mk 2866 profile

ID Source	ID
PubMed CID	11326715
CHEMBL ID	1738889
SCHEMBL ID	109069
MeSH ID	M0543613

Synonym
HY-13273
AKOS005266718
mk-2866
enobosarm
gtx-024
CHEMBL1738889
RLJ ,
(2s)-3-(4-cyanophenoxy)-n-[4-cyano-3-(trifluoromethyl)phenyl]-2-hydroxy-2-methylpropanamide
ostarine ,
EX-8408
1202044-20-9
mk 2866
mk2866
D10221
enobosarm (usan)
sarm s-22
propanamide, 3-(4-cyanophenoxy)-n-(4-cyano-3-(trifluoromethyl)phenyl)-2-hydroxy-2-methyl-, (2s)-
enobosarm [usan:inn]
o3571h3r8n ,
(2s)-3-(4-cyanophenoxy)-n-(4-cyano-3-(trifluoromethyl)phenyl)-2-hydroxy-2-methylpropanamide
unii-o3571h3r8n
gtx 024
841205-47-8
NCGC00346499-01
CS-0562
S1174
enobosarm [who-dd]
enobosarm [inn]
enobosarm [usan]
MLS006010739
smr004701698
SCHEMBL109069
DTXSID30233006
ostarine(mk-2866)
(s)-n-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide
mk-2866 (gtx-024)
AC-30221
ostarine(mk2286); 1202044-20-9
EX-A638
propanamide, 3-?(4-?cyanophenoxy)?-?n-?[4-?cyano-?3-?(trifluoromethyl)?phenyl]?-?2-?hydroxy-?2-?methyl-?, (2s)?-
HMS3654E16
SW219159-1
ostarine(mk-2286)
not for sale-patented
DB12078
Q5379258
((2s)-3-(4-cyanophenoxy)-n-[4-cyano-3-(trifluoromethyl)phenyl]-2-hydroxy-2-methylpropanamide)
ostarine (mk2866)
BCP02391
SB16683
ostarine-d4
BCP28483
mk-2866(d4);mk2866(d4);gtx-024(d4);gtx024;(s)-n-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide-d4
AMY38131
CCG-268514
H12015
mk-2866; gtx024;((2s)-3-(4-cyanophenoxy)-n-[4-cyano-3-(trifluoromethyl)phenyl]-2-hydroxy-2-methylpropanamide)
A864177
bdbm50529668
jngvjmblxiuvrd-sfhvurjksa-n

Excerpt	Reference
" Preclinical studies of GTx-024 supported the evaluation of several potential drug-drug interactions in a clinical setting."	( Pharmacokinetic drug interactions of the selective androgen receptor modulator GTx-024(Enobosarm) with itraconazole, rifampin, probenecid, celecoxib and rosuvastatin. Coss, CC; Dalton, JT; Jones, A, 2016)

Excerpt	Reference
"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)

Excerpt	Reference
" In a standard castrated male rat model, several compounds showed good anabolic activity on levator ani muscle, dissociated from the androgenic activity on ventral prostate, after oral dosing at 30 mg/kg."	( Discovery of diarylhydantoins as new selective androgen receptor modulators. Annoot, D; Clément-Lacroix, P; Deprez, P; Duval, E; Fleury, D; Guédin, D; Hebbe, S; Lefrançois, JM; Lemoullec, JM; Michoux, L; Minet, D; Mollat, P; Nique, F; Peixoto, C; Prangé, T; Robin-Jagerschmidt, C; Thauvin, M; Triballeau, N, 2012)

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
EWS/FLI fusion protein	Homo sapiens (human)	Potency	33.1734	0.0013	10.1577	42.8575	AID1259253
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Androgen receptor	Homo sapiens (human)	IC50 (µMol)	0.0038	0.0000	0.8753	10.0000	AID1612503
Androgen receptor	Homo sapiens (human)	Ki	0.0022	0.0002	0.4240	7.2000	AID1612502; AID1885044
Androgen receptor	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0364	0.0010	1.9794	14.1600	AID1635241
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Androgen receptor	Homo sapiens (human)	Activity	0.0015	0.0015	0.0096	0.0370	AID706411
Neuropeptide FF receptor 2	Rattus norvegicus (Norway rat)	Activity	0.0015	0.0015	0.0120	0.0370	AID706411
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
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]

Process	via Protein(s)	Taxonomy
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]

Process	via Protein(s)	Taxonomy
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 (63)

Assay ID	Title	Year	Journal	Article
AID1347154	Primary screen GU AMC 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.
AID1347103	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347106	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
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.
AID1347091	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347108	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630	Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347105	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347094	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
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.
AID1347096	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1635254	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability at 100 uM after 72 hrs by MTT assay relative to control	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1635258	Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation at 100 nM preincubated for 30 mins followed by R1881 addition measure	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1635247	Apparent permeability from basolateral to apical side in human Caco2 cells at 10 uM incubated for 120 mins by LC-MS/MS analysis	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1612512	Intrinsic clearance in mouse liver microsomes at 50 uM in presence of cofactors for phase 1 and 2 metabolism	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	New Generation of Selective Androgen Receptor Degraders: Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity.
AID1635255	Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation at 3160 nM preincubated for 30 mins followed by R1881 addition measur	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1635239	Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation at 10 uM preincubated for 30 mins followed by R1881 addition measured	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1635249	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1612534	Induction of androgen receptor splice variant mutant in human 22RV1 cells at 10 uM after 24 hrs in presence of R1881 by Western blot analysis relative to control	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	New Generation of Selective Androgen Receptor Degraders: Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity.
AID1635222	Antiproliferative activity against human LNCAP cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1612503	Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of R1881-induced receptor transactivation after 24 hrs by luciferase reporter gene assay	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	New Generation of Selective Androgen Receptor Degraders: Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity.
AID1635261	Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation at 3.16 nM preincubated for 30 mins followed by R1881 addition measur	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1635262	Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation at 1 nM preincubated for 30 mins followed by R1881 addition measured	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1612511	Half life in mouse liver microsomes at 50 uM in presence of cofactors for phase 1 and 2 metabolism	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	New Generation of Selective Androgen Receptor Degraders: Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity.
AID1635259	Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation at 31.6 nM preincubated for 30 mins followed by R1881 addition measur	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1612533	Induction of full length androgen receptor in human LNCaP cells at 1 uM after 24 hrs in presence of R1881 by Western blot analysis relative to control	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	New Generation of Selective Androgen Receptor Degraders: Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity.
AID1635244	Metabolic stability in human liver microsomes at 3 uM preincubated with compound followed by NADPH addition measured after 5 to 45 mins by LC-MS/MS analysis	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1635248	Efflux ratio of apparent permeability from basolateral to apical side over apical to basolateral side in human Caco2 cells at 10 uM incubated for 120 mins by LC-MS/MS analysis	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID706411	Transactivation of human androgen receptor transfected in human HeLa cells by luciferase reporter gene assay	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Discovery of diarylhydantoins as new selective androgen receptor modulators.
AID706190	Ratio of binding affinity to human androgen receptor in inactive state to human androgen receptor in active state	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Discovery of diarylhydantoins as new selective androgen receptor modulators.
AID1635260	Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation at 10 nM preincubated for 30 mins followed by R1881 addition measured	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1635263	Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation at 0.316 nM preincubated for 30 mins followed by R1881 addition measu	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1635223	Antiproliferative activity against human VCaP cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1885044	Displacement of [3H]mibolerone from Androgen receptor (unknown origin) measured by liquid scintillation counting method	2022	Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13	Therapeutic Strategies to Target the Androgen Receptor.
AID1612502	Displacement of [3H]-mibolerone from recombinant wild-type GST-tagged androgen receptor LBD (unknown origin) after 16 hrs by scintillation counting analysis	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	New Generation of Selective Androgen Receptor Degraders: Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity.
AID1635257	Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation at 316 nM preincubated for 30 mins followed by R1881 addition measure	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1635220	Antiproliferative activity against human 22Rv1 cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1635256	Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation at 1000 nM preincubated for 30 mins followed by R1881 addition measur	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID601821	Agonist activity at wild type androgen receptor expressed in african green monkey CV1 cells assessed as induction of transcriptional activity at 1 to 1000 nM by luciferase reporter gene assay	2011	Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11	Unexpected binding orientation of bulky-B-ring anti-androgens and implications for future drug targets.
AID601820	Displacement of [3H]MIB from GST-tagged wild type recombinant androgen receptor ligand binding domain after 18 hrs by scintillation counting relative to dihydrotestosterone	2011	Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11	Unexpected binding orientation of bulky-B-ring anti-androgens and implications for future drug targets.
AID1635246	Apparent permeability from apical to basolateral side in human Caco2 cells at 10 uM incubated for 120 mins by LC-MS/MS analysis	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1635241	Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation preincubated for 30 mins followed by R1881 addition measured after 16	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1635242	Agonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as receptor activation at 10 uM incubated for 16 to 24 hrs by betalactamase reporter gene assay relative to control	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1635221	Antiproliferative activity against human DU145 cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1347411	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	1 (1.79)	29.6817
2010's	34 (60.71)	24.3611
2020's	21 (37.50)	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	3 (5.36%)	5.53%
Reviews	8 (14.29%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	45 (80.36%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
atenolol Atenolol: A cardioselective beta-1 adrenergic blocker possessing properties and potency similar to PROPRANOLOL, but without a negative inotropic effect.. atenolol : An ethanolamine compound having a (4-carbamoylmethylphenoxy)methyl group at the 1-position and an N-isopropyl substituent.	2.13	1	0	ethanolamines; monocarboxylic acid amide; propanolamine	anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; environmental contaminant; sympatholytic agent; xenobiotic
bicalutamide bicalutamide: approved for treatment of advanced prostate cancer. N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide : A member of the class of (trifluoromethyl)benzenes that is 4-amino-2-(trifluoromethyl)benzonitrile in which one of the amino hydrogens is substituted by a 3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanoyl group.. bicalutamide : A racemate comprising of equal amounts of (R)-bicalutamide and (S)-bicalutamide. It is an oral non-steroidal antiandrogen used in the treatment of prostate cancer and hirsutism.	4.33	5	0	(trifluoromethyl)benzenes; monocarboxylic acid amide; monofluorobenzenes; nitrile; sulfone; tertiary alcohol
buspirone Buspirone: An anxiolytic agent and serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the BENZODIAZAPINES, but it has an efficacy comparable to DIAZEPAM.. buspirone : An azaspiro compound that is 8-azaspiro[4.5]decane-7,9-dione substituted at the nitrogen atom by a 4-(piperazin-1-yl)butyl group which in turn is substituted by a pyrimidin-2-yl group at the N(4) position.	2.21	1	0	azaspiro compound; N-alkylpiperazine; N-arylpiperazine; organic heteropolycyclic compound; piperidones; pyrimidines	anxiolytic drug; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; sedative; serotonergic agonist
verapamil Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent.. verapamil : A racemate comprising equimolar amounts of dexverapamil and (S)-verapamil. An L-type calcium channel blocker of the phenylalkylamine class, it is used (particularly as the hydrochloride salt) in the treatment of hypertension, angina pectoris and cardiac arrhythmia, and as a preventive medication for migraine.. 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile : A tertiary amino compound that is 3,4-dimethoxyphenylethylamine in which the hydrogens attached to the nitrogen are replaced by a methyl group and a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group.	2.57	2	0	aromatic ether; nitrile; polyether; tertiary amino compound
carbonyl cyanide m-chlorophenyl hydrazone Carbonyl Cyanide m-Chlorophenyl Hydrazone: A proton ionophore. It is commonly used as an uncoupling agent and inhibitor of photosynthesis because of its effects on mitochondrial and chloroplast membranes.. CCCP : A member of the class of monochlorobenzenes that is benzene substituted by 2-(1,3-dinitrilopropan-2-ylidene)hydrazinyl and chloro groups at positions 1 and 3, respectively. It is a mitochondrial depolarizing agent that induces reactive oxygen species mediated cell death.	2.13	1	0	hydrazone; monochlorobenzenes; nitrile	antibacterial agent; geroprotector; ionophore
celecoxib [no description available]	3.51	1	1	organofluorine compound; pyrazoles; sulfonamide; toluenes	cyclooxygenase 2 inhibitor; geroprotector; non-narcotic analgesic; non-steroidal anti-inflammatory drug
chlorpromazine Chlorpromazine: The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking DOPAMINE RECEPTORS. Chlorpromazine has several other actions and therapeutic uses, including as an antiemetic and in the treatment of intractable hiccup.. chlorpromazine : A substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropanamine moiety.	2.13	1	0	organochlorine compound; phenothiazines; tertiary amine	anticoronaviral agent; antiemetic; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; phenothiazine antipsychotic drug
nilutamide [no description available]	2.07	1	0	(trifluoromethyl)benzenes; C-nitro compound; imidazolidinone	androgen antagonist; antineoplastic agent
probenecid Probenecid: The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.. probenecid : A sulfonamide in which the nitrogen of 4-sulfamoylbenzoic acid is substituted with two propyl groups.	3.51	1	1	benzoic acids; sulfonamide	uricosuric drug
propranolol Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.. propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3.	2.13	1	0	naphthalenes; propanolamine; secondary amine	anti-arrhythmia drug; antihypertensive agent; anxiolytic drug; beta-adrenergic antagonist; environmental contaminant; human blood serum metabolite; vasodilator agent; xenobiotic
oxandrolone Oxandrolone: A synthetic hormone with anabolic and androgenic properties.	3.51	1	0	17beta-hydroxy steroid; 3-oxo steroid; anabolic androgenic steroid; oxa-steroid	anabolic agent; androgen
testosterone propionate Testosterone Propionate: An ester of TESTOSTERONE with a propionate substitution at the 17-beta position.. androgen : A sex hormone that stimulates or controls the development and maintenance of masculine characteristics in vertebrates by binding to androgen receptors.	2.07	1	0	steroid ester
carbostyril Quinolones: A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.. quinolin-2(1H)-one : A quinolone that is 1,2-dihydroquinoline substituted by an oxo group at position 2.	3.57	2	0	monohydroxyquinoline; quinolone	bacterial xenobiotic metabolite
cycloheximide Cycloheximide: Antibiotic substance isolated from streptomycin-producing strains of Streptomyces griseus. It acts by inhibiting elongation during protein synthesis.. cycloheximide : A dicarboximide that is 4-(2-hydroxyethyl)piperidine-2,6-dione in which one of the hydrogens attached to the carbon bearing the hydroxy group is replaced by a 3,5-dimethyl-2-oxocyclohexyl group. It is an antibiotic produced by the bacterium Streptomyces griseus.	2.21	1	0	antibiotic fungicide; cyclic ketone; dicarboximide; piperidine antibiotic; piperidones; secondary alcohol	anticoronaviral agent; bacterial metabolite; ferroptosis inhibitor; neuroprotective agent; protein synthesis inhibitor
medroxyprogesterone acetate [no description available]	3.51	1	0	20-oxo steroid; 3-oxo-Delta(4) steroid; acetate ester; corticosteroid; steroid ester	adjuvant; androgen; antineoplastic agent; antioxidant; female contraceptive drug; inhibitor; progestin; synthetic oral contraceptive
propionamide [no description available]	3.91	3	0	monocarboxylic acid amide; primary fatty amide
pyocyanine Pyocyanine: Antibiotic pigment produced by Pseudomonas aeruginosa.. pyocyanine : An iminium betaine that is 5-methylphenazin-5-ium which is substituted at position 1 by an oxidanidyl group. An antibiotic pigment produced by Pseudomonas aeruginosa.	2.31	1	0	iminium betaine; phenazines	antibacterial agent; bacterial metabolite; biological pigment; virulence factor
pyrroles 1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.	3.15	1	0	pyrrole; secondary amine
thiazoles [no description available]	2.53	2	0	1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
hydrazine diamine : Any polyamine that contains two amino groups.	4.2	2	0	azane; hydrazines	EC 4.3.1.10 (serine-sulfate ammonia-lyase) inhibitor
aminoimidazole carboxamide Aminoimidazole Carboxamide: An imidazole derivative which is a metabolite of the antineoplastic agents BIC and DIC. By itself, or as the ribonucleotide, it is used as a condensation agent in the preparation of nucleosides and nucleotides. Compounded with orotic acid, it is used to treat liver diseases.. 5-aminoimidazole-4-carboxamide : An aminoimidazole in which the amino group is at C-5 with a carboxamido group at C-4.	2.06	1	0	aminoimidazole; monocarboxylic acid amide	mouse metabolite
dihydrotestosterone Dihydrotestosterone: A potent androgenic metabolite of TESTOSTERONE. It is produced by the action of the enzyme 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE.. 17beta-hydroxyandrostan-3-one : A 17beta-hydroxy steroid that is testosterone in which the 4-5 double bond has been reduced to a single bond with unspecified configuration at position 5.. 17beta-hydroxy-5alpha-androstan-3-one : A 17beta-hydroxy steroid that is testosterone in which the 4,5 double bond has been reduced to a single bond with alpha-configuration at position 5.	4.32	5	0	17beta-hydroxy steroid; 17beta-hydroxyandrostan-3-one; 3-oxo-5alpha-steroid	androgen; Daphnia magna metabolite; human metabolite; mouse metabolite
methamphetamine Methamphetamine: A central nervous system stimulant and sympathomimetic with actions and uses similar to DEXTROAMPHETAMINE. The smokable form is a drug of abuse and is referred to as crank, crystal, crystal meth, ice, and speed.. methamphetamine : A member of the class of amphetamines in which the amino group of (S)-amphetamine carries a methyl substituent.	2.08	1	0	amphetamines; secondary amine	central nervous system stimulant; environmental contaminant; neurotoxin; psychotropic drug; xenobiotic
titanium Titanium: A dark-gray, metallic element of widespread distribution but occurring in small amounts with atomic number, 22, atomic weight, 47.867 and symbol, Ti; specific gravity, 4.5; used for fixation of fractures.	2.21	1	0	titanium group element atom
stanozolol Stanozolol: A synthetic steroid that has anabolic and androgenic properties. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1194). stanozolol : An organic heteropentacyclic compound resulting from the formal condensation of the 3-keto-aldehyde moiety of oxymetholone with hydrazine. Like oxymetholone, it is a synthetic anabolic steroid. It has both anabolic and androgenic properties, and has been used to treat hereditary angioedema and various vascular disorders. It has also been widely abused by professional athletes.	2.31	1	0	17beta-hydroxy steroid; anabolic androgenic steroid; organic heteropentacyclic compound; tertiary alcohol	anabolic agent; androgen
titanium dioxide titanium dioxide: used medically as protectant against externally caused irritation & sunlight; high concentrations of dust may cause irritation to respiratory tract; RN given refers to titanium oxide (TiO2); structure. titanium dioxide : A titanium oxide with the formula TiO2. A naturally occurring oxide sourced from ilmenite, rutile and anatase, it has a wide range of applications.	2.21	1	0	titanium oxides	food colouring
danazol Danazol: A synthetic steroid with antigonadotropic and anti-estrogenic activities that acts as an anterior pituitary suppressant by inhibiting the pituitary output of gonadotropins. It possesses some androgenic properties. Danazol has been used in the treatment of endometriosis and some benign breast disorders.	2.21	1	0	17beta-hydroxy steroid; terminal acetylenic compound	anti-estrogen; estrogen antagonist; geroprotector
itraconazole Itraconazole: A triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis.. itraconazole : An N-arylpiperazine that is cis-ketoconazole in which the imidazol-1-yl group is replaced by a 1,2,4-triazol-1-yl group and in which the actyl group attached to the piperazine moiety is replaced by a p-[(+-)1-sec-butyl-5-oxo-1,5-dihydro-4H-1,2,4-triazol-4-yl]phenyl group. A potent P-glycoprotein and CYP3A4 inhibitor, it is used as an antifungal drug for the treatment of various fungal infections, including aspergillosis, blastomycosis, candidiasis, chromoblastomycosis, coccidioidomycosis, cryptococcosis, histoplasmosis, and sporotrichosis.	3.51	1	1	aromatic ether; conazole antifungal drug; cyclic ketal; dichlorobenzene; dioxolane; N-arylpiperazine; triazole antifungal drug; triazoles	EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor; Hedgehog signaling pathway inhibitor; P450 inhibitor
nitrogenase stabilizing-protective protein, bacteria [no description available]	4	3	0	N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide	androgen antagonist; antineoplastic agent
aica ribonucleotide AICA ribonucleotide: purine precursor that has antineoplastic activity. AICA ribonucleotide : A 1-(phosphoribosyl)imidazolecarboxamide that is acadesine in which the hydroxy group at the 5' position has been converted to its monophosphate derivative.	2.06	1	0	1-(phosphoribosyl)imidazolecarboxamide; aminoimidazole	cardiovascular drug; Escherichia coli metabolite; human metabolite; mouse metabolite; plant metabolite; Saccharomyces cerevisiae metabolite
talinolol [no description available]	2.13	1	0	ureas
hydroxyflutamide [no description available]	3.51	1	0
glucuronic acid Glucuronic Acid: A sugar acid formed by the oxidation of the C-6 carbon of GLUCOSE. In addition to being a key intermediate metabolite of the uronic acid pathway, glucuronic acid also plays a role in the detoxification of certain drugs and toxins by conjugating with them to form GLUCURONIDES.. D-glucuronic acid : The D-enantiomer of glucuronic acid.. D-glucopyranuronic acid : A D-glucuronic acid in cyclic pyranose form.	2.06	1	0	D-glucuronic acid	algal metabolite
metribolone Metribolone: A synthetic non-aromatizable androgen and anabolic steroid. It binds strongly to the androgen receptor and has therefore also been used as an affinity label for this receptor in the prostate and in prostatic tumors.. 17beta-hydroxy-17-methylestra-4,9,11-trien-3-one : A synthetic non-aromatisable androgen and anabolic steroid. It binds strongly to the androgen receptor and has therefore also been used as an affinity label for this receptor in the prostate and in prostatic tumors.	3.51	1	0	17beta-hydroxy steroid; 3-oxo steroid; anabolic androgenic steroid	androgen
(S)-bicalutamide (S)-bicalutamide : A N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide that is the (S)-enantiomer of bicalutamide.	3.51	1	0	N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide
enclomiphene Enclomiphene: The trans or (E)-isomer of clomiphene.	2.31	1	0
epi 001 EPI 001: an antineoplastic agent and androgen receptor antagonist; structure in first source. bisphenol A (3-chloro-2-hydroxypropyl) (2,3-dihydroxypropyl) ether : The (3-chloro-2-hydroxypropyl) (2,3-dihydroxypropyl) diether of bisphenol A; a small molecule that inhibits transactivation of the AR amino-terminal domain (NTD).	3.51	1	0	diether; organochlorine compound	androgen antagonist
pyrvinium pyrvinium: RN given refers to parent cpd; synonyms vanquin & vankin refer to pamoate[2:1]; structure in Merck Index, 9th ed, #7810. pyrvinium : A quinolinium ion that is 1-methylquinolinium substituted by dimethylamino group at position 6 and a (E)-2-(2,5-dimethyl-1-phenyl-1H-pyrrol-3-yl)ethenyl at position 2. It is a anthelminthic drug active against pinworms. The salts of pyrvinium can also be used as anticancer agents.	3.51	1	0	quinolinium ion	anthelminthic drug; antineoplastic agent
dextromethorphan Dextromethorphan: Methyl analog of DEXTRORPHAN that shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist (RECEPTORS, N-METHYL-D-ASPARTATE) and acts as a non-competitive channel blocker. It is one of the widely used ANTITUSSIVES, and is also used to study the involvement of glutamate receptors in neurotoxicity.. dextromethorphan : A 6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene in which the sterocenters at positions 4a, 10 and 10a have S-configuration. It is a prodrug of dextrorphan and used as an antitussive drug for suppressing cough.	2.13	1	0	6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene	antitussive; environmental contaminant; neurotoxin; NMDA receptor antagonist; oneirogen; prodrug; xenobiotic
phosphorus Phosphorus: A non-metal element that has the atomic symbol P, atomic number 15, and atomic weight 31. It is an essential element that takes part in a broad variety of biochemical reactions.	2.21	1	0	monoatomic phosphorus; nonmetal atom; pnictogen	macronutrient
gw 501516 GW 501516: a selective PPARdelta agonist; structure in first source. GW 501516 : An aromatic ether that is phenoxyacetic acid in which the phenyl group is substituted at position 2 by a methyl group and at position 4 by a (1,3-thiazol-5-ylmethyl)sulfanediyl group, and in which the 1,3-thiazolyl group is substituted at positions 2 and 4 by p-trifluoromethylphenyl and methyl groups, respectively.	2.53	2	0	1,3-thiazoles; aromatic ether; aryl sulfide; monocarboxylic acid; organofluorine compound	carcinogenic agent; PPARbeta/delta agonist
andarine [no description available]	5.69	9	0	acetamides; anilide
anamorelin anamorelin: a ghrelin receptor agonist for treatment of cachexia; structure in first source	4.2	2	0
lg 121071 [no description available]	3.51	1	0
bms-564929 [no description available]	3.51	1	0
lgd 2226 [no description available]	3.51	1	0
mdv 3100 [no description available]	4.22	4	0	(trifluoromethyl)benzenes; benzamides; imidazolidinone; monofluorobenzenes; nitrile; thiocarbonyl compound	androgen antagonist; antineoplastic agent
apalutamide [no description available]	3.78	2	0
pf 998425 [no description available]	3.51	1	0
lgd 3303 9-chloro-2-ethyl-1-methyl-3-(2,2,2-trifluoroethyl)-3H-pyrrolo(3,2-f)quinolin-7(6H)-one: an androgen receptor modulator; structure in first source	3.15	1	0
azd3514 AZD3514: in Phase I clinical trial in patients with castrate-resistant prostate cancer (2/2013); structure in first source	3.51	1	0
rifampin Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)	3.51	1	1	cyclic ketal; hydrazone; N-iminopiperazine; N-methylpiperazine; rifamycins; semisynthetic derivative; zwitterion	angiogenesis inhibitor; antiamoebic agent; antineoplastic agent; antitubercular agent; DNA synthesis inhibitor; EC 2.7.7.6 (RNA polymerase) inhibitor; Escherichia coli metabolite; geroprotector; leprostatic drug; neuroprotective agent; pregnane X receptor agonist; protein synthesis inhibitor
leptin Leptin: A 16-kDa peptide hormone secreted from WHITE ADIPOCYTES. Leptin serves as a feedback signal from fat cells to the CENTRAL NERVOUS SYSTEM in regulation of food intake, energy balance, and fat storage.	2.72	2	0

Condition	Indicated	Relationship Strength	Studies	Trials
Cancer of Prostate [description not available]	0	3.05	4	0
Prostatic Neoplasms Tumors or cancer of the PROSTATE.	0	3.05	4	0
Congenital Zika Syndrome [description not available]	0	2.25	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	2.66	2	0
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.	0	2.25	1	0
Androgen-Independent Prostatic Cancer [description not available]	0	3.33	1	0
Prostatic Neoplasms, Castration-Resistant Tumors or cancer of the PROSTATE which can grow in the presence of low or residual amount of androgen hormones such as TESTOSTERONE.	0	3.33	1	0
Overweight A status with BODY WEIGHT that is above certain standards. In the scale of BODY MASS INDEX, overweight is defined as having a BMI of 25.0-29.9 kg/m2. Overweight may or may not be due to increases in body fat (ADIPOSE TISSUE), hence overweight does not equal over fat.	0	2.6	1	0
Obesity A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).	0	2.6	1	0
Age-Related Osteoporosis [description not available]	0	4.43	4	0
Osteoporosis Reduction of bone mass without alteration in the composition of bone, leading to fractures. Primary osteoporosis can be of two major types: postmenopausal osteoporosis (OSTEOPOROSIS, POSTMENOPAUSAL) and age-related or senile osteoporosis.	0	4.43	4	0
ER-Negative PR-Negative HER2-Negative Breast Cancer [description not available]	0	3.7	1	1
Triple Negative Breast Neoplasms Breast neoplasms that do not express ESTROGEN RECEPTORS; PROGESTERONE RECEPTORS; and do not overexpress the NEU RECEPTOR/HER-2 PROTO-ONCOGENE PROTEIN.	0	3.7	1	1
Cachexia General ill health, malnutrition, and weight loss, usually associated with chronic disease.	1	13.95	16	4
Benign Neoplasms [description not available]	0	11.62	13	4
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	0	11.62	13	4
Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.	0	2.21	1	0
Bone Loss, Perimenopausal [description not available]	0	2.21	1	0
Osteoporosis, Postmenopausal Metabolic disorder associated with fractures of the femoral neck, vertebrae, and distal forearm. It occurs commonly in women within 15-20 years after menopause, and is caused by factors associated with menopause including estrogen deficiency.	0	2.21	1	0
Experimental Neoplasms [description not available]	0	2.21	1	0
Weight Reduction [description not available]	0	7.51	4	4
Weight Loss Decrease in existing BODY WEIGHT.	0	7.51	4	4
Bone Fractures [description not available]	0	3.01	1	0
Fractures, Bone Breaks in bones.	0	3.01	1	0
Sarcopenia Progressive decline in muscle mass due to aging which results in decreased functional capacity of muscles.	0	4.19	3	0
Osteoporotic Fractures Breaks in bones resulting from low bone mass and microarchitectural deterioration characteristic of OSTEOPOROSIS.	0	3.01	1	0
Wasting Disease [description not available]	0	3.44	2	0
Breast Cancer [description not available]	0	2.13	1	0
Breast Neoplasms Tumors or cancer of the human BREAST.	1	4.53	2	0
Urinary Incontinence, Stress Involuntary discharge of URINE as a result of physical activities that increase abdominal pressure on the URINARY BLADDER without detrusor contraction or overdistended bladder. The subtypes are classified by the degree of leakage, descent and opening of the bladder neck and URETHRA without bladder contraction, and sphincter deficiency.	0	2.15	1	0

mk 2866

Cross-References

Synonyms (60)

Compound-Compound Interactions

Bioavailability

Dosage Studied

Protein Targets (4)

Potency Measurements

Inhibition Measurements

Other Measurements

Biological Processes (56)

Molecular Functions (23)

Ceullar Components (8)

Bioassays (63)

Research

Studies (56)

Study Types

mk 2866

Cross-References

Synonyms (60)

Compound-Compound Interactions

Bioavailability

Dosage Studied

Protein Targets (4)

Potency Measurements

Inhibition Measurements

Other Measurements

Biological Processes (56)

Molecular Functions (23)

Ceullar Components (8)

Bioassays (63)

Research

Studies (56)

Study Types

Related Drugs (53)

Related Conditions (30)