azd3514 profile

AZD3514: in Phase I clinical trial in patients with castrate-resistant prostate cancer (2/2013); structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	46893585
CHEMBL ID	2346976
SCHEMBL ID	3056463
MeSH ID	M0588024

Synonym
bdbm50432188
S7040
azd-3514
azd 3514
CHEMBL2346976 ,
azd3514
cs-1443 ,
HY-16079
1240299-33-5
SCHEMBL3056463
6-(4-{4-[2-(4-acetylpiperazin-1-yl)ethoxy]phenyl}piperidin-1-yl)-3-(trifluoromethyl)-7,8-dihydro[1,2,4]triazolo[4,3-b]pyridazine
1-(4-(2-(4-(1-(3-(trifluoromethyl)-7,8-dihydro-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl)phenoxy)ethyl)piperazin-1-yl)ethanone
unii-127dss8x7j
1-{4-[2-(4-{1-[3-(trifluoromethyl)-7,8-dihydro[1,2,4]triazolo[4,3-b]pyridazin-6-yl]piperidin-4-yl}phenoxy)ethyl]piperazin-1-yl}ethan-1-one
DTXSID80677133
AKOS027422738
HMS3652H18
NCGC00386284-05
ethanone, 1-(4-(2-(4-(1-(7,8-dihydro-3-(trifluoromethyl)-1,2,4-triazolo(4,3-b)pyridazin-6-yl)-4-piperidinyl)phenoxy)ethyl)-1-piperazinyl)-
azd 3514 [who-dd]
127DSS8X7J ,
SW219684-1
BCP07896
FT-0735650
SB19559
1-[4-[2-[4-[1-[3-(trifluoromethyl)-7,8-dihydro-[1,2,4]triazolo[4,3-b]pyridazin-6-yl]piperidin-4-yl]phenoxy]ethyl]piperazin-1-yl]ethanone
CCG-264708
EX-A1806
F84948
MS-29635
AC-35907
nsc-765776
nsc765776
NCGC00386284-02
Z2037280630

Excerpt	Reference	Relevance
"AZD3514 is a first-in-class, orally bio-available, androgen-dependent and -independent androgen receptor inhibitor and selective androgen-receptor down-regulator (SARD)."	( AZD3514, an oral selective androgen receptor down-regulator in patients with castration-resistant prostate cancer - results of two parallel first-in-human phase I studies. Alumkal, JJ; Clack, G; Crespo, M; de Bono, J; Dickinson, PA; Dive, C; Dymond, A; Elliott, T; Finkelman, RD; Graham, J; Jones, RJ; Malone, MD; Moore, D; Nava-Rodrigues, D; Niwakawa, M; Omlin, A; Ong, M; Ranson, M; Riisnaes, R; Satoh, T; Schellens, JH; Sloane, R; Smith, SA; van der Noll, R; Zivi, A, 2015)	3.3
"AZD3514 is a novel, orally-administered compound that inhibits androgen receptor signaling and down-regulates androgen receptor expression."	( The value of integrating pre-clinical data to predict nausea and vomiting risk in humans as illustrated by AZD3514, a novel androgen receptor modulator. Clack, G; Deavall, D; Ewart, L; Grant, C; Muthas, D; Newham, P; Smith, SA, 2016)	1.37

Excerpt	Reference	Relevance
" Here, we describe the biological characterization of AZD3514, an orally bioavailable drug that inhibits androgen-dependent and -independent AR signaling."	( AZD3514: a small molecule that modulates androgen receptor signaling and function in vitro and in vivo. Barry, ST; Bradbury, RH; Brave, SR; Broadbent, N; Brooks, AN; Critchlow, SE; Cumberbatch, M; Dunkley, TP; Gaughan, L; Jacobs, VN; Jones, RD; Loddick, SA; Mouchet, E; Rabow, A; Robinson, DM; Robson, CN; Ross, SJ; Shaheen, FS; Stratton, NC; Thomason, AG; Trueman, D; Walker, GE; Wedge, SR; Wilson, J; Womack, C, 2013)	2.08
"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

Excerpt	Relevance	Reference
" In study 1, pharmacokinetic assessments led to twice daily (BID) dosing (schedule B) to increase exposure."	( AZD3514, an oral selective androgen receptor down-regulator in patients with castration-resistant prostate cancer - results of two parallel first-in-human phase I studies. Alumkal, JJ; Clack, G; Crespo, M; de Bono, J; Dickinson, PA; Dive, C; Dymond, A; Elliott, T; Finkelman, RD; Graham, J; Jones, RJ; Malone, MD; Moore, D; Nava-Rodrigues, D; Niwakawa, M; Omlin, A; Ong, M; Ranson, M; Riisnaes, R; Satoh, T; Schellens, JH; Sloane, R; Smith, SA; van der Noll, R; Zivi, A, 2015)	1.86

Protein Targets (11)

Potency Measurements

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
PPM1D protein	Homo sapiens (human)	Potency	13.1373	0.0052	9.4661	32.9993	AID1347411
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	3.0112	0.0123	7.9835	43.2770	AID1645841
G	Vesicular stomatitis virus	Potency	11.9877	0.0123	8.9648	39.8107	AID1645842
Interferon beta	Homo sapiens (human)	Potency	12.8499	0.0033	9.1582	39.8107	AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)	Potency	11.9877	0.0123	8.9648	39.8107	AID1645842
Inositol hexakisphosphate kinase 1	Homo sapiens (human)	Potency	11.9877	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2C9, partial	Homo sapiens (human)	Potency	11.9877	0.0123	8.9648	39.8107	AID1645842
[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)
Androgen receptor	Homo sapiens (human)	IC50 (µMol)	1.7789	0.0000	0.8753	10.0000	AID1673919; AID1885087; AID738102
Androgen receptor	Homo sapiens (human)	Ki	3.1333	0.0002	0.4240	7.2000	AID1673917; AID1673918; AID738094
Androgen receptor	Rattus norvegicus (Norway rat)	Ki	5.0000	0.0003	1.2185	8.9270	AID738099
Cannabinoid receptor 1	Mus musculus (house mouse)	IC50 (µMol)	1.7783	0.0030	0.9294	3.2000	AID738102
Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)	IC50 (µMol)	100.0000	0.0009	1.9014	10.0000	AID738101
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (121)

Process	via Protein(s)	Taxonomy
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell activation involved in immune response	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to virus	Interferon beta	Homo sapiens (human)
positive regulation of autophagy	Interferon beta	Homo sapiens (human)
cytokine-mediated signaling pathway	Interferon beta	Homo sapiens (human)
natural killer cell activation	Interferon beta	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT protein	Interferon beta	Homo sapiens (human)
cellular response to interferon-beta	Interferon beta	Homo sapiens (human)
B cell proliferation	Interferon beta	Homo sapiens (human)
negative regulation of viral genome replication	Interferon beta	Homo sapiens (human)
innate immune response	Interferon beta	Homo sapiens (human)
positive regulation of innate immune response	Interferon beta	Homo sapiens (human)
regulation of MHC class I biosynthetic process	Interferon beta	Homo sapiens (human)
negative regulation of T cell differentiation	Interferon beta	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Interferon beta	Homo sapiens (human)
defense response to virus	Interferon beta	Homo sapiens (human)
type I interferon-mediated signaling pathway	Interferon beta	Homo sapiens (human)
neuron cellular homeostasis	Interferon beta	Homo sapiens (human)
cellular response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
cellular response to virus	Interferon beta	Homo sapiens (human)
negative regulation of Lewy body formation	Interferon beta	Homo sapiens (human)
negative regulation of T-helper 2 cell cytokine production	Interferon beta	Homo sapiens (human)
positive regulation of apoptotic signaling pathway	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell differentiation	Interferon beta	Homo sapiens (human)
natural killer cell activation involved in immune response	Interferon beta	Homo sapiens (human)
adaptive immune response	Interferon beta	Homo sapiens (human)
T cell activation involved in immune response	Interferon beta	Homo sapiens (human)
humoral immune response	Interferon beta	Homo sapiens (human)
positive regulation of T cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
adaptive immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independent	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of T cell anergy	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
defense response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
detection of bacterium	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-12 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-6 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protection from natural killer cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
innate immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of dendritic cell differentiation	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class Ib	HLA class I histocompatibility antigen, B alpha chain	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)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by hormone	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of DNA-templated transcription	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion homeostasis	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cardiac muscle contraction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cellular response to xenobiotic stimulus	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane depolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion import across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inositol phosphate metabolic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
negative regulation of cold-induced thermogenesis	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (49)

Process	via Protein(s)	Taxonomy
cytokine activity	Interferon beta	Homo sapiens (human)
cytokine receptor binding	Interferon beta	Homo sapiens (human)
type I interferon receptor binding	Interferon beta	Homo sapiens (human)
protein binding	Interferon beta	Homo sapiens (human)
chloramphenicol O-acetyltransferase activity	Interferon beta	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
signaling receptor binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
peptide antigen binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein-folding chaperone binding	HLA class I histocompatibility antigen, B alpha chain	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)
transcription cis-regulatory region binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
delayed rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ubiquitin protein ligase binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
identical protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein homodimerization activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
C3HC4-type RING finger domain binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
scaffold protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol heptakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
protein binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
ATP binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 1-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 3-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (28)

Process	via Protein(s)	Taxonomy
extracellular space	Interferon beta	Homo sapiens (human)
extracellular region	Interferon beta	Homo sapiens (human)
Golgi membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
endoplasmic reticulum	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
Golgi apparatus	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
cell surface	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
ER to Golgi transport vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
secretory granule membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
phagocytic vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
early endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
recycling endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular exosome	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
lumenal side of endoplasmic reticulum membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
MHC class I protein complex	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular space	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
external side of plasma membrane	HLA class I histocompatibility antigen, B alpha chain	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)
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cell surface	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
perinuclear region of cytoplasm	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
fibrillar center	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytosol	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleus	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (28)

Assay ID	Title	Year	Journal	Article
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.
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.
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.
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.
AID1885087	Antagonist activity at Androgen receptor (unknown origin) assessed as downregulation of AR	2022	Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13	Therapeutic Strategies to Target the Androgen Receptor.
AID738097	Fraction unbound in human plasma by equilibrium dialysis method	2013	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7	Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer.
AID738100	Lipophilicity, log D of the compound at pH 7.4	2013	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7	Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer.
AID1673919	Induction of androgen receptor degradation in human LNCaP cells	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Monomeric Targeted Protein Degraders.
AID738086	Clearance in Han Wistar rat at 4 umol/kg, iv and 5 umol/kg, po	2013	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7	Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer.
AID1673918	Inhibition of full length androgen receptor (unknown origin)	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Monomeric Targeted Protein Degraders.
AID738101	Inhibition of human ERG by IonWorks assay	2013	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7	Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer.
AID738082	Oral bioavailability in Han Wistar rat at 5 umol/kg	2013	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7	Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer.
AID738102	Inhibition of androgen receptor-mediated cellular downregulation in human LNCAP cells assessed as decrease in nuclear receptor level after 20 to 22 hrs by laser-scanning fluorescence microplate cytometeric analysis	2013	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7	Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer.
AID738095	Thermodynamic solubility of the compound in phosphate buffer after 24 hrs	2013	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7	Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer.
AID1885089	Oral bioavailability in dog	2022	Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13	Therapeutic Strategies to Target the Androgen Receptor.
AID738096	Fraction unbound in Han Wistar rat plasma by equilibrium dialysis method	2013	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7	Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer.
AID738090	Volume of distribution at steady state in Han Wistar rat at 4 umol/kg, iv and 5 umol/kg, po	2013	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7	Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer.
AID738098	Intrinsic clearance in human hepatocytes measured per 10'6 cells	2013	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7	Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer.
AID738092	Volume of distribution at steady state in beagle dog at 2 umol/kg, iv and 10 umol/kg, po	2013	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7	Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer.
AID738099	Binding affinity to rat androgen receptor ligand binding domain by fluorescence polarization assay	2013	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7	Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer.
AID738083	Oral bioavailability in beagle dog at 10 umol/kg	2013	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7	Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer.
AID738094	Displacement of [3H]R1881 from full length androgen receptor in human LNCAP cells	2013	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7	Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer.
AID738081	Antiandrogenic activity in immature castrated Hershberger rat model assessed as inhibition of testosterone propionate-induced seminal vesicle growth at 50 to 100 mg/kg, po bid for 7 days	2013	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7	Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer.
AID738088	Clearance in beagle dog at 2 umol/kg, iv and 10 umol/kg, po	2013	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7	Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer.
AID1885048	Oral bioavailability in rat	2022	Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13	Therapeutic Strategies to Target the Androgen Receptor.
AID1673917	Inhibition of androgen receptor LBD domain (unknown origin)	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Monomeric Targeted Protein Degraders.
[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	0 (0.00)	29.6817
2010's	9 (64.29)	24.3611
2020's	5 (35.71)	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	2 (14.29%)	5.53%
Reviews	2 (14.29%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	10 (71.43%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
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.	3.66	2	(trifluoromethyl)benzenes; monocarboxylic acid amide; monofluorobenzenes; nitrile; sulfone; tertiary alcohol
oxandrolone Oxandrolone: A synthetic hormone with anabolic and androgenic properties.	3.51	1	17beta-hydroxy steroid; 3-oxo steroid; anabolic androgenic steroid; oxa-steroid	anabolic agent; androgen
medroxyprogesterone acetate [no description available]	3.51	1	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
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.	3.51	1	17beta-hydroxy steroid; 17beta-hydroxyandrostan-3-one; 3-oxo-5alpha-steroid	androgen; Daphnia magna metabolite; human metabolite; mouse metabolite
nitrogenase stabilizing-protective protein, bacteria [no description available]	3.51	1	N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide	androgen antagonist; antineoplastic agent
hydroxyflutamide [no description available]	3.51	1
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	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	N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide
artenimol [no description available]	3.35	1
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	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	quinolinium ion	anthelminthic drug; antineoplastic agent
abiraterone acetate Abiraterone Acetate: An androstene derivative that inhibits STEROID 17-ALPHA-HYDROXYLASE and is used as an ANTINEOPLASTIC AGENT in the treatment of metastatic castration-resistant PROSTATE CANCER.. abiraterone acetate : A sterol ester obtained by formal condensation of the 3-hydroxy group of abiraterone with the carboxy group of acetic acid. A prodrug that is converted in vivo into abiraterone. Used for treatment of metastatic castrate-resistant prostate cancer.	2.08	1	pyridines; sterol ester	antineoplastic agent; EC 1.14.99.9 (steroid 17alpha-monooxygenase) inhibitor; prodrug
andarine [no description available]	3.51	1	acetamides; anilide
lg 121071 [no description available]	3.51	1
bms-564929 [no description available]	3.51	1
mk 2866 [no description available]	3.51	1
lgd 2226 [no description available]	3.51	1
mdv 3100 [no description available]	3.66	2	(trifluoromethyl)benzenes; benzamides; imidazolidinone; monofluorobenzenes; nitrile; thiocarbonyl compound	androgen antagonist; antineoplastic agent
olaparib [no description available]	2.17	1	cyclopropanes; monofluorobenzenes; N-acylpiperazine; phthalazines	antineoplastic agent; apoptosis inducer; EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor
mln 8237 MLN 8237: an aurora kinase A inhibitor	3.35	1	benzazepine
apalutamide [no description available]	3.51	1
pf 998425 [no description available]	3.51	1
lrrk2-in1 LRRK2-IN1: inhibits leucine-rich repeat kinase 2; structure in first source	3.35	1	aromatic amine; aromatic ether; N-acylpiperidine; N-alkylpiperazine; pyrimidobenzodiazepine; secondary amino compound; tertiary amino compound	antineoplastic agent; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor
pf 956980 PF 956980: structure in first source. PF-956980 : A pyrrolopyrimidine that is 7H-pyrrolo[2,3-d]pyrimidine substituted at position 4 by a methyl[(3R,4R)-4-methyl-1-(pyrrolidin-1-ylcarbonyl)piperidin-3-yl]nitrilo group. It is a potent JAK3-selective chemical probe.	3.35	1	N-acylpiperidine; N-acylpyrrolidine; pyrrolopyrimidine; tertiary amino compound	EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
gne-7915 [no description available]	3.35	1
gne-0877 2-methyl-2-(3-methyl-4-((4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)-1H-pyrazol-1-yl)propanenitrile: a leucine-rich repeat kinase 2 (LRRK2) inhibitor; structure in first source	3.35	1
9-(1-methyl-4-pyrazolyl)-1-[1-(1-oxoprop-2-enyl)-2,3-dihydroindol-6-yl]-2-benzo[h][1,6]naphthyridinone [no description available]	3.35	1	naphthyridine derivative
MLI-2 MLI-2 : A member of the class of indazoles that is 1H-indazole that is substituted at position 3 by a 6-(cis-2,6-dimethylmorpholin-4-yl)pyrimidin-4-yl group and at position 5 by a (1-methylcyclopropoxy)group. It is an inhibitor of leucine-rich repeat kinase 2 (LRRK2).	3.35	1	aromatic ether; cyclopropanes; indazoles; morpholines; pyrimidines; tertiary amino compound	EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor

Condition	Indicated	Relationship Strength	Studies	Trials
Cancer of Prostate [description not available]	0	2.49	2	0
Prostatic Neoplasms Tumors or cancer of the PROSTATE.	0	2.49	2	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	2.54	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	6.45	5	1
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.	1	8.45	5	1
Breast Cancer [description not available]	0	2.17	1	0
Breast Neoplasms Tumors or cancer of the human BREAST.	0	2.17	1	0
Cells, Neoplasm Circulating [description not available]	0	3.89	2	1
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	0	2.1	1	0
Emesis [description not available]	0	3.51	1	1
Nausea An unpleasant sensation in the stomach usually accompanied by the urge to vomit. Common causes are early pregnancy, sea and motion sickness, emotional stress, intense pain, food poisoning, and various enteroviruses.	0	8.51	1	1
Vomiting The forcible expulsion of the contents of the STOMACH through the MOUTH.	0	8.51	1	1

azd3514

Description

Cross-References

Synonyms (35)

Research Excerpts

Overview

Bioavailability

Dosage Studied

Protein Targets (11)

Potency Measurements

Inhibition Measurements

Biological Processes (121)

Molecular Functions (49)

Ceullar Components (28)

Bioassays (28)

Research

Studies (14)

Market Indicators

Research Demand Index: 21.00

Study Types

azd3514

Description

Cross-References

Synonyms (35)

Research Excerpts

Overview

Bioavailability

Dosage Studied

Protein Targets (11)

Potency Measurements

Inhibition Measurements

Biological Processes (121)

Molecular Functions (49)

Ceullar Components (28)

Bioassays (28)

Research

Studies (14)

Market Indicators

Research Demand Index: 21.00

Study Types

Related Drugs (28)

Related Conditions (14)