gsk5182 profile

GSK5182: an estrogen-related receptor gamma inverse agonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	6852176
CHEMBL ID	201013
SCHEMBL ID	20534177
MeSH ID	M0587202

Synonym
TXF ,
gsk5182
(z)-4-(1-{4-[2-(dimethylamino)ethoxy]phenyl}-5-hydroxy-2-phenylpent-1-enyl)phenol
bdbm22435
gsk 5182
4-[(1z)-1-{4-[2-(dimethylamino)ethoxy]phenyl}-5-hydroxy-2-phenylpent-1-en-1-yl]phenol
2EWP
CHEMBL201013
877387-37-6
gsk-5182
4-[(z)-1-[4-(2-dimethylaminoethoxy)phenyl]-5-hydroxy-2-phenylpent-1-enyl]phenol
gtpl8908
(z)-4-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-5-hydroxy-2-phenylpent-1-en-1-yl)phenol
4-[(z)-1-[4-(2-dimethylaminoethyloxy)phenyl]-hydroxy-2-phenylpent-1-enyl]phenol
EX-A2580
4-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-5-hydroxy-2-phenylpent-1-en-1-yl)phenol
SCHEMBL20534177
Q27077910
MS-27290
(e/z)-gsk5182
HY-111226A
CS-0113537
AC-36159
S3449
4-[(z)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-5-hydroxy-2-phenylpent-1-enyl]phenol
AKOS040759231
AKOS040759377

Excerpt	Reference	Relevance
"GSK5182 treatment enhanced the membrane localization of NIS in both ATC cell lines."	( Inverse Agonist of Estrogen-Related Receptor γ Enhances Sodium Iodide Symporter Function Through Mitogen-Activated Protein Kinase Signaling in Anaplastic Thyroid Cancer Cells. Ahn, BC; Cho, SJ; Ha, JH; Jeon, YH; Jeong, SY; Kim, J; Kim, SH; Lee, IK; Lee, J; Lee, SW; Singh, TD, 2015)	1.14
"Treatment with GSK5182 resulted in dose- and time-dependent increases in iodide uptake in ATC cells, which were accompanied by both the downregulation of ERRγ protein and the activation of extracellular signal-regulated kinase (ERK) 1/2. "	( Inverse Agonist of Estrogen-Related Receptor γ Enhances Sodium Iodide Symporter Function Through Mitogen-Activated Protein Kinase Signaling in Anaplastic Thyroid Cancer Cells. Ahn, BC; Cho, SJ; Ha, JH; Jeon, YH; Jeong, SY; Kim, J; Kim, SH; Lee, IK; Lee, J; Lee, SW; Singh, TD, 2015)	0.77

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Chain A, Estrogen-related receptor gamma	Homo sapiens (human)	IC50 (µMol)	0.0790	0.0790	0.0790	0.0790	AID977608
Steroid hormone receptor ERR2	Homo sapiens (human)	IC50 (µMol)	7.8333	0.3950	1.3577	3.5000	AID1432443; AID1686565; AID1704116
Estrogen receptor	Homo sapiens (human)	IC50 (µMol)	1.0618	0.0000	0.7237	32.7000	AID1686566; AID1704117; AID1798194; AID260520
Steroid hormone receptor ERR1	Homo sapiens (human)	IC50 (µMol)	10.0000	0.0020	1.1663	9.6400	AID1686564; AID1704115
Estrogen-related receptor gamma	Homo sapiens (human)	IC50 (µMol)	0.1464	0.0020	0.2273	2.0000	AID1686562; AID1704113; AID1704157; AID1798194; AID260519; AID260522
Estrogen-related receptor gamma	Mus musculus (house mouse)	IC50 (µMol)	2.7000	0.6000	1.6500	2.7000	AID1432444
Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)	IC50 (µMol)	30.0000	0.0009	1.9014	10.0000	AID1686575; AID1704131
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
embryonic placenta development	Steroid hormone receptor ERR2	Homo sapiens (human)
regulation of DNA-templated transcription	Steroid hormone receptor ERR2	Homo sapiens (human)
stem cell division	Steroid hormone receptor ERR2	Homo sapiens (human)
stem cell population maintenance	Steroid hormone receptor ERR2	Homo sapiens (human)
cell dedifferentiation	Steroid hormone receptor ERR2	Homo sapiens (human)
photoreceptor cell maintenance	Steroid hormone receptor ERR2	Homo sapiens (human)
positive regulation of DNA-templated transcription	Steroid hormone receptor ERR2	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Steroid hormone receptor ERR2	Homo sapiens (human)
inner ear development	Steroid hormone receptor ERR2	Homo sapiens (human)
positive regulation of stem cell population maintenance	Steroid hormone receptor ERR2	Homo sapiens (human)
regulation of stem cell division	Steroid hormone receptor ERR2	Homo sapiens (human)
negative regulation of stem cell differentiation	Steroid hormone receptor ERR2	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Steroid hormone receptor ERR2	Homo sapiens (human)
intracellular steroid hormone receptor signaling pathway	Steroid hormone receptor ERR2	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Estrogen receptor	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Estrogen receptor	Homo sapiens (human)
antral ovarian follicle growth	Estrogen receptor	Homo sapiens (human)
epithelial cell development	Estrogen receptor	Homo sapiens (human)
chromatin remodeling	Estrogen receptor	Homo sapiens (human)
regulation of DNA-templated transcription	Estrogen receptor	Homo sapiens (human)
signal transduction	Estrogen receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Estrogen receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Estrogen receptor	Homo sapiens (human)
androgen metabolic process	Estrogen receptor	Homo sapiens (human)
male gonad development	Estrogen receptor	Homo sapiens (human)
negative regulation of gene expression	Estrogen receptor	Homo sapiens (human)
positive regulation of phospholipase C activity	Estrogen receptor	Homo sapiens (human)
intracellular steroid hormone receptor signaling pathway	Estrogen receptor	Homo sapiens (human)
intracellular estrogen receptor signaling pathway	Estrogen receptor	Homo sapiens (human)
response to estradiol	Estrogen receptor	Homo sapiens (human)
regulation of toll-like receptor signaling pathway	Estrogen receptor	Homo sapiens (human)
negative regulation of smooth muscle cell apoptotic process	Estrogen receptor	Homo sapiens (human)
negative regulation of canonical NF-kappaB signal transduction	Estrogen receptor	Homo sapiens (human)
negative regulation of DNA-binding transcription factor activity	Estrogen receptor	Homo sapiens (human)
response to estrogen	Estrogen receptor	Homo sapiens (human)
positive regulation of DNA-templated transcription	Estrogen receptor	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Estrogen receptor	Homo sapiens (human)
fibroblast proliferation	Estrogen receptor	Homo sapiens (human)
positive regulation of fibroblast proliferation	Estrogen receptor	Homo sapiens (human)
stem cell differentiation	Estrogen receptor	Homo sapiens (human)
regulation of inflammatory response	Estrogen receptor	Homo sapiens (human)
positive regulation of DNA-binding transcription factor activity	Estrogen receptor	Homo sapiens (human)
RNA polymerase II preinitiation complex assembly	Estrogen receptor	Homo sapiens (human)
uterus development	Estrogen receptor	Homo sapiens (human)
vagina development	Estrogen receptor	Homo sapiens (human)
prostate epithelial cord elongation	Estrogen receptor	Homo sapiens (human)
prostate epithelial cord arborization involved in prostate glandular acinus morphogenesis	Estrogen receptor	Homo sapiens (human)
regulation of branching involved in prostate gland morphogenesis	Estrogen receptor	Homo sapiens (human)
mammary gland branching involved in pregnancy	Estrogen receptor	Homo sapiens (human)
mammary gland alveolus development	Estrogen receptor	Homo sapiens (human)
epithelial cell proliferation involved in mammary gland duct elongation	Estrogen receptor	Homo sapiens (human)
protein localization to chromatin	Estrogen receptor	Homo sapiens (human)
cellular response to estradiol stimulus	Estrogen receptor	Homo sapiens (human)
negative regulation of miRNA transcription	Estrogen receptor	Homo sapiens (human)
regulation of epithelial cell apoptotic process	Estrogen receptor	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Estrogen receptor	Homo sapiens (human)
cellular response to estrogen stimulus	Estrogen receptor	Homo sapiens (human)
regulation of DNA-templated transcription	Steroid hormone receptor ERR1	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Steroid hormone receptor ERR1	Homo sapiens (human)
intracellular steroid hormone receptor signaling pathway	Steroid hormone receptor ERR1	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Steroid hormone receptor ERR1	Homo sapiens (human)
regulation of DNA-templated transcription	Estrogen-related receptor gamma	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Estrogen-related receptor gamma	Homo sapiens (human)
retinoic acid receptor signaling pathway	Estrogen-related receptor gamma	Homo sapiens (human)
positive regulation of cold-induced thermogenesis	Estrogen-related receptor gamma	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Estrogen-related receptor gamma	Homo sapiens (human)
intracellular steroid hormone receptor signaling pathway	Estrogen-related receptor gamma	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by hormone	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of DNA-templated transcription	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion homeostasis	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cardiac muscle contraction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cellular response to xenobiotic stimulus	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane depolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion import across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Steroid hormone receptor ERR2	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Steroid hormone receptor ERR2	Homo sapiens (human)
cis-regulatory region sequence-specific DNA binding	Steroid hormone receptor ERR2	Homo sapiens (human)
RNA polymerase II complex binding	Steroid hormone receptor ERR2	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	Steroid hormone receptor ERR2	Homo sapiens (human)
DNA-binding transcription factor activity	Steroid hormone receptor ERR2	Homo sapiens (human)
nuclear steroid receptor activity	Steroid hormone receptor ERR2	Homo sapiens (human)
steroid binding	Steroid hormone receptor ERR2	Homo sapiens (human)
zinc ion binding	Steroid hormone receptor ERR2	Homo sapiens (human)
sequence-specific DNA binding	Steroid hormone receptor ERR2	Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor binding	Steroid hormone receptor ERR2	Homo sapiens (human)
sequence-specific double-stranded DNA binding	Steroid hormone receptor ERR2	Homo sapiens (human)
estrogen response element binding	Steroid hormone receptor ERR2	Homo sapiens (human)
nuclear receptor activity	Steroid hormone receptor ERR2	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Estrogen receptor	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Estrogen receptor	Homo sapiens (human)
TFIIB-class transcription factor binding	Estrogen receptor	Homo sapiens (human)
transcription coregulator binding	Estrogen receptor	Homo sapiens (human)
transcription corepressor binding	Estrogen receptor	Homo sapiens (human)
transcription coactivator binding	Estrogen receptor	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	Estrogen receptor	Homo sapiens (human)
chromatin binding	Estrogen receptor	Homo sapiens (human)
DNA-binding transcription factor activity	Estrogen receptor	Homo sapiens (human)
nuclear receptor activity	Estrogen receptor	Homo sapiens (human)
steroid binding	Estrogen receptor	Homo sapiens (human)
protein binding	Estrogen receptor	Homo sapiens (human)
calmodulin binding	Estrogen receptor	Homo sapiens (human)
beta-catenin binding	Estrogen receptor	Homo sapiens (human)
zinc ion binding	Estrogen receptor	Homo sapiens (human)
TBP-class protein binding	Estrogen receptor	Homo sapiens (human)
enzyme binding	Estrogen receptor	Homo sapiens (human)
protein kinase binding	Estrogen receptor	Homo sapiens (human)
nitric-oxide synthase regulator activity	Estrogen receptor	Homo sapiens (human)
nuclear estrogen receptor activity	Estrogen receptor	Homo sapiens (human)
nuclear estrogen receptor binding	Estrogen receptor	Homo sapiens (human)
estrogen response element binding	Estrogen receptor	Homo sapiens (human)
identical protein binding	Estrogen receptor	Homo sapiens (human)
ATPase binding	Estrogen receptor	Homo sapiens (human)
14-3-3 protein binding	Estrogen receptor	Homo sapiens (human)
sequence-specific double-stranded DNA binding	Estrogen receptor	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Steroid hormone receptor ERR1	Homo sapiens (human)
DNA-binding transcription factor activity	Steroid hormone receptor ERR1	Homo sapiens (human)
nuclear steroid receptor activity	Steroid hormone receptor ERR1	Homo sapiens (human)
steroid binding	Steroid hormone receptor ERR1	Homo sapiens (human)
protein binding	Steroid hormone receptor ERR1	Homo sapiens (human)
zinc ion binding	Steroid hormone receptor ERR1	Homo sapiens (human)
protein domain specific binding	Steroid hormone receptor ERR1	Homo sapiens (human)
sequence-specific DNA binding	Steroid hormone receptor ERR1	Homo sapiens (human)
sequence-specific double-stranded DNA binding	Steroid hormone receptor ERR1	Homo sapiens (human)
estrogen response element binding	Steroid hormone receptor ERR1	Homo sapiens (human)
nuclear receptor activity	Steroid hormone receptor ERR1	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Estrogen-related receptor gamma	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	Estrogen-related receptor gamma	Homo sapiens (human)
nuclear steroid receptor activity	Estrogen-related receptor gamma	Homo sapiens (human)
steroid binding	Estrogen-related receptor gamma	Homo sapiens (human)
protein binding	Estrogen-related receptor gamma	Homo sapiens (human)
zinc ion binding	Estrogen-related receptor gamma	Homo sapiens (human)
AF-2 domain binding	Estrogen-related receptor gamma	Homo sapiens (human)
sequence-specific double-stranded DNA binding	Estrogen-related receptor gamma	Homo sapiens (human)
estrogen response element binding	Estrogen-related receptor gamma	Homo sapiens (human)
nuclear receptor activity	Estrogen-related receptor gamma	Homo sapiens (human)
transcription cis-regulatory region binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
delayed rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ubiquitin protein ligase binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
identical protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein homodimerization activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
C3HC4-type RING finger domain binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
scaffold protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
integrator complex	Steroid hormone receptor ERR2	Homo sapiens (human)
condensed chromosome	Steroid hormone receptor ERR2	Homo sapiens (human)
nucleus	Steroid hormone receptor ERR2	Homo sapiens (human)
nucleoplasm	Steroid hormone receptor ERR2	Homo sapiens (human)
cytoplasm	Steroid hormone receptor ERR2	Homo sapiens (human)
cytosol	Steroid hormone receptor ERR2	Homo sapiens (human)
chromatin	Steroid hormone receptor ERR2	Homo sapiens (human)
nucleus	Steroid hormone receptor ERR2	Homo sapiens (human)
nucleus	Estrogen receptor	Homo sapiens (human)
nucleoplasm	Estrogen receptor	Homo sapiens (human)
transcription regulator complex	Estrogen receptor	Homo sapiens (human)
cytoplasm	Estrogen receptor	Homo sapiens (human)
Golgi apparatus	Estrogen receptor	Homo sapiens (human)
cytosol	Estrogen receptor	Homo sapiens (human)
plasma membrane	Estrogen receptor	Homo sapiens (human)
membrane	Estrogen receptor	Homo sapiens (human)
chromatin	Estrogen receptor	Homo sapiens (human)
euchromatin	Estrogen receptor	Homo sapiens (human)
protein-containing complex	Estrogen receptor	Homo sapiens (human)
nucleus	Estrogen receptor	Homo sapiens (human)
fibrillar center	Steroid hormone receptor ERR1	Homo sapiens (human)
nucleus	Steroid hormone receptor ERR1	Homo sapiens (human)
nucleoplasm	Steroid hormone receptor ERR1	Homo sapiens (human)
cytoplasm	Steroid hormone receptor ERR1	Homo sapiens (human)
microtubule cytoskeleton	Steroid hormone receptor ERR1	Homo sapiens (human)
intercellular bridge	Steroid hormone receptor ERR1	Homo sapiens (human)
chromatin	Steroid hormone receptor ERR1	Homo sapiens (human)
nucleus	Steroid hormone receptor ERR1	Homo sapiens (human)
nucleoplasm	Estrogen-related receptor gamma	Homo sapiens (human)
chromatin	Estrogen-related receptor gamma	Homo sapiens (human)
nucleus	Estrogen-related receptor gamma	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cell surface	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
perinuclear region of cytoplasm	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (46)

Assay ID	Title	Year	Journal	Article
AID1686569	Inhibition of CYP2C19 in human liver microsomes assessed as reduction in S-mephenytoin 4-hydroxylase activity at 10 uM preincubated for 5 mins followed by addition of NADPH-regenerating system and measured after 15 mins by LC-MS/MS analysis relative to co	2016	Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22	Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists.
AID1432442	Inverse agonist activity at GAL4-DNA binding domain-fused human ERRalpha ligand binding domain expressed in African green monkey CV1 cells assessed as decrease in receptor transcriptional activity at 10 uM after 45 hrs by luciferase reporter gene assay	2017	Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5	Identification of novel inverse agonists of estrogen-related receptors ERRγ and ERRβ.
AID1704124	Inhibition of CYP2D6 (unknown origin) in liver microsomes at 10 uM incubated for 15 mins relative to control	2020	European journal of medicinal chemistry, Nov-01, Volume: 205	An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.
AID1704117	Binding affinity to ERalpha (unknown origin) by TR-FRET assay	2020	European journal of medicinal chemistry, Nov-01, Volume: 205	An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.
AID260521	Selectivity for ERRgamma over ERalpha relative to 4-hydroxytamoxifen	2006	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4	Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
AID1686563	Inverse agonist activity at Gal4-fused ERRgamma (unknown origin) expressed in human AD293 cells assessed as decrease in luciferase activity at 10 uM incubated for 24 hrs by luciferase reporter gene assay relative to control	2016	Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22	Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists.
AID1704128	Metabolic stability in rat liver microsomes assessed as parent compound remaining	2020	European journal of medicinal chemistry, Nov-01, Volume: 205	An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.
AID1704127	Metabolic stability in dog liver microsomes assessed as parent compound remaining	2020	European journal of medicinal chemistry, Nov-01, Volume: 205	An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.
AID1686573	Metabolic stability in rat liver microsome assessed as parent compound remaining at 1 uM incubated for 30 mins in presence of NADPH generating system by LC-MS/MS analysis	2016	Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22	Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists.
AID1704125	Inhibition of CYP3A4 (unknown origin) in liver microsomes at 10 uM incubated for 15 mins relative to control	2020	European journal of medicinal chemistry, Nov-01, Volume: 205	An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.
AID1704123	Inhibition of CYP2C19 (unknown origin) in liver microsomes at 10 uM incubated for 15 mins relative to control	2020	European journal of medicinal chemistry, Nov-01, Volume: 205	An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.
AID260524	Repression of transcriptional activity in ERRgamma transfected HeLa cell luciferase assay at 1 uM	2006	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4	Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
AID1686565	Binding affinity to GST-tagged ERRbeta LBD (unknown origin) using fluorescein PGC1alpha as coactivator incubated for 1 hr by LanthaScreen TR-FRET co-regulator assay	2016	Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22	Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists.
AID260520	Displacement of [3H]estradiol from ERalpha	2006	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4	Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
AID1704113	Binding affinity to ERRgamma (unknown origin) by TR-FRET assay	2020	European journal of medicinal chemistry, Nov-01, Volume: 205	An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.
AID260519	Displacement of [3H]4-OHT from ERRgamma	2006	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4	Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
AID1686576	Clearance in Sprague-Dawley rat at 10 mg/kg, po or 1 mg/kg, iv measured upto 8 hrs by LC-MS/MS analysis	2016	Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22	Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists.
AID1686566	Binding affinity to GST-tagged ERalpha LBD (unknown origin) using fluorescein PGC1alpha as coactivator incubated for 1 hr by LanthaScreen TR-FRET co-regulator assay	2016	Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22	Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists.
AID1704115	Binding affinity to ERRalpha (unknown origin) by TR-FRET assay	2020	European journal of medicinal chemistry, Nov-01, Volume: 205	An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.
AID1704130	Permeability of compound incubated for 5 hrs by PAMPA assay	2020	European journal of medicinal chemistry, Nov-01, Volume: 205	An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.
AID1686575	Inhibition of human ERG measured after 4 hrs by fluorescence polarization assay	2016	Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22	Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists.
AID260522	Inhibition of interaction between ERRgamma and NR cofactor RIP140 in FRET assay	2006	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4	Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
AID1686571	Inhibition of CYP3A4 in human liver microsomes assessed as reduction in midazolam 1-hydroxylase activity at 10 uM preincubated for 5 mins followed by addition of NADPH-regenerating system and measured after 15 mins by LC-MS/MS analysis relative to control	2016	Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22	Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists.
AID1704116	Binding affinity to ERRbeta (unknown origin) by TR-FRET assay	2020	European journal of medicinal chemistry, Nov-01, Volume: 205	An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.
AID1686570	Inhibition of CYP2D6 in human liver microsomes assessed as reduction in dextromethorphan O-demethylase activity at 10 uM preincubated for 5 mins followed by addition of NADPH-regenerating system and measured after 15 mins by LC-MS/MS analysis relative to	2016	Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22	Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists.
AID1704114	Inverse agonist activity at ERRgamma (unknown origin) assessed as receptor mediated luciferase activity at 10 uM by luciferase reporter gene assay relative to control	2020	European journal of medicinal chemistry, Nov-01, Volume: 205	An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.
AID1704122	Inhibition of CYP2C9 (unknown origin) in liver microsomes at 10 uM incubated for 15 mins relative to control	2020	European journal of medicinal chemistry, Nov-01, Volume: 205	An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.
AID1704129	Metabolic stability in mouse liver microsomes assessed as parent compound remaining	2020	European journal of medicinal chemistry, Nov-01, Volume: 205	An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.
AID1686562	Binding affinity to GST-tagged ERRgamma LBD (unknown origin) using fluorescein PGC1alpha as coactivator incubated for 1 hr by LanthaScreen TR-FRET co-regulator assay	2016	Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22	Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists.
AID1686564	Binding affinity to GST-tagged ERRalpha LBD (unknown origin) using fluorescein PGC1alpha as coactivator incubated for 1 hr by LanthaScreen TR-FRET co-regulator assay	2016	Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22	Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists.
AID1704126	Metabolic stability in human liver microsomes assessed as parent compound remaining	2020	European journal of medicinal chemistry, Nov-01, Volume: 205	An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.
AID1686567	Inhibition of CYP1A2 in human liver microsomes assessed as reduction in phenacetin O-deethylase activity at 10 uM preincubated for 5 mins followed by addition of NADPH-regenerating system and measured after 15 mins by LC-MS/MS analysis relative to control	2016	Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22	Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists.
AID1704121	Inhibition of CYP1A2 (unknown origin) in liver microsomes at 10 uM incubated for 15 mins relative to control	2020	European journal of medicinal chemistry, Nov-01, Volume: 205	An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.
AID1432444	Inverse agonist activity at GAL4-DNA binding domain-fused mouse ERRgamma ligand binding domain expressed in African green monkey CV1 cells assessed as decrease in receptor transcriptional activity after 45 hrs by luciferase reporter gene assay	2017	Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5	Identification of novel inverse agonists of estrogen-related receptors ERRγ and ERRβ.
AID1686574	Effective permeability of compound at 10 uM in PBS buffer at pH 7.4 after 5 hrs by LC-MS/MS analysis based PAMPA method	2016	Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22	Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists.
AID260523	Repression of transcriptional activity in ERalpha transfected HeLa cell luciferase assay at 1 uM	2006	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4	Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
AID1432443	Inverse agonist activity at GAL4-DNA binding domain-fused human ERRbeta ligand binding domain expressed in African green monkey CV1 cells assessed as decrease in receptor transcriptional activity after 45 hrs by luciferase reporter gene assay	2017	Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5	Identification of novel inverse agonists of estrogen-related receptors ERRγ and ERRβ.
AID1686572	Metabolic stability in human liver microsome assessed as parent compound remaining at 1 uM incubated for 30 mins in presence of NADPH generating system by LC-MS/MS analysis	2016	Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22	Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists.
AID1704131	Inhibition of human ERG by fluorescence polarization assay	2020	European journal of medicinal chemistry, Nov-01, Volume: 205	An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.
AID1704157	Inverse agonist activity at ERRgamma (unknown origin) by luciferase reporter gene assay	2020	European journal of medicinal chemistry, Nov-01, Volume: 205	An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.
AID1686568	Inhibition of CYP2C9 in human liver microsomes assessed as reduction in tolbutamide 4-hydroxylase activity at 10 uM preincubated for 5 mins followed by addition of NADPH-regenerating system and measured after 15 mins by LC-MS/MS analysis relative to contr	2016	Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22	Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists.
AID1798194	Radioligand Displacement Assay from Article 10.1016/j.bmcl.2005.11.030: \\Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.\\	2006	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4	Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
AID1811	Experimentally measured binding affinity data derived from PDB	2006	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4	Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
AID977608	Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB	2006	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4	Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
AID1346845	Human Estrogen receptor-alpha (3A. Estrogen receptors)	2006	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4	Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
AID1346836	Human Estrogen-related receptor-gamma (3B. Estrogen-related receptors)	2006	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4	Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
[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	2 (7.14)	29.6817
2010's	14 (50.00)	24.3611
2020's	12 (42.86)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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	28 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
glutamine Glutamine: A non-essential amino acid present abundantly throughout the body and is involved in many metabolic processes. It is synthesized from GLUTAMIC ACID and AMMONIA. It is the principal carrier of NITROGEN in the body and is an important energy source for many cells.. L-glutamine : An optically active form of glutamine having L-configuration.. glutamine : An alpha-amino acid that consists of butyric acid bearing an amino substituent at position 2 and a carbamoyl substituent at position 4.	2.25	1	amino acid zwitterion; glutamine family amino acid; glutamine; L-alpha-amino acid; polar amino acid zwitterion; proteinogenic amino acid	EC 1.14.13.39 (nitric oxide synthase) inhibitor; Escherichia coli metabolite; human metabolite; metabolite; micronutrient; mouse metabolite; nutraceutical; Saccharomyces cerevisiae metabolite
rotenone Derris: A plant genus of the family FABACEAE. The root is a source of rotenoids (ROTENONE) and flavonoids. Some species of Pongamia have been reclassified to this genus and some to MILLETTIA. Some species of Deguelia have been reclassified to this genus.. rotenoid : Members of the class of tetrahydrochromenochromene that consists of a cis-fused tetrahydrochromeno[3,4-b]chromene skeleton and its substituted derivatives. The term was originally restricted to natural products, but is now also used to describe semi-synthetic and fully synthetic compounds.	2.25	1	organic heteropentacyclic compound; rotenones	antineoplastic agent; metabolite; mitochondrial NADH:ubiquinone reductase inhibitor; phytogenic insecticide; piscicide; toxin
chenodeoxycholic acid Chenodeoxycholic Acid: A bile acid, usually conjugated with either glycine or taurine. It acts as a detergent to solubilize fats for intestinal absorption and is reabsorbed by the small intestine. It is used as cholagogue, a choleretic laxative, and to prevent or dissolve gallstones.. chenodeoxycholic acid : A dihydroxy-5beta-cholanic acid that is (5beta)-cholan-24-oic acid substituted by hydroxy groups at positions 3 and 7 respectively.. chenodeoxycholate : Conjugate base of chenodeoxycholic acid; major species at pH 7.3.	2.6	1	bile acid; C24-steroid; dihydroxy-5beta-cholanic acid	human metabolite; mouse metabolite
gold Gold: A yellow metallic element with the atomic symbol Au, atomic number 79, and atomic weight 197. It is used in jewelry, goldplating of other metals, as currency, and in dental restoration. Many of its clinical applications, such as ANTIRHEUMATIC AGENTS, are in the form of its salts.	2.15	1	copper group element atom; elemental gold
paclitaxel Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).	2.25	1	taxane diterpenoid; tetracyclic diterpenoid	antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent
4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol [no description available]	2.47	2	stilbenoid
fibrinogen Fibrinogen: Plasma glycoprotein clotted by thrombin, composed of a dimer of three non-identical pairs of polypeptide chains (alpha, beta, gamma) held together by disulfide bonds. Fibrinogen clotting is a sol-gel change involving complex molecular arrangements: whereas fibrinogen is cleaved by thrombin to form polypeptides A and B, the proteolytic action of other enzymes yields different fibrinogen degradation products.. D-iditol : The D-enantiomer of iditol.	2.17	1	iditol	fungal metabolite
tretinoin Tretinoin: An important regulator of GENE EXPRESSION during growth and development, and in NEOPLASMS. Tretinoin, also known as retinoic acid and derived from maternal VITAMIN A, is essential for normal GROWTH; and EMBRYONIC DEVELOPMENT. An excess of tretinoin can be teratogenic. It is used in the treatment of PSORIASIS; ACNE VULGARIS; and several other SKIN DISEASES. It has also been approved for use in promyelocytic leukemia (LEUKEMIA, PROMYELOCYTIC, ACUTE).. retinoic acid : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraenoic acid substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified).. all-trans-retinoic acid : A retinoic acid in which all four exocyclic double bonds have E- (trans-) geometry.	2.25	1	retinoic 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
afimoxifene afimoxifene : A tertiary amino compound that is tamoxifen in which the phenyl group which is in a Z- relationship to the ethyl substituent is hydroxylated at the para- position. It is the active metabolite of tamoxifen.	2.03	1	phenols; tertiary amino compound	antineoplastic agent; estrogen receptor antagonist; metabolite
enclomiphene Enclomiphene: The trans or (E)-isomer of clomiphene.	2.61	2
tamoxifen [no description available]	4.5	20	stilbenoid; tertiary amino compound	angiogenesis inhibitor; antineoplastic agent; bone density conservation agent; EC 1.2.3.1 (aldehyde oxidase) inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; estrogen antagonist; estrogen receptor antagonist; estrogen receptor modulator
4-hydroxytoremifene 4-hydroxytoremifene: metabolite of toremifene; RN refers to (Z)-isomer; structure in first source	2.03	1
dasatinib N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source. dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN).	2.25	1	1,3-thiazoles; aminopyrimidine; monocarboxylic acid amide; N-(2-hydroxyethyl)piperazine; N-arylpiperazine; organochlorine compound; secondary amino compound; tertiary amino compound	anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor
furylfuramide Furylfuramide: Used formerly as antimicrobial food additive. It causes mutations in many cell cultures and may be carcinogenic.. (Z)-2-(2-furyl)-3-(5-nitro-2-furyl)acrylamide : A member of the class of acrylamides that is acrylamide which is substituted at positions 2 and 3 by 2-furyl and 5-nitro-2-furyl groups, respectively (the trans isomer). Formerly used as a food preservative, it was withdrawn from the market following suspicions of carcenogenicity.	2.41	1	acrylamides; C-nitro compound; nitrofuran antibiotic; primary carboxamide
glyceryl 2-arachidonate glyceryl 2-arachidonate: binds to cannabinoid receptors; structure in first source. 2-arachidonoylglycerol : An endocannabinoid and an endogenous agonist of the cannabinoid receptors (CB1 and CB2). It is an ester formed from omega-6-arachidonic acid and glycerol.	2.25	1	2-acylglycerol 20:4; endocannabinoid	human metabolite
afimoxifene [no description available]	2.03	1
arachidonyl-2-chloroethylamide arachidonyl-2-chloroethylamide: a potent and selective agonist of the neuronal cannabinoid receptor; structure in first source. arachidonyl-2'-chloroethylamide : A fatty amide obtained by the formal condensation of arachidonic acid with 2-chloroethanamine. It is a potent agonist of the CB1 receptor (Ki = 1.4 nM) and also has a low affinity for the CB2 receptor (Ki = 3100 nM).	2.25	1	fatty amide; organochlorine compound; secondary carboxamide; synthetic cannabinoid	CB1 receptor agonist; CB2 receptor agonist; neuroprotective agent
afimoxifene [no description available]	2.15	1
vx680 [no description available]	2.25	1	N-arylpiperazine
atrial natriuretic factor Atrial Natriuretic Factor: A potent natriuretic and vasodilatory peptide or mixture of different-sized low molecular weight PEPTIDES derived from a common precursor and secreted mainly by the HEART ATRIUM. All these peptides share a sequence of about 20 AMINO ACIDS.	2.08	1	polypeptide

Condition	Relationship Strength	Studies
Cancer of the Thyroid [description not available]	2.57	2
Thyroid Neoplasms Tumors or cancer of the THYROID GLAND.	2.57	2
Acute Brain Injuries [description not available]	3.52	4
Hemorrhage, Subarachnoid [description not available]	3.52	4
Brain Injuries Acute and chronic (see also BRAIN INJURIES, CHRONIC) injuries to the brain, including the cerebral hemispheres, CEREBELLUM, and BRAIN STEM. Clinical manifestations depend on the nature of injury. Diffuse trauma to the brain is frequently associated with DIFFUSE AXONAL INJURY or COMA, POST-TRAUMATIC. Localized injuries may be associated with NEUROBEHAVIORAL MANIFESTATIONS; HEMIPARESIS, or other focal neurologic deficits.	3.52	4
Subarachnoid Hemorrhage Bleeding into the intracranial or spinal SUBARACHNOID SPACE, most resulting from INTRACRANIAL ANEURYSM rupture. It can occur after traumatic injuries (SUBARACHNOID HEMORRHAGE, TRAUMATIC). Clinical features include HEADACHE; NAUSEA; VOMITING, nuchal rigidity, variable neurological deficits and reduced mental status.	3.52	4
Cirrhosis, Liver [description not available]	2.6	1
Liver Cirrhosis Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules.	2.6	1
Hepatocellular Carcinoma [description not available]	2.6	1
Cancer of Liver [description not available]	2.6	1
Carcinoma, Hepatocellular A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested.	2.6	1
Liver Neoplasms Tumors or cancer of the LIVER.	2.6	1
Breast Cancer [description not available]	2.25	1
Breast Neoplasms Tumors or cancer of the human BREAST.	2.25	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.53	2
Innate Inflammatory Response [description not available]	2.15	1
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	2.15	1
Infections, Salmonella [description not available]	2.17	1
Cardiac Hypertrophy Enlargement of the HEART due to chamber HYPERTROPHY, an increase in wall thickness without an increase in the number of cells (MYOCYTES, CARDIAC). It is the result of increase in myocyte size, mitochondrial and myofibrillar mass, as well as changes in extracellular matrix.	2.08	1
Cardiomegaly Enlargement of the HEART, usually indicated by a cardiothoracic ratio above 0.50. Heart enlargement may involve the right, the left, or both HEART VENTRICLES or HEART ATRIA. Cardiomegaly is a nonspecific symptom seen in patients with chronic systolic heart failure (HEART FAILURE) or several forms of CARDIOMYOPATHIES.	2.08	1
Thyroid Cancer, Anaplastic [description not available]	2.11	1
Thyroid Carcinoma, Anaplastic An aggressive THYROID GLAND malignancy which generally occurs in IODINE-deficient areas in people with previous thyroid pathology such as GOITER. It is associated with CELL DEDIFFERENTIATION of THYROID CARCINOMA (e.g., FOLLICULAR THYROID CARCINOMA; PAPILLARY THYROID CANCER). Typical initial presentation is a rapidly growing neck mass which upon metastasis is associated with DYSPHAGIA; NECK PAIN; bone pain; DYSPNEA; and NEUROLOGIC DEFICITS.	2.11	1
Vascular Calcification Deposition of calcium into the blood vessel structures. Excessive calcification of the vessels are associated with ATHEROSCLEROTIC PLAQUES formation particularly after MYOCARDIAL INFARCTION (see MONCKEBERG MEDIAL CALCIFIC SCLEROSIS) and chronic kidney diseases which in turn increase VASCULAR STIFFNESS.	2.11	1
Aortic Diseases Pathological processes involving any part of the AORTA.	2.11	1
Alcoholic Liver Diseases [description not available]	2.08	1
Liver Diseases, Alcoholic Liver diseases associated with ALCOHOLISM. It usually refers to the coexistence of two or more subentities, i.e., ALCOHOLIC FATTY LIVER; ALCOHOLIC HEPATITIS; and ALCOHOLIC CIRRHOSIS.	2.08	1

gsk5182

Description

Cross-References

Synonyms (27)

Research Excerpts

Treatment

Protein Targets (7)

Inhibition Measurements

Biological Processes (74)

Molecular Functions (43)

Ceullar Components (20)

Bioassays (46)

Research

Studies (28)

Market Indicators

Research Demand Index: 21.66

Study Types

gsk5182

Description

Cross-References

Synonyms (27)

Research Excerpts

Treatment

Protein Targets (7)

Inhibition Measurements

Biological Processes (74)

Molecular Functions (43)

Ceullar Components (20)

Bioassays (46)

Research

Studies (28)

Market Indicators

Research Demand Index: 21.66

Study Types

Related Drugs (20)

Related Conditions (26)