Compounds > azd3965
Page last updated: 2024-08-02 16:10:17

azd3965

Description

AZD3965: a monocarboxylate transporter-1 inhibitor with antineoplastic activity; structure in first source [MeSH]

Cross-References

ID SourceID
PubMed CID10369242
SCHEMBL ID2875156
MeSH IDM000598956

Synonyms (34)

Synonym
cid 10369242
S7339
5-[[(4s)-4-hydroxy-4-methyl-2-isoxazolidinyl]carbonyl]-3-methyl-1-(1-methylethyl)-6-[[5-methyl-3-(trifluoromethyl)-1h-pyrazol-4-yl]methyl]-thieno[2,3-d]pyrimidine-2,4(1h,3h)-dione
SCHEMBL2875156
azd3965
1448671-31-5
HY-12750
AC-33040
4-(2-{[5-methyl-1-(2-naphthyl)-1h-pyrazol-3-yl]oxy}ethyl)morpholine hydrochloride
J-690346
azd-3965 ,
azd 3965
EX-A806
AKOS027323783
(s)-5-(4-hydroxy-4-methylisoxazolidine-2-carbonyl)-1-isopropyl-3-methyl-6-((3-methyl-5-(trifluoromethyl)-1h-pyrazol-4-yl)methyl)thieno[2,3-d]pyrimidine-2,4(1h,3h)-dione
(s)-5-(4-hydroxy-4-methylisoxazolidine-2-carbonyl)-1-isopropyl-3-methyl-6-((5-methyl-3-(trifluoromethyl)-1h-pyrazol-4-yl)methyl)thieno[2,3-d]pyrimidine-2,4(1h,3h)-dione
NCGC00415059-01
733809-45-5
unii-39om5y4k2f
39OM5Y4K2F ,
azd 3965 [who-dd]
5-(((4s)-4-hydroxy-4-methyl-2-isoxazolidinyl)carbonyl)-3-methyl-1-(1-methylethyl)-6-((5-methyl-3-(trifluoromethyl)-1h-pyrazol-4-yl)methyl)thieno(2,3-d)pyrimidine-2,4(1h,3h)-dione
BCP17734
5-[(4s)-4-hydroxy-4-methyl-1,2-oxazolidine-2-carbonyl]-3-methyl-6-{[5-methyl-3-(trifluoromethyl)-1h-pyrazol-4-yl]methyl}-1-(propan-2-yl)-1h,2h,3h,4h-thieno[2,3-d]pyrimidine-2,4-dione
AS-75322
BCP09948
5-[(4s)-4-hydroxy-4-methyl-1,2-oxazolidine-2-carbonyl]-1-isopropyl-3-methyl-6-{[3-methyl-5-(trifluoromethyl)-2h-pyrazol-4-yl]methyl}thieno[2,3-d]pyrimidine-2,4-dione
HMS3873L03
CCG-269813
5-[(4s)-4-hydroxy-4-methyl-1,2-oxazolidine-2-carbonyl]-3-methyl-6-[[5-methyl-3-(trifluoromethyl)-1h-pyrazol-4-yl]methyl]-1-propan-2-ylthieno[2,3-d]pyrimidine-2,4-dione
gtpl10605
nsc-787047
nsc787047
BA164976

Protein Targets (1)

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Monocarboxylate transporter 1Homo sapiens (human)Kd0.0016AID1167921

Bioassays (10)

Assay IDTitleYearJournalArticle
AID1167921Binding affinity to MCT1 (unknown origin)2014Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21
ISSN: 1464-3405		An update on therapeutic opportunities offered by cancer glycolytic metabolism.
AID1654519Inhibition of MCT1 in human A673 cells assessed as reduction in BrPA-induced cytotoxicity at 10 nM by SRB assay2020Journal of natural products, 03-27, Volume: 83, Issue:3
ISSN: 1520-6025		Using the Cancer Dependency Map to Identify the Mechanism of Action of a Cytotoxic Alkenyl Derivative from the Fruit of
AID1654520Growth inhibition of human A673 cells assessed as reduction in cell viability up to 10 uM after 48 hrs by SRB assay2020Journal of natural products, 03-27, Volume: 83, Issue:3
ISSN: 1520-6025		Using the Cancer Dependency Map to Identify the Mechanism of Action of a Cytotoxic Alkenyl Derivative from the Fruit of
AID1723954Antiplasmodial activity against Plasmodium falciparum 3D7 assessed as reduction in parasitemia incubated for 48 hrs supplemented with fresh medium containing compound at 24 hrs by LSR II FACS method2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
ISSN: 1520-4804		Introduction of Scaffold Nitrogen Atoms Renders Inhibitors of the Malarial l-Lactate Transporter, PfFNT, Effective against the Gly107Ser Resistance Mutation.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
ISSN: 2472-5560		Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
ISSN: 1091-6490		Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111		A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111		A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
ISSN: 1091-6490		Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347411qHTS 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) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
ISSN: 1554-8937		High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.

Research

Studies (41)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's17 (41.46)24.3611
2020's24 (58.54)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (2.44%)5.53%
Reviews3 (7.32%)6.00%
Case Studies1 (2.44%)4.05%
Observational0 (0.00%)0.25%
Other36 (87.80%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
1
enone;
pyridines		angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
autophagy inducer;
EC 2.7.1.105 (6-phosphofructo-2-kinase) inhibitor		2014201410.0low000010
wzb117
1
2014201410.0low000010
methyl 1-hydroxy-6-phenyl-4-(trifluoromethyl)-1h-indole-2-carboxylate
1
2014201410.0medium000010
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
formic acid
1
monocarboxylic acidantibacterial agent;
astringent;
metabolite;
protic solvent;
solvent		201820186.0low000010
lactic acid
11
2-hydroxy monocarboxylic acidalgal metabolite;
Daphnia magna metabolite		201420234.5medium000065
pyruvic acid
1
2-oxo monocarboxylic acidcofactor;
fundamental metabolite		201620168.0low000010
uracil
5
pyrimidine nucleobase;
pyrimidone		allergen;
Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
prodrug;
Saccharomyces cerevisiae metabolite		201820214.8low000041
acetaminophen
1
acetamides;
phenols		antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
cyclooxygenase 3 inhibitor;
environmental contaminant;
ferroptosis inducer;
geroprotector;
hepatotoxic agent;
human blood serum metabolite;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic		201920195.0low000010
alpha-cyano-4-hydroxycinnamate
2
201920204.5low000020
fluorouracil
1
nucleobase analogue;
organofluorine compound		antimetabolite;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
radiosensitizing agent;
xenobiotic		201720177.0low000010
metformin
1
guanidinesenvironmental contaminant;
geroprotector;
hypoglycemic agent;
xenobiotic		201720177.0low000010
phloretin
1
dihydrochalconesantineoplastic agent;
plant metabolite		202120213.0low000001
reserpine
1
alkaloid ester;
methyl ester;
yohimban alkaloid		adrenergic uptake inhibitor;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
first generation antipsychotic;
plant metabolite;
xenobiotic		202120213.0low000001
acetonitrile
1
aliphatic nitrile;
volatile organic compound		EC 3.5.1.4 (amidase) inhibitor;
NMR chemical shift reference compound;
polar aprotic solvent		201820186.0low000010
syrosingopine
1
yohimban alkaloid202120213.0low000001
thiophenes
29
mancude organic heteromonocyclic parent;
monocyclic heteroarene;
thiophenes;
volatile organic compound		non-polar solvent201420235.0high1000209
phenformin
1
biguanidesantineoplastic agent;
geroprotector;
hypoglycemic agent		202120213.0low000001
pyrimidine
1
diazine;
pyrimidines		Daphnia magna metabolite201820186.0low000010
triazoles
1
1,2,3-triazole202120213.0low000001
nadp
1
201920195.0low000010
quercetin
1
7-hydroxyflavonol;
pentahydroxyflavone		antibacterial agent;
antineoplastic agent;
antioxidant;
Aurora kinase inhibitor;
chelator;
EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor;
geroprotector;
phytoestrogen;
plant metabolite;
protein kinase inhibitor;
radical scavenger		202120213.0low000001
2-cyano-3-(1-phenylindol-3-yl)acrylate
1
201720177.0low000010
bromopyruvate
1
2-oxo monocarboxylic acid anion201920195.0low000010
ar c155858
5
201820214.8high000041
gsk2194069
1
202120213.0medium000001
pyrimidinones
29
201420235.0high1000209
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Acidosis, Lactic0
1
202020204.0low000010
Adenocarcinoma0
1
202320231.0low000001
Adenocarcinoma, Basal Cell0
1
202320231.0low000001
Aerobic Glycolysis, Oncologic0
1
202120213.0low000001
African Lymphoma0
1
201720177.0low000010
Angiogenesis, Pathologic0
1
202120213.0low000001
Anoxemia0
1
202320231.0low000001
Benign Neoplasms0
6
201420234.8low100033
Breast Cancer0
4
201620205.8low000040
Breast Neoplasms0
4
201620205.8low000040
Burkitt Lymphoma0
1
201720177.0low000010
Cancer of Head0
1
201820186.0low000010
Cancer of Liver0
1
202120213.0low000001
Cancer of Lung0
3
201420207.3low000030
Cancer of Stomach0
1
201720177.0low000010
Carcinoma, Hepatocellular0
1
202120213.0low000001
Carcinoma, Small Cell Lung0
2
201420159.5low000020
Cells, Neoplasm Circulating0
1
201520159.0low000010
Colorectal Cancer0
1
202320231.0low000001
Colorectal Neoplasms0
1
202320231.0low000001
Congenital Zika Syndrome0
1
202020204.0low000010
Diffuse Large B-Cell Lymphoma0
2
201720196.0low000020
Diffuse Mixed Small and Large Cell Lymphoma0
1
201920195.0low000010
Disease Exacerbation0
1
202120213.0low000001
Disease Models, Animal0
3
201420206.0low000030
Experimental Neoplasms0
1
202120213.0low000001
Germinoblastoma0
1
201720177.0low000010
Granulocytic Leukemia0
1
202120213.0low000001
Head and Neck Neoplasms0
1
201820186.0low000010
Hepatocellular Carcinoma0
1
202120213.0low000001
Hyperlactatemia0
1
202020204.0low000010
Hypoxia0
1
202320231.0low000001
Inflammation0
1
202120213.0low000001
Innate Inflammatory Response0
1
202120213.0low000001
Insulin Resistance0
1
202220222.0low000001
Insulin Sensitivity0
1
202220222.0low000001
Kahler Disease0
1
202320231.0low000001
Lactic Acidosis0
1
202020204.0low000010
Leukemia, Myeloid0
1
202120213.0low000001
Liver Neoplasms0
1
202120213.0low000001
Lung Neoplasms0
3
201420207.3low000030
Lymphoma0
1
201720177.0low000010
Lymphoma, Large B-Cell, Diffuse0
2
201720196.0low000020
Lymphoma, Non-Hodgkin0
1
201920195.0low000010
Malignant Melanoma0
1
202020204.0low000010
Melanoma0
1
202020204.0low000010
Multiple Myeloma0
1
202320231.0low000001
Neoplasms0
6
201420234.8low100033
Neuroblastoma0
1
202120213.0low000001
Small Cell Lung Carcinoma0
2
201420159.5low000020
Stomach Neoplasms0
1
201720177.0low000010
Zika Virus Infection0
1
202020204.0low000010

Safety/Toxicity (1)

ArticleYear
Acetaminophen cytotoxicity in HepG2 cells is associated with a decoupling of glycolysis from the TCA cycle, loss of NADPH production, and suppression of anabolism.
Archives of toxicology, , Volume: 93, Issue:2		2019

Pharmacokinetics (2)

ArticleYear
Pharmacokinetics of the Monocarboxylate Transporter 1 Inhibitor AZD3965 in Mice: Potential Enterohepatic Circulation and Target-Mediated Disposition.
Pharmaceutical research, , Dec-10, Volume: 37, Issue:1		2019
Development and validation of a liquid chromatography tandem mass spectrometry assay for AZD3965 in mouse plasma and tumor tissue: Application to pharmacokinetic and breast tumor xenograft studies.
Journal of pharmaceutical and biomedical analysis, , Jun-05, Volume: 155		2018

Bioavailability (3)

ArticleYear
Pharmacokinetics of the Monocarboxylate Transporter 1 Inhibitor AZD3965 in Mice: Potential Enterohepatic Circulation and Target-Mediated Disposition.
Pharmaceutical research, , Dec-10, Volume: 37, Issue:1		2019
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology, , Volume: 96, Issue:5		2019
Development and validation of a liquid chromatography tandem mass spectrometry assay for AZD3965 in mouse plasma and tumor tissue: Application to pharmacokinetic and breast tumor xenograft studies.
Journal of pharmaceutical and biomedical analysis, , Jun-05, Volume: 155		2018

Dosage (1)

ArticleYear
Effects of a monocarboxylate transport 1 inhibitor, AZD3965, on retinal and visual function in the rat.
British journal of pharmacology, , Volume: 177, Issue:20		2020