ns 1643 profile

1,3-bis(2-hydroxy-5-trifluoromethylphenyl)urea: an antiarrhythmic agent that activates HERG channels; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	10177784
CHEMBL ID	1514181
SCHEMBL ID	1462428
MeSH ID	M0494676

Synonym
gtpl2308
1,3-bis[2-hydroxy-5-(trifluoromethyl)phenyl]urea
ns1643
ns-1643
ns1643, >=98% (hplc), solid
NCGC00165838-01
SCHEMBL1462428
448895-37-2
1,3-bis(2-hydroxy-5-(trifluoromethyl)phenyl)urea
AKOS016007392
ns 1643
S5773
urea, n,n'-bis(2-hydroxy-5-(trifluoromethyl)phenyl)-
0I579CNG0I ,
1,3-bis(2-hydroxy-5-trifluoromethylphenyl)urea
unii-0i579cng0i
c15h10f6n2o3
n,n'-bis[2-hydroxy-5-(trifluoromethyl)phenyl]urea
HB1066
n,n'-bis[2-hydroxy-5-(trifluoromethy l)phenyl]urea
CHEMBL1514181
HY-16916
DTXSID00436481
mfcd08705418
BCP15446
Q27088049
AMY36462
N11077
EX-A4161
n,n'-bis[2-hydroxy-5-(trifluoromethyl)phenyl] urea
AS-55847
YSA89537
njfvqmryjzhgme-uhfffaoysa-n

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
nuclear receptor ROR-gamma isoform 1	Mus musculus (house mouse)	Potency	28.1838	0.0079	8.2332	1,122.0200	AID2546
histone acetyltransferase KAT2A isoform 1	Homo sapiens (human)	Potency	39.8107	0.2512	15.8432	39.8107	AID504327
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Assay ID	Title	Year	Journal	Article
AID1346751	Human Kv11.1 (Voltage-gated potassium channels)	2006	Molecular pharmacology, Jan, Volume: 69, Issue:1	Activation of human ether-a-go-go-related gene potassium channels by the diphenylurea 1,3-bis-(2-hydroxy-5-trifluoromethyl-phenyl)-urea (NS1643).
AID1346771	Human Kv11.2 (Voltage-gated potassium channels)	2007	Neuropharmacology, Aug, Volume: 53, Issue:2	Activation of ERG2 potassium channels by the diphenylurea NS1643.
AID1346751	Human Kv11.1 (Voltage-gated potassium channels)	2006	Molecular pharmacology, Feb, Volume: 69, Issue:2	Mechanism of action of a novel human ether-a-go-go-related gene channel activator.
AID1346446	Human KCa1.1 (Calcium- and sodium-activated potassium channels)	1996	Neuropharmacology, , Volume: 35, Issue:7	Modulation of the Ca(2+)-dependent K+ channel, hslo, by the substituted diphenylurea NS 1608, paxilline and internal Ca2+.
AID1346727	Rat Kv11.3 (Voltage-gated potassium channels)	2012	PloS one, , Volume: 7, Issue:11	Effects of the small molecule HERG activator NS1643 on Kv11.3 channels.
[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	1 (3.13)	18.2507
2000's	11 (34.38)	29.6817
2010's	18 (56.25)	24.3611
2020's	2 (6.25)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	1 (3.13%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	31 (96.88%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
4-aminopyridine [no description available]	2.05	1	aminopyridine; aromatic amine	avicide; orphan drug; potassium channel blocker
e 4031 E 4031: class III anti-arrhythmia agent; structure given in UD	2.48	2	sulfonamide
pinacidil Pinacidil: A guanidine that opens POTASSIUM CHANNELS producing direct peripheral vasodilatation of the ARTERIOLES. It reduces BLOOD PRESSURE and peripheral resistance and produces fluid retention. (Martindale The Extra Pharmacopoeia, 31st ed)	2.05	1	pyridines
terfenadine Terfenadine: A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME.	2.21	1	diarylmethane
nicorandil Nicorandil: A derivative of the NIACINAMIDE that is structurally combined with an organic nitrate. It is a potassium-channel opener that causes vasodilatation of arterioles and large coronary arteries. Its nitrate-like properties produce venous vasodilation through stimulation of guanylate cyclase.. nicorandil : A pyrimidinecarboxamide that is nicotinamide in which one of the hydrogens attached to the carboxamide nitrogen is replaced by a 2-(nitrooxy)ethyl group. It has both nitrate-like and ATP-sensitive potassium channel activator properties, and is used for the prevention and treatment of angina pectoris.	2.04	1	nitrate ester; pyridinecarboxamide	potassium channel opener; vasodilator agent
uk 68798 [no description available]	2.49	2	aromatic ether; sulfonamide; tertiary amino compound	anti-arrhythmia drug; potassium channel blocker
oxytocin Oxytocin: A nonapeptide hormone released from the neurohypophysis (PITUITARY GLAND, POSTERIOR). It differs from VASOPRESSIN by two amino acids at residues 3 and 8. Oxytocin acts on SMOOTH MUSCLE CELLS, such as causing UTERINE CONTRACTIONS and MILK EJECTION.. oxytocin : A cyclic nonapeptide hormone with amino acid sequence CYIQNCPLG that also acts as a neurotransmitter in the brain; the principal uterine-contracting and milk-ejecting hormone of the posterior pituitary. Together with the neuropeptide vasopressin, it is believed to influence social cognition and behaviour.	2.05	1	heterodetic cyclic peptide; peptide hormone	oxytocic; vasodilator agent
3-nitro-n-(4-phenoxyphenyl)benzamide [no description available]	2.08	1
rpr260243 RPR260243: small molecule activator of the human ether-a-go-go-related gene (HERG) cardiac K+ channel; structure in first source	2.51	2
piperidines Piperidines: A family of hexahydropyridines.	3	4
ns 309 6,7-dichloro-1H-indole-2,3-dione 3-oxime: activates IK and SK calcium-activated channels; structure in first source	2.04	1

Condition	Relationship Strength	Studies
ER-Negative PR-Negative HER2-Negative Breast Cancer [description not available]	2.69	2
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.	2.69	2
Blood Poisoning [description not available]	2.31	1
Cardiac Diseases [description not available]	2.31	1
Heart Diseases Pathological conditions involving the HEART including its structural and functional abnormalities.	2.31	1
Sepsis Systemic inflammatory response syndrome with a proven or suspected infectious etiology. When sepsis is associated with organ dysfunction distant from the site of infection, it is called severe sepsis. When sepsis is accompanied by HYPOTENSION despite adequate fluid infusion, it is called SEPTIC SHOCK.	2.31	1
Electrocardiogram QT Prolonged [description not available]	2.77	3
Long QT Syndrome A condition that is characterized by episodes of fainting (SYNCOPE) and varying degree of ventricular arrhythmia as indicated by the prolonged QT interval. The inherited forms are caused by mutation of genes encoding cardiac ion channel proteins. The two major forms are ROMANO-WARD SYNDROME and JERVELL-LANGE NIELSEN SYNDROME.	2.77	3
Metastase [description not available]	2.21	1
Neoplasm Metastasis The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.	2.21	1
Breast Cancer [description not available]	2.51	2
Breast Neoplasms Tumors or cancer of the human BREAST.	2.51	2
Arrhythmia [description not available]	2.74	3
Arrhythmias, Cardiac Any disturbances of the normal rhythmic beating of the heart or MYOCARDIAL CONTRACTION. Cardiac arrhythmias can be classified by the abnormalities in HEART RATE, disorders of electrical impulse generation, or impulse conduction.	2.74	3
Aura [description not available]	2.1	1
Epilepsy A disorder characterized by recurrent episodes of paroxysmal brain dysfunction due to a sudden, disorderly, and excessive neuronal discharge. Epilepsy classification systems are generally based upon: (1) clinical features of the seizure episodes (e.g., motor seizure), (2) etiology (e.g., post-traumatic), (3) anatomic site of seizure origin (e.g., frontal lobe seizure), (4) tendency to spread to other structures in the brain, and (5) temporal patterns (e.g., nocturnal epilepsy). (From Adams et al., Principles of Neurology, 6th ed, p313)	2.1	1
Carcinogenesis The origin, production or development of cancer through genotypic and phenotypic changes which upset the normal balance between cell proliferation and cell death. Carcinogenesis generally requires a constellation of steps, which may occur quickly or over a period of many years.	2.13	1
Cancer of Pituitary [description not available]	2.04	1
Pituitary Neoplasms Neoplasms which arise from or metastasize to the PITUITARY GLAND. The majority of pituitary neoplasms are adenomas, which are divided into non-secreting and secreting forms. Hormone producing forms are further classified by the type of hormone they secrete. Pituitary adenomas may also be characterized by their staining properties (see ADENOMA, BASOPHIL; ADENOMA, ACIDOPHIL; and ADENOMA, CHROMOPHOBE). Pituitary tumors may compress adjacent structures, including the HYPOTHALAMUS, several CRANIAL NERVES, and the OPTIC CHIASM. Chiasmal compression may result in bitemporal HEMIANOPSIA.	2.04	1
Pregnancy The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.	2.05	1
Hypokalemia Abnormally low potassium concentration in the blood. It may result from potassium loss by renal secretion or by the gastrointestinal route, as by vomiting or diarrhea. It may be manifested clinically by neuromuscular disorders ranging from weakness to paralysis, by electrocardiographic abnormalities (depression of the T wave and elevation of the U wave), by renal disease, and by gastrointestinal disorders. (Dorland, 27th ed)	2.04	1
Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.	2.04	1
Atrioventricular Conduction Block [description not available]	2.04	1
Bradyarrhythmia [description not available]	2.04	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.04	1
Torsade de Pointes [description not available]	2.04	1
Bradycardia Cardiac arrhythmias that are characterized by excessively slow HEART RATE, usually below 50 beats per minute in human adults. They can be classified broadly into SINOATRIAL NODE dysfunction and ATRIOVENTRICULAR BLOCK.	2.04	1
Atrioventricular Block Impaired impulse conduction from HEART ATRIA to HEART VENTRICLES. AV block can mean delayed or completely blocked impulse conduction.	2.04	1
Hyperpotassemia [description not available]	2.04	1
Hyperkalemia Abnormally high potassium concentration in the blood, most often due to defective renal excretion. It is characterized clinically by electrocardiographic abnormalities (elevated T waves and depressed P waves, and eventually by atrial asystole). In severe cases, weakness and flaccid paralysis may occur. (Dorland, 27th ed)	2.04	1

ns 1643

Description

Cross-References

Synonyms (33)

Protein Targets (2)

Potency Measurements

Bioassays (5)

Research

Studies (32)

Market Indicators

Research Demand Index: 28.73

Study Types