyl)phenyl]-3-methyl-, (2e,4e,6e)-
AKOS040747797

Protein Targets (7)

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Chain A, NUCLEAR RECEPTOR ROR-BETARattus norvegicus (Norway rat)Ki0.1600AID977610
Retinoic acid receptor alphaHomo sapiens (human)Ki0.0323AID198057
Retinoic acid receptor betaHomo sapiens (human)Ki0.0454AID198547
Retinoic acid receptor gamma Homo sapiens (human)Ki0.0630AID199058
Retinoic acid receptor RXR-alphaHomo sapiens (human)Ki0.1138AID199640
Retinoic acid receptor RXR-betaHomo sapiens (human)Ki0.2851AID199807
Retinoic acid receptor RXR-gammaHomo sapiens (human)Ki0.1646AID199967

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Retinoic acid receptor alphaHomo sapiens (human)EC500.0345AID198028
Retinoic acid receptor betaHomo sapiens (human)EC500.0131AID198381
Retinoic acid receptor gamma Homo sapiens (human)EC500.0082AID198902
Retinoic acid receptor RXR-alphaHomo sapiens (human)EC500.1340AID199629
Retinoic acid receptor RXR-betaHomo sapiens (human)EC500.0870AID199800
Retinoic acid receptor RXR-gammaHomo sapiens (human)EC500.0770AID199957

Bioassays (25)

Assay IDTitleYearJournalArticle
AID199807Inhibition of [3H]9-cis-RA binding to Retinoid X receptor RXR beta1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
ISSN: 0022-2623
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
AID199039Percent transcriptional activation relative to ATRA in CV-1 cells expressing Retinoic acid receptor RAR gamma1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
ISSN: 0022-2623
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
AID198902Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR gamma1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
ISSN: 0022-2623
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
AID199957Transcriptional activation in CV-1 cells expressing Retinoid X receptor RXR gamma1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
ISSN: 0022-2623
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
AID198037Percent transcriptional activation relative to ATRA in CV-1 cells expressing Retinoic acid receptor RAR alpha1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
ISSN: 0022-2623
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
AID198528Percent transcriptional activation relative to ATRA in CV-1 cells expressing Retinoic acid receptor RAR beta1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
ISSN: 0022-2623
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
AID198057Inhibition of [3H]ATRA binding to Retinoic acid receptor RAR alpha1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
ISSN: 0022-2623
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
AID199630Transcriptional activation in CV-1 cells expressing Retinoid X receptor RXR alpha; Not active1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
ISSN: 0022-2623
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
AID199640Inhibition of [3H]9-cis-RA binding to Retinoid X receptor RXR alpha1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
ISSN: 0022-2623
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
AID198381Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR beta1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
ISSN: 0022-2623
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
AID199967Inhibition of [3H]9-cis-RA binding to Retinoid X receptor RXR gamma1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
ISSN: 0022-2623
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
AID199811Transcriptional activation in CV-1 cells expressing Retinoid X receptor RXR beta1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
ISSN: 0022-2623
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
AID198547Inhibition of [3H]ATRA binding to Retinoic acid receptor RAR beta1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
ISSN: 0022-2623
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
AID199803Percent transcriptional activation relative to ATRA in CV-1 cells expressing Retinoid X receptor RXR beta1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
ISSN: 0022-2623
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
AID199058Inhibition of [3H]ATRA binding to Retinoic acid receptor RAR gamma1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
ISSN: 0022-2623
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
AID199800Transcriptional activation in CV-1 cells expressing Retinoid X receptor RXR beta1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
ISSN: 0022-2623
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
AID199629Transcriptional activation in CV-1 cells expressing Retinoid X receptor RXR alpha1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
ISSN: 0022-2623
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
AID199634Percent transcriptional activation relative to ATRA in CV-1 cells expressing Retinoid X receptor RXR alpha1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
ISSN: 0022-2623
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
AID198028Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR alpha1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
ISSN: 0022-2623
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
AID199962Percent transcriptional activation relative to ATRA in CV-1 cells expressing Retinoid X receptor RXR gamma1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
ISSN: 0022-2623
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
AID199958Transcriptional activation in CV-1 cells expressing Retinoid X receptor RXR gamma; Not active1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
ISSN: 0022-2623
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
AID1346777Human RAR-related orphan receptor-beta (1F. Retinoic acid-related orphans)2003Nature structural biology, Oct, Volume: 10, Issue:10
ISSN: 1072-8368
All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta.
AID1346769Human RAR-related orphan receptor-gamma (1F. Retinoic acid-related orphans)2003Nature structural biology, Oct, Volume: 10, Issue:10
ISSN: 1072-8368
All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2003Journal of chromatography. A, Dec-12, Volume: 1020, Issue:2
ISSN: 0021-9673
Analysis of multiple pesticide residues in tobacco using pressurized liquid extraction, automated solid-phase extraction clean-up and gas chromatography-tandem mass spectrometry.
AID1811Experimentally measured binding affinity data derived from PDB2003Journal of chromatography. A, Dec-12, Volume: 1020, Issue:2
ISSN: 0021-9673
Analysis of multiple pesticide residues in tobacco using pressurized liquid extraction, automated solid-phase extraction clean-up and gas chromatography-tandem mass spectrometry.

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (40.00)18.2507
2000's3 (60.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (16.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (83.33%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
tretinoinretinoic acid;
vitamin A
anti-inflammatory agent;
antineoplastic agent;
antioxidant;
AP-1 antagonist;
human metabolite;
keratolytic drug;
retinoic acid receptor agonist;
retinoid X receptor agonist;
signalling molecule
1996200324.5high001100
alitretinoinretinoic acidantineoplastic agent;
keratolytic drug;
metabolite;
retinoid X receptor agonist
1996199628.0medium001000
4-oxoretinoic acidenone;
retinoid
human xenobiotic metabolite2003200321.0medium000100
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
thymidinepyrimidine 2'-deoxyribonucleosideEscherichia coli metabolite;
human metabolite;
metabolite;
mouse metabolite
1996199628.0medium001000
bexarotenebenzoic acids;
naphthalenes;
retinoid
antineoplastic agent2005200519.0medium000100
tretinoinretinoic acid;
vitamin A
anti-inflammatory agent;
antineoplastic agent;
antioxidant;
AP-1 antagonist;
human metabolite;
keratolytic drug;
retinoic acid receptor agonist;
retinoid X receptor agonist;
signalling molecule
2005200519.0medium000100
alitretinoinretinoic acidantineoplastic agent;
keratolytic drug;
metabolite;
retinoid X receptor agonist
2005200519.0medium000100
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Benign Neoplasms02005200519.0medium000100
Cancer of Cervix01996199628.0medium001000
Cancer of Mouth01997199727.0medium001000
Carcinoma, Epidermoid01997199727.0medium001000
Carcinoma, Squamous Cell01997199727.0medium001000
Mouth Neoplasms01997199727.0medium001000
Neoplasms02005200519.0medium000100
Sensitivity and Specificity02003200321.0medium000100
Uterine Cervical Neoplasms01996199628.0medium001000

Dosage (1)

ArticleYear
A novel retinoic acid receptor-selective retinoid, ALRT1550, has potent antitumor activity against human oral squamous carcinoma xenografts in nude mice.
Cancer research, , Jan-01, Volume: 57, Issue:1
1997