zk 216348 profile

ZK 216348: ZK-209614 is the racemic mixture, ZK-216348 is the (+)-isomer, and ZK-216347 is the (-)-isomer; a selective glucocorticoid receptor agonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	9805004
CHEMBL ID	216272
SCHEMBL ID	17066437
MeSH ID	M0461211

Synonym
4-(2,3-dihydrobenzofuran-7-yl)-2-hydroxy-4-methyl-n-(4-methyl-1-oxo-1h-benzo[d][1,2]oxazin-6-yl)-2-(trifluoromethyl)pentanamide
bdbm50201099
CHEMBL216272 ,
zk-216348
zk 216348
gtpl8643
4-(2,3-dihydro-1-benzofuran-7-yl)-2-hydroxy-4-methyl-n-(4-methyl-1-oxo-2,3-benzoxazin-6-yl)-2-(trifluoromethyl)pentanamide
(+)-4-(2,3-dihydrobenzofuran-7-yl)-2-hydroxy-4-methyl-n-(4-methyl-1-oxo-1h-benzo[d][1,2]oxazin-6-yl)-2-(trifluoromethyl)pentanamide
(+)-zk 216348
zk216348
669073-68-1
7-benzofuranbutanamide, 2,3-dihydro-alpha-hydroxy-gamma,gamma-dimethyl-n-(4-methyl-1-oxo-1h-2,3-benzoxazin-6-yl)-alpha-(trifluoromethyl)-, (r-),(+)-
7-benzofuranbutanamide, 2,3-dihydro-alpha-hydroxy-gamma,gamma-dimethyl-n-(4-methyl-1-oxo-1h-2,3-benzoxazin-6-yl)-alpha-(trifluoromethyl)-, (+)-
zk 216348, (+)-
8by7xk862l ,
unii-8by7xk862l
SCHEMBL17066437
NCGC00386729-01
CS-0082547
HY-123352
Q27089293
vrzvkijrjrbqjt-uhfffaoysa-n
7-benzofuranbutanamide, 2,3-dihydro-.alpha.-hydroxy-.gamma.,.gamma.-dimethyl-n-(4-methyl-1-oxo-1h-2,3-benzoxazin-6-yl)-.alpha.-(trifluoromethyl)-, (r-),(+)-
7-benzofuranbutanamide, 2,3-dihydro-.alpha.-hydroxy-.gamma.,.gamma.-dimethyl-n-(4-methyl-1-oxo-1h-2,3-benzoxazin-6-yl)-.alpha.-(trifluoromethyl)-, (+)-
E99033
AKOS040742845
CS-0834294
HY-123352A
(-)-zk 216348

Excerpt	Reference	Relevance
" For this reason, one goal of research in the GC field is the development of new drugs, which show a reduced side-effect profile while maintaining the antiinflammatory and immunosuppressive properties of classical GCs."	( Dissociation of transactivation from transrepression by a selective glucocorticoid receptor agonist leads to separation of therapeutic effects from side effects. Asadullah, K; Döcke, WD; Hennekes, H; Jaroch, S; Rehwinkel, H; Schäcke, H; Schmees, N; Schottelius, A; Strehlke, P, 2004)	0.32

Excerpt	Reference	Relevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51

Protein Targets (6)

Potency Measurements

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	1.3450	0.0123	7.9835	43.2770	AID1645841
cytochrome P450 2D6	Homo sapiens (human)	Potency	26.8370	0.0010	8.3798	61.1304	AID1645840
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Glucocorticoid receptor	Homo sapiens (human)	IC50 (µMol)	0.0152	0.0000	0.4953	10.0000	AID274990; AID516371; AID516375; AID516377
Progesterone receptor	Homo sapiens (human)	IC50 (µMol)	0.0195	0.0000	0.5807	10.0000	AID274991; AID516372
Mineralocorticoid receptor	Homo sapiens (human)	IC50 (µMol)	0.0587	0.0003	0.7484	10.0000	AID274992; AID516373
Androgen receptor	Homo sapiens (human)	IC50 (µMol)	0.6310	0.0000	0.8753	10.0000	AID516374
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Glucocorticoid receptor	Homo sapiens (human)	EC50 (µMol)	0.0126	0.0004	0.0540	1.0000	AID516378
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (91)

Process	via Protein(s)	Taxonomy
negative regulation of transcription by RNA polymerase II	Glucocorticoid receptor	Homo sapiens (human)
regulation of gluconeogenesis	Glucocorticoid receptor	Homo sapiens (human)
chromatin organization	Glucocorticoid receptor	Homo sapiens (human)
regulation of DNA-templated transcription	Glucocorticoid receptor	Homo sapiens (human)
apoptotic process	Glucocorticoid receptor	Homo sapiens (human)
chromosome segregation	Glucocorticoid receptor	Homo sapiens (human)
signal transduction	Glucocorticoid receptor	Homo sapiens (human)
glucocorticoid metabolic process	Glucocorticoid receptor	Homo sapiens (human)
gene expression	Glucocorticoid receptor	Homo sapiens (human)
microglia differentiation	Glucocorticoid receptor	Homo sapiens (human)
adrenal gland development	Glucocorticoid receptor	Homo sapiens (human)
regulation of glucocorticoid biosynthetic process	Glucocorticoid receptor	Homo sapiens (human)
synaptic transmission, glutamatergic	Glucocorticoid receptor	Homo sapiens (human)
maternal behavior	Glucocorticoid receptor	Homo sapiens (human)
intracellular glucocorticoid receptor signaling pathway	Glucocorticoid receptor	Homo sapiens (human)
glucocorticoid mediated signaling pathway	Glucocorticoid receptor	Homo sapiens (human)
positive regulation of neuron apoptotic process	Glucocorticoid receptor	Homo sapiens (human)
negative regulation of DNA-templated transcription	Glucocorticoid receptor	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Glucocorticoid receptor	Homo sapiens (human)
astrocyte differentiation	Glucocorticoid receptor	Homo sapiens (human)
cell division	Glucocorticoid receptor	Homo sapiens (human)
mammary gland duct morphogenesis	Glucocorticoid receptor	Homo sapiens (human)
motor behavior	Glucocorticoid receptor	Homo sapiens (human)
cellular response to steroid hormone stimulus	Glucocorticoid receptor	Homo sapiens (human)
cellular response to glucocorticoid stimulus	Glucocorticoid receptor	Homo sapiens (human)
cellular response to dexamethasone stimulus	Glucocorticoid receptor	Homo sapiens (human)
cellular response to transforming growth factor beta stimulus	Glucocorticoid receptor	Homo sapiens (human)
neuroinflammatory response	Glucocorticoid receptor	Homo sapiens (human)
positive regulation of miRNA transcription	Glucocorticoid receptor	Homo sapiens (human)
intracellular steroid hormone receptor signaling pathway	Glucocorticoid receptor	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Glucocorticoid receptor	Homo sapiens (human)
ovulation from ovarian follicle	Progesterone receptor	Homo sapiens (human)
glandular epithelial cell maturation	Progesterone receptor	Homo sapiens (human)
regulation of DNA-templated transcription	Progesterone receptor	Homo sapiens (human)
signal transduction	Progesterone receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Progesterone receptor	Homo sapiens (human)
cell-cell signaling	Progesterone receptor	Homo sapiens (human)
positive regulation of gene expression	Progesterone receptor	Homo sapiens (human)
negative regulation of gene expression	Progesterone receptor	Homo sapiens (human)
paracrine signaling	Progesterone receptor	Homo sapiens (human)
negative regulation of phosphorylation	Progesterone receptor	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Progesterone receptor	Homo sapiens (human)
lung alveolus development	Progesterone receptor	Homo sapiens (human)
regulation of epithelial cell proliferation	Progesterone receptor	Homo sapiens (human)
progesterone receptor signaling pathway	Progesterone receptor	Homo sapiens (human)
maintenance of protein location in nucleus	Progesterone receptor	Homo sapiens (human)
tertiary branching involved in mammary gland duct morphogenesis	Progesterone receptor	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Progesterone receptor	Homo sapiens (human)
intracellular steroid hormone receptor signaling pathway	Progesterone receptor	Homo sapiens (human)
signal transduction	Mineralocorticoid receptor	Homo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transduction	Mineralocorticoid receptor	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Mineralocorticoid receptor	Homo sapiens (human)
intracellular steroid hormone receptor signaling pathway	Mineralocorticoid receptor	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Androgen receptor	Homo sapiens (human)
MAPK cascade	Androgen receptor	Homo sapiens (human)
in utero embryonic development	Androgen receptor	Homo sapiens (human)
regulation of systemic arterial blood pressure	Androgen receptor	Homo sapiens (human)
epithelial cell morphogenesis	Androgen receptor	Homo sapiens (human)
transcription by RNA polymerase II	Androgen receptor	Homo sapiens (human)
signal transduction	Androgen receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Androgen receptor	Homo sapiens (human)
cell-cell signaling	Androgen receptor	Homo sapiens (human)
spermatogenesis	Androgen receptor	Homo sapiens (human)
single fertilization	Androgen receptor	Homo sapiens (human)
positive regulation of cell population proliferation	Androgen receptor	Homo sapiens (human)
negative regulation of cell population proliferation	Androgen receptor	Homo sapiens (human)
positive regulation of gene expression	Androgen receptor	Homo sapiens (human)
male somatic sex determination	Androgen receptor	Homo sapiens (human)
intracellular estrogen receptor signaling pathway	Androgen receptor	Homo sapiens (human)
androgen receptor signaling pathway	Androgen receptor	Homo sapiens (human)
intracellular receptor signaling pathway	Androgen receptor	Homo sapiens (human)
positive regulation of intracellular estrogen receptor signaling pathway	Androgen receptor	Homo sapiens (human)
Leydig cell differentiation	Androgen receptor	Homo sapiens (human)
multicellular organism growth	Androgen receptor	Homo sapiens (human)
positive regulation of phosphorylation	Androgen receptor	Homo sapiens (human)
positive regulation of MAPK cascade	Androgen receptor	Homo sapiens (human)
positive regulation of insulin-like growth factor receptor signaling pathway	Androgen receptor	Homo sapiens (human)
positive regulation of cell differentiation	Androgen receptor	Homo sapiens (human)
negative regulation of integrin biosynthetic process	Androgen receptor	Homo sapiens (human)
positive regulation of integrin biosynthetic process	Androgen receptor	Homo sapiens (human)
positive regulation of DNA-templated transcription	Androgen receptor	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Androgen receptor	Homo sapiens (human)
positive regulation of transcription by RNA polymerase III	Androgen receptor	Homo sapiens (human)
insulin-like growth factor receptor signaling pathway	Androgen receptor	Homo sapiens (human)
regulation of developmental growth	Androgen receptor	Homo sapiens (human)
animal organ formation	Androgen receptor	Homo sapiens (human)
male genitalia morphogenesis	Androgen receptor	Homo sapiens (human)
epithelial cell proliferation	Androgen receptor	Homo sapiens (human)
negative regulation of epithelial cell proliferation	Androgen receptor	Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activity	Androgen receptor	Homo sapiens (human)
activation of prostate induction by androgen receptor signaling pathway	Androgen receptor	Homo sapiens (human)
morphogenesis of an epithelial fold	Androgen receptor	Homo sapiens (human)
lateral sprouting involved in mammary gland duct morphogenesis	Androgen receptor	Homo sapiens (human)
prostate gland growth	Androgen receptor	Homo sapiens (human)
prostate gland epithelium morphogenesis	Androgen receptor	Homo sapiens (human)
epithelial cell differentiation involved in prostate gland development	Androgen receptor	Homo sapiens (human)
tertiary branching involved in mammary gland duct morphogenesis	Androgen receptor	Homo sapiens (human)
mammary gland alveolus development	Androgen receptor	Homo sapiens (human)
positive regulation of epithelial cell proliferation involved in prostate gland development	Androgen receptor	Homo sapiens (human)
cellular response to steroid hormone stimulus	Androgen receptor	Homo sapiens (human)
cellular response to estrogen stimulus	Androgen receptor	Homo sapiens (human)
cellular response to testosterone stimulus	Androgen receptor	Homo sapiens (human)
seminiferous tubule development	Androgen receptor	Homo sapiens (human)
non-membrane-bounded organelle assembly	Androgen receptor	Homo sapiens (human)
positive regulation of miRNA transcription	Androgen receptor	Homo sapiens (human)
regulation of protein localization to plasma membrane	Androgen receptor	Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway	Androgen receptor	Homo sapiens (human)
male gonad development	Androgen receptor	Homo sapiens (human)
intracellular steroid hormone receptor signaling pathway	Androgen receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (36)

Process	via Protein(s)	Taxonomy
RNA polymerase II transcription regulatory region sequence-specific DNA binding	Glucocorticoid receptor	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Glucocorticoid receptor	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Glucocorticoid receptor	Homo sapiens (human)
core promoter sequence-specific DNA binding	Glucocorticoid receptor	Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specific	Glucocorticoid receptor	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	Glucocorticoid receptor	Homo sapiens (human)
DNA-binding transcription factor activity	Glucocorticoid receptor	Homo sapiens (human)
RNA binding	Glucocorticoid receptor	Homo sapiens (human)
nuclear receptor activity	Glucocorticoid receptor	Homo sapiens (human)
nuclear glucocorticoid receptor activity	Glucocorticoid receptor	Homo sapiens (human)
steroid binding	Glucocorticoid receptor	Homo sapiens (human)
protein binding	Glucocorticoid receptor	Homo sapiens (human)
zinc ion binding	Glucocorticoid receptor	Homo sapiens (human)
TBP-class protein binding	Glucocorticoid receptor	Homo sapiens (human)
protein kinase binding	Glucocorticoid receptor	Homo sapiens (human)
identical protein binding	Glucocorticoid receptor	Homo sapiens (human)
Hsp90 protein binding	Glucocorticoid receptor	Homo sapiens (human)
steroid hormone binding	Glucocorticoid receptor	Homo sapiens (human)
sequence-specific double-stranded DNA binding	Glucocorticoid receptor	Homo sapiens (human)
estrogen response element binding	Glucocorticoid receptor	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Progesterone receptor	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Progesterone receptor	Homo sapiens (human)
transcription coactivator binding	Progesterone receptor	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	Progesterone receptor	Homo sapiens (human)
DNA binding	Progesterone receptor	Homo sapiens (human)
nuclear steroid receptor activity	Progesterone receptor	Homo sapiens (human)
G protein-coupled receptor activity	Progesterone receptor	Homo sapiens (human)
steroid binding	Progesterone receptor	Homo sapiens (human)
protein binding	Progesterone receptor	Homo sapiens (human)
zinc ion binding	Progesterone receptor	Homo sapiens (human)
enzyme binding	Progesterone receptor	Homo sapiens (human)
identical protein binding	Progesterone receptor	Homo sapiens (human)
ATPase binding	Progesterone receptor	Homo sapiens (human)
estrogen response element binding	Progesterone receptor	Homo sapiens (human)
nuclear receptor activity	Progesterone receptor	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Mineralocorticoid receptor	Homo sapiens (human)
DNA-binding transcription factor activity	Mineralocorticoid receptor	Homo sapiens (human)
nuclear steroid receptor activity	Mineralocorticoid receptor	Homo sapiens (human)
steroid binding	Mineralocorticoid receptor	Homo sapiens (human)
protein binding	Mineralocorticoid receptor	Homo sapiens (human)
zinc ion binding	Mineralocorticoid receptor	Homo sapiens (human)
TBP-class protein binding	Mineralocorticoid receptor	Homo sapiens (human)
sequence-specific double-stranded DNA binding	Mineralocorticoid receptor	Homo sapiens (human)
nuclear receptor activity	Mineralocorticoid receptor	Homo sapiens (human)
estrogen response element binding	Mineralocorticoid receptor	Homo sapiens (human)
transcription cis-regulatory region binding	Androgen receptor	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Androgen receptor	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Androgen receptor	Homo sapiens (human)
RNA polymerase II general transcription initiation factor binding	Androgen receptor	Homo sapiens (human)
transcription coactivator binding	Androgen receptor	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	Androgen receptor	Homo sapiens (human)
chromatin binding	Androgen receptor	Homo sapiens (human)
DNA-binding transcription factor activity	Androgen receptor	Homo sapiens (human)
nuclear receptor activity	Androgen receptor	Homo sapiens (human)
G protein-coupled receptor activity	Androgen receptor	Homo sapiens (human)
signaling receptor binding	Androgen receptor	Homo sapiens (human)
steroid binding	Androgen receptor	Homo sapiens (human)
androgen binding	Androgen receptor	Homo sapiens (human)
protein binding	Androgen receptor	Homo sapiens (human)
beta-catenin binding	Androgen receptor	Homo sapiens (human)
zinc ion binding	Androgen receptor	Homo sapiens (human)
enzyme binding	Androgen receptor	Homo sapiens (human)
ATPase binding	Androgen receptor	Homo sapiens (human)
molecular adaptor activity	Androgen receptor	Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor binding	Androgen receptor	Homo sapiens (human)
POU domain binding	Androgen receptor	Homo sapiens (human)
molecular condensate scaffold activity	Androgen receptor	Homo sapiens (human)
estrogen response element binding	Androgen receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (16)

Process	via Protein(s)	Taxonomy
nucleus	Glucocorticoid receptor	Homo sapiens (human)
nucleus	Glucocorticoid receptor	Homo sapiens (human)
nucleoplasm	Glucocorticoid receptor	Homo sapiens (human)
cytoplasm	Glucocorticoid receptor	Homo sapiens (human)
mitochondrial matrix	Glucocorticoid receptor	Homo sapiens (human)
centrosome	Glucocorticoid receptor	Homo sapiens (human)
spindle	Glucocorticoid receptor	Homo sapiens (human)
cytosol	Glucocorticoid receptor	Homo sapiens (human)
membrane	Glucocorticoid receptor	Homo sapiens (human)
nuclear speck	Glucocorticoid receptor	Homo sapiens (human)
synapse	Glucocorticoid receptor	Homo sapiens (human)
chromatin	Glucocorticoid receptor	Homo sapiens (human)
protein-containing complex	Glucocorticoid receptor	Homo sapiens (human)
plasma membrane	Progesterone receptor	Homo sapiens (human)
nucleoplasm	Progesterone receptor	Homo sapiens (human)
mitochondrial outer membrane	Progesterone receptor	Homo sapiens (human)
cytosol	Progesterone receptor	Homo sapiens (human)
chromatin	Progesterone receptor	Homo sapiens (human)
nucleus	Progesterone receptor	Homo sapiens (human)
nucleoplasm	Mineralocorticoid receptor	Homo sapiens (human)
endoplasmic reticulum membrane	Mineralocorticoid receptor	Homo sapiens (human)
cytosol	Mineralocorticoid receptor	Homo sapiens (human)
chromatin	Mineralocorticoid receptor	Homo sapiens (human)
receptor complex	Mineralocorticoid receptor	Homo sapiens (human)
nucleus	Mineralocorticoid receptor	Homo sapiens (human)
plasma membrane	Androgen receptor	Homo sapiens (human)
nucleus	Androgen receptor	Homo sapiens (human)
nucleoplasm	Androgen receptor	Homo sapiens (human)
cytoplasm	Androgen receptor	Homo sapiens (human)
cytosol	Androgen receptor	Homo sapiens (human)
nuclear speck	Androgen receptor	Homo sapiens (human)
chromatin	Androgen receptor	Homo sapiens (human)
protein-containing complex	Androgen receptor	Homo sapiens (human)
nucleus	Androgen receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (25)

Assay ID	Title	Year	Journal	Article
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID274993	Inhibition of IL1-stimulated IL6 production in HFF cells	2006	Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26	Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.
AID274997	Activation of MMTV in HeLa cells measured by luciferase activity	2006	Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26	Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.
AID516379	Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human HeLa cells assessed as inhibition of TPA-induced collagenase promoter activity by luciferase reporter gene assay relative to Dexamethasone	2010	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19	Discovery of quinolines as selective glucocorticoid receptor agonists.
AID516374	Binding affinity to human recombinant androgen receptor expressed in baculovirus infected Sf9 cells	2010	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19	Discovery of quinolines as selective glucocorticoid receptor agonists.
AID516377	Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human HeLa cells assessed as inhibition of TPA-induced collagenase promoter activity by luciferase reporter gene assay	2010	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19	Discovery of quinolines as selective glucocorticoid receptor agonists.
AID274992	Inhibition of tetramethylrhodamine labeled dexamethasone binding to MR by FP assay	2006	Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26	Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.
AID516376	Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL-8 production relative to Dexamethasone	2010	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19	Discovery of quinolines as selective glucocorticoid receptor agonists.
AID274998	Activation of MMTV in HeLa cells measured by luciferase activity relative to Dexamethasone	2006	Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26	Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.
AID516375	Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL-8 production	2010	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19	Discovery of quinolines as selective glucocorticoid receptor agonists.
AID516372	Binding affinity to human recombinant progesterone receptor expressed in baculovirus infected Sf9 cells	2010	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19	Discovery of quinolines as selective glucocorticoid receptor agonists.
AID274991	Inhibition of tetramethylrhodamine labeled RU486 binding to PR by FP assay	2006	Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26	Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.
AID274994	Inhibition of IL1-stimulated IL6 production in HFF cells relative to Dexamethasone	2006	Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26	Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.
AID516380	Transactivation activity at glucocorticoid receptor in human HeLa cells assessed as induction of MMTV promoter activity by luciferase reporter gene assay relative to Dexamethasone	2010	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19	Discovery of quinolines as selective glucocorticoid receptor agonists.
AID274996	Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay relative to Dexamethasone	2006	Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26	Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.
AID516378	Transactivation activity at glucocorticoid receptor in human HeLa cells assessed as induction of MMTV promoter activity by luciferase reporter gene assay	2010	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19	Discovery of quinolines as selective glucocorticoid receptor agonists.
AID516371	Binding affinity to human recombinant glucocorticoid receptor expressed in baculovirus infected Sf9 cells	2010	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19	Discovery of quinolines as selective glucocorticoid receptor agonists.
AID274995	Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay	2006	Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26	Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.
AID274990	Inhibition of tetramethylrhodamine labeled dexamethasone binding to GR by FP assay	2006	Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26	Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.
AID516373	Binding affinity to human recombinant mineralocorticoid receptor expressed in baculovirus infected Sf9 cells	2010	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19	Discovery of quinolines as selective glucocorticoid receptor agonists.
AID1346849	Human Glucocorticoid receptor (3C. 3-Ketosteroid receptors)	2004	Proceedings of the National Academy of Sciences of the United States of America, Jan-06, Volume: 101, Issue:1	Dissociation of transactivation from transrepression by a selective glucocorticoid receptor agonist leads to separation of therapeutic effects from side effects.
[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 (18.18)	29.6817
2010's	7 (63.64)	24.3611
2020's	2 (18.18)	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	1 (9.09%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	10 (90.91%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
prednisolone Prednisolone: A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.. prednisolone : A glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone.	2.43	2	11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone	adrenergic agent; anti-inflammatory drug; antineoplastic agent; drug metabolite; environmental contaminant; immunosuppressive agent; xenobiotic
n-pentanol n-pentanol: RN given refers to parent cpd. pentan-1-ol : A short-chain primary fatty alcohol that is pentane in which a hydrogen of one of the methyl groups is substituted by a hydroxy group. It has been isolated from Melicope ptelefolia.	2.07	1	pentanol; short-chain primary fatty alcohol	human metabolite; plant metabolite
betamethasone Betamethasone: A glucocorticoid given orally, parenterally, by local injection, by inhalation, or applied topically in the management of various disorders in which corticosteroids are indicated. Its lack of mineralocorticoid properties makes betamethasone particularly suitable for treating cerebral edema and congenital adrenal hyperplasia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p724)	2.06	1	11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; fluorinated steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone	anti-asthmatic agent; anti-inflammatory drug; immunosuppressive agent
trinitrobenzenesulfonic acid Trinitrobenzenesulfonic Acid: A reagent that is used to neutralize peptide terminal amino groups.. 2,4,6-trinitrobenzenesulfonic acid : The arenesulfonic acid that is benzenesulfonic acid with three nitro substituents in the 2-, 4- and 6-positions.	2.07	1	arenesulfonic acid; C-nitro compound	epitope; explosive; reagent
betamethasone sodium phosphate betamethasone sodium phosphate: phosphate ester of betamethasone; RN given refers to the di-Na salt (11beta,16beta)-isomer; structure in Negwer,5th ed, 4975. betamethasone sodium phosphate : An organic sodium salt that is the disodium salt of betamethasone phosphate.	2.06	1	organic sodium salt; tertiary alpha-hydroxy ketone
benzofurans Benzofurans: Compounds that contain a BENZENE ring fused to a furan ring.	4.41	6
desoximetasone Desoximetasone: A topical anti-inflammatory glucocorticoid used in DERMATOSES, skin allergies, PSORIASIS, etc.. desoximetasone : Dexamethasone in which the hydroxy group at the 17alpha position is substituted by hydrogen. A synthetic corticosteroid with glucocorticoid activity, it is used as an anti-inflammatory and anti-pruritic in the treatment of various skin disorders, including skin allergies and psoriasis.	3.17	1	11beta-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; fluorinated steroid; glucocorticoid; primary alpha-hydroxy ketone	anti-inflammatory drug; antipruritic drug
ru24858 RU24858: a glucocorticoid; structure in first source	3.17	1
interleukin-8 Interleukin-8: A member of the CXC chemokine family that plays a role in the regulation of the acute inflammatory response. It is secreted by variety of cell types and induces CHEMOTAXIS of NEUTROPHILS and other inflammatory cells.	2.02	1
epidermal growth factor Epidermal Growth Factor: A 6-kDa polypeptide growth factor initially discovered in mouse submaxillary glands. Human epidermal growth factor was originally isolated from urine based on its ability to inhibit gastric secretion and called urogastrone. Epidermal growth factor exerts a wide variety of biological effects including the promotion of proliferation and differentiation of mesenchymal and EPITHELIAL CELLS. It is synthesized as a transmembrane protein which can be cleaved to release a soluble active form.	2.07	1
transforming growth factor beta Transforming Growth Factor beta: A factor synthesized in a wide variety of tissues. It acts synergistically with TGF-alpha in inducing phenotypic transformation and can also act as a negative autocrine growth factor. TGF-beta has a potential role in embryonal development, cellular differentiation, hormone secretion, and immune function. TGF-beta is found mostly as homodimer forms of separate gene products TGF-beta1, TGF-beta2 or TGF-beta3. Heterodimers composed of TGF-beta1 and 2 (TGF-beta1.2) or of TGF-beta2 and 3 (TGF-beta2.3) have been isolated. The TGF-beta proteins are synthesized as precursor proteins.	2.07	1

Condition	Relationship Strength	Studies
Congenital Zika Syndrome [description not available]	2.25	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.52	2
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	2.25	1
Pink Eye [description not available]	2.06	1
Allergic Conjunctivitis [description not available]	2.06	1
Conjunctivitis INFLAMMATION of the CONJUNCTIVA.	2.06	1
Conjunctivitis, Allergic Conjunctivitis due to hypersensitivity to various allergens.	2.06	1
Intraocular Pressure The pressure of the fluids in the eye.	2.06	1
Idiopathic Inflammatory Myopathies [description not available]	2.99	1
Myositis Inflammation of a muscle or muscle tissue.	2.99	1
Bowel Diseases, Inflammatory [description not available]	2.07	1
Acute Disease Disease having a short and relatively severe course.	2.07	1
Colitis Inflammation of the COLON section of the large intestine (INTESTINE, LARGE), usually with symptoms such as DIARRHEA (often with blood and mucus), ABDOMINAL PAIN, and FEVER.	2.07	1
Inflammatory Bowel Diseases Chronic, non-specific inflammation of the GASTROINTESTINAL TRACT. Etiology may be genetic or environmental. This term includes CROHN DISEASE and ULCERATIVE COLITIS.	2.07	1
Innate Inflammatory Response [description not available]	2.07	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.	2.07	1

zk 216348

Description

Cross-References

Synonyms (29)

Research Excerpts

Toxicity

Bioavailability

Protein Targets (6)

Potency Measurements

Inhibition Measurements

Activation Measurements

Biological Processes (91)

Molecular Functions (36)

Ceullar Components (16)

Bioassays (25)

Research

Studies (11)

Market Indicators

Research Demand Index: 12.38

Study Types

zk 216348

Description

Cross-References

Synonyms (29)

Research Excerpts

Toxicity

Bioavailability

Protein Targets (6)

Potency Measurements

Inhibition Measurements

Activation Measurements

Biological Processes (91)

Molecular Functions (36)

Ceullar Components (16)

Bioassays (25)

Research

Studies (11)

Market Indicators

Research Demand Index: 12.38

Study Types

Related Drugs (11)

Related Conditions (16)