Compounds > t16ainh-a01
Page last updated: 2024-10-15

t16ainh-a01

Description

T16AInh-A01: a TMEM16A inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID135460621
CHEMBL ID1299863
SCHEMBL ID16504337
MeSH IDM0581661

Synonyms (36)

Synonym
BB 0263143
OPREA1_490830
MLS000714464
smr000274443
OPREA1_393059
AKOS000697276
2-[(5-ethyl-6-methyl-4-oxo-1h-pyrimidin-2-yl)sulfanyl]-n-[4-(4-methoxyphenyl)-1,3-thiazol-2-yl]acetamide
HMS2696F08
CHEMBL1299863
VU0462191-1
AKOS016023818
t16ainh-a01
SCHEMBL16504337
t16a(inh)-a01
552309-42-9
t16ainh - a01
2-[(5-ethyl-1,6-dihydro-4-methyl-6-oxo-2-pyrimidinyl)thio]-n-[4-(4-methoxyphenyl)-2-thiazolyl]acetamide
AKOS027320699
2-(5-ethyl-4-hydroxy-6-methylpyrimidin-2-ylthio)-n-(4-(4-methoxyphenyl)thiazol-2-yl)acetamide
t16ainh-a01, >=95% (hplc)
2-((5-ethyl-4-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)thio)-n-(4-(4-methoxyphenyl)thiazol-2-yl)acetamide ,
t-16ainh-a01
AS-16407
2-[(5-ethyl-4-hydroxy-6-methylpyrimidin-2-yl)sulfanyl]-n-[4-(4-methoxyphenyl)-1,3-thiazol-2-yl]acetamide
EN300-127951
CS-0019784
D94996
HY-100612
SB60412
A899766
EX-A4754
2-[(5-ethyl-4-methyl-6-oxo-1h-pyrimidin-2-yl)sulfanyl]-n-[4-(4-methoxyphenyl)-1,3-thiazol-2-yl]acetamide
CXA30942
tmem16a inhibitor, t16ainh-a01
2-[(5-ethyl-1,6-dihydro-4-methyl-6-oxo-2-pyrimidinyl)thio]-n-[4-(4-methoxyphenyl)-2-thiazolyl]-acetamide
Z1606818714
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency14.12540.044717.8581100.0000AID485341
LuciferasePhotinus pyralis (common eastern firefly)Potency9.52830.007215.758889.3584AID588342
glp-1 receptor, partialHomo sapiens (human)Potency0.50120.01846.806014.1254AID624417
mitogen-activated protein kinase 1Homo sapiens (human)Potency39.81070.039816.784239.8107AID1454
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency70.79460.050127.073689.1251AID588590
lamin isoform A-delta10Homo sapiens (human)Potency0.01120.891312.067628.1838AID1487
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Anoctamin-1Homo sapiens (human)IC50 (µMol)1.00000.02800.62641.6000AID1448055
Anoctamin-2Homo sapiens (human)IC50 (µMol)4.00004.00004.00004.0000AID1448075
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (13)

Processvia Protein(s)Taxonomy
chloride transportAnoctamin-1Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAnoctamin-1Homo sapiens (human)
iodide transportAnoctamin-1Homo sapiens (human)
monoatomic ion transmembrane transportAnoctamin-1Homo sapiens (human)
cellular response to heatAnoctamin-1Homo sapiens (human)
positive regulation of insulin secretion involved in cellular response to glucose stimulusAnoctamin-1Homo sapiens (human)
detection of temperature stimulus involved in sensory perception of painAnoctamin-1Homo sapiens (human)
mucus secretionAnoctamin-1Homo sapiens (human)
protein localization to membraneAnoctamin-1Homo sapiens (human)
monoatomic cation transmembrane transportAnoctamin-1Homo sapiens (human)
glial cell projection elongationAnoctamin-1Homo sapiens (human)
cellular response to peptideAnoctamin-1Homo sapiens (human)
chloride transmembrane transportAnoctamin-1Homo sapiens (human)
monoatomic ion transmembrane transportAnoctamin-2Homo sapiens (human)
chloride transmembrane transportAnoctamin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (11)

Processvia Protein(s)Taxonomy
signaling receptor bindingAnoctamin-1Homo sapiens (human)
calcium-activated cation channel activityAnoctamin-1Homo sapiens (human)
intracellularly calcium-gated chloride channel activityAnoctamin-1Homo sapiens (human)
voltage-gated chloride channel activityAnoctamin-1Homo sapiens (human)
chloride channel activityAnoctamin-1Homo sapiens (human)
protein bindingAnoctamin-1Homo sapiens (human)
iodide transmembrane transporter activityAnoctamin-1Homo sapiens (human)
identical protein bindingAnoctamin-1Homo sapiens (human)
protein homodimerization activityAnoctamin-1Homo sapiens (human)
metal ion bindingAnoctamin-1Homo sapiens (human)
intracellularly calcium-gated chloride channel activityAnoctamin-2Homo sapiens (human)
protein bindingAnoctamin-2Homo sapiens (human)
protein dimerization activityAnoctamin-2Homo sapiens (human)
chloride channel activityAnoctamin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
nucleoplasmAnoctamin-1Homo sapiens (human)
plasma membraneAnoctamin-1Homo sapiens (human)
apical plasma membraneAnoctamin-1Homo sapiens (human)
cell projectionAnoctamin-1Homo sapiens (human)
extracellular exosomeAnoctamin-1Homo sapiens (human)
presynapseAnoctamin-1Homo sapiens (human)
chloride channel complexAnoctamin-1Homo sapiens (human)
plasma membraneAnoctamin-1Homo sapiens (human)
nucleoplasmAnoctamin-2Homo sapiens (human)
plasma membraneAnoctamin-2Homo sapiens (human)
chloride channel complexAnoctamin-2Homo sapiens (human)
plasma membraneAnoctamin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (18)

Assay IDTitleYearJournalArticle
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1448055Inhibition of human TMEM16A expressed in FRT cells assessed as reduction of ATP-induced in chloride conductance preincubated for 5 mins followed by ATP addition by short-circuit current assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Substituted 2-Acylaminocycloalkylthiophene-3-carboxylic Acid Arylamides as Inhibitors of the Calcium-Activated Chloride Channel Transmembrane Protein 16A (TMEM16A).
AID1448058Cytotoxicity against human HT-29 cells assessed as cell survival at 5 uM after 8 hrs by alamar blue assay relative to control2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Substituted 2-Acylaminocycloalkylthiophene-3-carboxylic Acid Arylamides as Inhibitors of the Calcium-Activated Chloride Channel Transmembrane Protein 16A (TMEM16A).
AID1448059Inhibition of human wild type CFTR expressed in FRT cells co-expressing halide sensitive YFP-H148Q assessed as reduction in forskolin induced cAMP activated chloride conductance by measuring decrease in iodide influx after 15 mins by fluorescence assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Substituted 2-Acylaminocycloalkylthiophene-3-carboxylic Acid Arylamides as Inhibitors of the Calcium-Activated Chloride Channel Transmembrane Protein 16A (TMEM16A).
AID1448075Inhibition of TMEM16B (unknown origin) expressed in FRT cells assessed as reduction of ATP-induced chloride conductance preincubated for 20 mins followed by ATP addition by short-circuit current assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Substituted 2-Acylaminocycloalkylthiophene-3-carboxylic Acid Arylamides as Inhibitors of the Calcium-Activated Chloride Channel Transmembrane Protein 16A (TMEM16A).
AID1448061Inhibition of calcium activated chloride channel in ATP-activated human HT-29 cells expressing YFP-H148Q/152L assessed as reduction in iodide influx preincubated for 10 mins followed by ATP addition by fluorescence assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Substituted 2-Acylaminocycloalkylthiophene-3-carboxylic Acid Arylamides as Inhibitors of the Calcium-Activated Chloride Channel Transmembrane Protein 16A (TMEM16A).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (28)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (3.57)29.6817
2010's22 (78.57)24.3611
2020's5 (17.86)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other28 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
chlorine
chloride : A halide anion formed when chlorine picks up an electron to form an an anion.		2.5820halide anion;
monoatomic chlorine		cofactor;
Escherichia coli metabolite;
human metabolite
dimethyl sulfoxide
Dimethyl Sulfoxide: A highly polar organic liquid, that is used widely as a chemical solvent. Because of its ability to penetrate biological membranes, it is used as a vehicle for topical application of pharmaceuticals. It is also used to protect tissue during CRYOPRESERVATION. Dimethyl sulfoxide shows a range of pharmacological activity including analgesia and anti-inflammation.. dimethyl sulfoxide : A 2-carbon sulfoxide in which the sulfur atom has two methyl substituents.		2.4110sulfoxide;
volatile organic compound		alkylating agent;
antidote;
Escherichia coli metabolite;
geroprotector;
MRI contrast agent;
non-narcotic analgesic;
polar aprotic solvent;
radical scavenger
benzbromarone
Benzbromarone: Uricosuric that acts by increasing uric acid clearance. It is used in the treatment of gout.. benzbromarone : 1-Benzofuran substituted at C-2 and C-3 by an ethyl group and a 3,5-dibromo-4-hydroxybenzoyl group respectively. An inhibitor of CYP2C9, it is used as an anti-gout medication.		7.61201-benzofurans;
aromatic ketone		uricosuric drug
indomethacin
Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.. indometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis.		2.0710aromatic ether;
indole-3-acetic acids;
monochlorobenzenes;
N-acylindole		analgesic;
drug metabolite;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
gout suppressant;
non-steroidal anti-inflammatory drug;
xenobiotic metabolite;
xenobiotic
nifedipine
Nifedipine: A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure.		2.0710C-nitro compound;
dihydropyridine;
methyl ester		calcium channel blocker;
human metabolite;
tocolytic agent;
vasodilator agent
niflumic acid
Niflumic Acid: An analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis.		3.2250aromatic carboxylic acid;
pyridines
galactose
galactopyranose : The pyranose form of galactose.		2.2110D-galactose;
galactopyranose		Escherichia coli metabolite;
mouse metabolite
thiophenes
Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.		3.2550mancude organic heteromonocyclic parent;
monocyclic heteroarene;
thiophenes;
volatile organic compound		non-polar solvent
anthracene
acene : A polycyclic aromatic hydrocarbon consisting of fused benzene rings in a rectilinear arrangement.. acenes : Polycyclic aromatic hydrocarbons consisting of fused benzene rings in a rectilinear arrangement and their substitution derivatives.		2.110acene;
anthracenes;
ortho-fused tricyclic hydrocarbon
thiazoles
[no description available]		4.592201,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
monocrotaline
Monocrotaline: A pyrrolizidine alkaloid and a toxic plant constituent that poisons livestock and humans through the ingestion of contaminated grains and other foods. The alkaloid causes pulmonary artery hypertension, right ventricular hypertrophy, and pathological changes in the pulmonary vasculature. Significant attenuation of the cardiopulmonary changes are noted after oral magnesium treatment.		2.0710pyrrolizidine alkaloid
capsaicin
ALGRX-4975: an injectable capsaicin (TRPV1 receptor agonist) formulation for longlasting pain relief. capsaicinoid : A family of aromatic fatty amides produced as secondary metabolites by chilli peppers.		2.1110capsaicinoidnon-narcotic analgesic;
TRPV1 agonist;
voltage-gated sodium channel blocker
u 0126
U 0126: protein kinase kinase inhibitor; structure in first source		2.3110aryl sulfide;
dinitrile;
enamine;
substituted aniline		antineoplastic agent;
antioxidant;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
osteogenesis regulator;
vasoconstrictor agent
n-((4-methoxy)-2-naphthyl)-5-nitroanthranilic acid
N-((4-methoxy)-2-naphthyl)-5-nitroanthranilic acid: inhibits anoctamin-1; structure in first source		2.8330
ConditionIndicatedRelationship StrengthStudiesTrials
Innate Inflammatory Response
[description not available]		02.0510
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		02.0510
Pain, Chronic
[description not available]		02.3110
Allodynia
[description not available]		02.6320
Nerve Pain
[description not available]		02.6320
Neuralgia
Intense or aching pain that occurs along the course or distribution of a peripheral or cranial nerve.		02.6320
Chronic Pain
Aching sensation that persists for more than a few months. It may or may not be associated with trauma or disease, and may persist after the initial injury has healed. Its localization, character, and timing are more vague than with acute pain.		02.3110
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.8630
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		02.1710
Presbycusis
Gradual bilateral hearing loss associated with aging that is due to progressive degeneration of cochlear structures and central auditory pathways. Hearing loss usually begins with the high frequencies then progresses to sounds of middle and low frequencies.		02.2110
Aging
The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time.		02.2110
Gastrointestinal Stromal Neoplasm
[description not available]		02.5420
Cancer of Gastrointestinal Tract
[description not available]		02.5420
Gastrointestinal Stromal Tumors
All tumors in the GASTROINTESTINAL TRACT arising from mesenchymal cells (MESODERM) except those of smooth muscle cells (LEIOMYOMA) or Schwann cells (SCHWANNOMA).		02.5420
Lung Injury, Acute
[description not available]		02.1310
Edema, Pulmonary
[description not available]		02.1310
Pulmonary Edema
Excessive accumulation of extravascular fluid in the lung, an indication of a serious underlying disease or disorder. Pulmonary edema prevents efficient PULMONARY GAS EXCHANGE in the PULMONARY ALVEOLI, and can be life-threatening.		02.1310
Acute Lung Injury
A condition of lung damage that is characterized by bilateral pulmonary infiltrates (PULMONARY EDEMA) rich in NEUTROPHILS, and in the absence of clinical HEART FAILURE. This can represent a spectrum of pulmonary lesions, endothelial and epithelial, due to numerous factors (physical, chemical, or biological).		02.1310
Epithelial Neoplasms
[description not available]		02.1310
Hypertrophy, Right Ventricular
Enlargement of the RIGHT VENTRICLE of the heart. This increase in ventricular mass is often attributed to PULMONARY HYPERTENSION and is a contributor to cardiovascular morbidity and mortality.		02.0710
Pulmonary Hypertension
[description not available]		02.0710
Hypertension, Pulmonary
Increased VASCULAR RESISTANCE in the PULMONARY CIRCULATION, usually secondary to HEART DISEASES or LUNG DISEASES.		02.0710