Closantel is a synthetic anthelmintic drug used to treat and prevent infections caused by parasitic worms in livestock, particularly sheep and cattle. It is a member of the salicylanilide class of drugs. Closantel is effective against a wide range of flukes and roundworms. Its mechanism of action is related to its ability to inhibit the enzyme mitochondrial electron transport, which is essential for parasite metabolism. Closantel is typically administered orally, either as a drench or bolus. The drug is well absorbed and distributed throughout the body, reaching therapeutic concentrations in the target tissues. Closantel is metabolized in the liver and excreted in the urine and feces. The development of resistance to closantel is a growing concern, and there is an ongoing need for research to understand the mechanisms of resistance and to develop new drugs to overcome it. Research on closantel is also focused on improving its efficacy and safety, as well as exploring its potential use in other animal species. The compound is being investigated for its potential to treat parasitic infections in humans, particularly in developing countries where these infections are a major public health problem.'
closantel: structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
N-{5-chloro-4-[(4-chlorophenyl)(cyano)methyl]-2-methylphenyl}-2-hydroxy-3,5-diiodobenzamide : An aromatic amide resulting from the formal condensation of the carboxy group of 3,5-diiodosalicylic acid with the amino group of aniline substituted at positions 2, 4, and 5 by methyl, (4-chlorophenyl)(cyano)methyl, and methyl groups respectively. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
closantel : A racemate comprising equimolar amounts of (R)- and (S)-clostanel. An anthelmintic, it is used (as the dihydrate of the sodium salt) in veterinary medicine for the treatment of fluke and nematode infections. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
ID Source | ID |
---|---|
PubMed CID | 42574 |
CHEMBL ID | 12131 |
CHEBI ID | 77054 |
SCHEMBL ID | 116617 |
MeSH ID | M0080518 |
Synonym |
---|
AC-277 |
AKOS005448897 |
r 31,520 |
nsc335306 |
5'-chloro-.alpha.4-(p-chlorophenyl)-.alpha.4-cyano-3,4'-salicyloxylidide |
57808-65-8 |
nsc-335306 |
closantel |
benzamide, n-(5-chloro-4-((4-chlorophenyl)cyanomethyl)-2-methylphenyl)-2-hydroxy-3,5-diiodo- |
c22h14cl2i2n2o2 |
nsc 335306 |
closantelum [inn-latin] |
r 31520 |
5'-chloro-alpha(sup 4)-(p-chlorophenyl)-alpha(sup 4)-cyano-3,5-diiodo-2',4'-salicyloxylidide |
n-(5-chloro-4-((4-chlorophenyl)cyanomethyl)-2-methylphenyl)-2-hydroxy-3,5-diiodobenzamide |
einecs 260-967-1 |
closantel (usan/inn) |
D03567 |
MLS001332594 |
MLS001332593 , |
smr000857079 |
NCGC00166312-01 |
n-{5-chloro-4-[(4-chlorophenyl)(cyano)methyl]-2-methylphenyl}-2-hydroxy-3,5-diiodobenzamide |
STK378904 |
HMS2090A06 |
KUC107298N |
ksc-18-157-1 |
r-31520 |
CHEMBL12131 , |
chebi:77054 , |
n-[5-chloro-4-[(4-chlorophenyl)-cyanomethyl]-2-methylphenyl]-2-hydroxy-3,5-diiodobenzamide |
n-(5-chloro-4-((4-chlorophenyl)(cyano)methyl)-2-methylphenyl)-2-hydroxy-3,5-diiodobenzamide |
n-{5-chloro-4-[(4-chloro-phenyl)-cyano-methyl]-2-methyl-phenyl}-2-hydroxy-3,5-diiodo-benzamide |
bdbm50063753 |
cid_42574 |
n-[5-chloranyl-4-[(4-chlorophenyl)-cyano-methyl]-2-methyl-phenyl]-3,5-bis(iodanyl)-2-oxidanyl-benzamide |
A831617 |
sr-05000001507 |
SR-05000001507-4 |
dtxcid4020662 |
dtxsid6040662 , |
cas-57808-65-8 |
tox21_112408 |
pharmakon1600-01504835 |
nsc-759819 |
nsc759819 |
HMS2230O20 |
S4106 |
unii-eul532ei54 |
closantelum |
closantel [usan:inn:ban] |
eul532ei54 , |
ccris 9345 |
FT-0603196 |
AM20060678 |
CCG-213322 |
SCHEMBL116617 |
NCGC00166312-02 |
tox21_112408_1 |
KS-1255 |
closantel [mi] |
closantel [usan] |
closantel [inn] |
closantel [mart.] |
(rs)-5'-chloro-4'-(4-chloro-.alpha.-cyanobenzyl)-3,5-diiodosalicyl-o-toluidide |
CS-3975 |
HY-17596 |
AB00918405_05 |
AB00918405_06 |
mfcd00661151 |
benzamide, n-[5-chloro-4-[(4-chlorophenyl)cyanomethyl]-2-methylphenyl]-2-hydroxy-3,5-diiodo- |
SR-05000001507-1 |
closantel, pestanal(r), analytical standard |
HMS3652O14 |
SR-05000001507-3 |
n-[5-chloro-4-[(4-chlorophenyl)cyanomethyl]-2-methylphenyl]-2-hydroxy-3,5-diiodobenzamide; closantel; clozantin; nsc 335306; seponver; zycloz |
HMS3713O22 |
SW198946-2 |
n-[5-chloro-4-[(chlorophenyl)cyannomethyl]-2-methylphenyl]-2-hydroxy-3,5-diiodobenzamide |
Q2560163 |
closantel 100 microg/ml in acetonitrile |
A928072 |
n-(5-chloro-4-((2-chlorophenyl)(cyano)methyl)-2-methylphenyl)-2-hydroxy-3,5-diiodobenzamide |
n-(5-chloro-4-[(r,s)-(4-chlorophenyl)cyanomethyl]-2-methylphenyl)-2-hydroxy-3,5-diiodobenzamide |
57808-65-8 (free acid) |
GLXC-26298 |
closantel 1000 microg/ml in acetonitrile |
Closantel is a veterinary anti-helminthic drug used mainly in livestock. It is a potentially toxic drug causing destruction of the neurosensory retina and visual disturbances. Closantal is a halogenated salicylanilide with a potent anti parasitic activity.
The first six-monthly greasy fleece yield was greater in the group treated with medicated pellets. Treatment with closantel (7.5 mg/kg) at the same times was very effective against H.
Excerpt | Reference | Relevance |
---|---|---|
"Closantel is a potentially toxic drug causing destruction of the neurosensory retina and visual disturbances." | ( Closantel retinal toxicity: Recovery from severe vision loss after corticosteroid therapy. Alizadeh, Y; Azaripour, E; Behboudi, H; Medghalchi, A; Moravvej, Z; Soltani-Moghadam, R, 2023) | 3.8 |
Excerpt | Reference | Relevance |
---|---|---|
"The pharmacokinetic disposition of closantel was examined following intraruminal (i." | ( Comparative pharmacokinetic disposition of closantel in sheep and goats. Collins, GH; Hennessy, DR; Sangster, NC; Steel, JW, 1993) | 0.83 |
" With ivermectin it was noted that absorption and excretion were more rapid and Cmax higher in the combination, although the AUC of both formulations were not significantly different." | ( Pharmacokinetics of a novel closantel/ivermectin injection in cattle. Couper, A; Cromie, L; Ferry, M; Fields, C; Taylor, SM, 2006) | 0.63 |
" The aim of the current review article was to provide an overview of the relationship between the pharmacokinetic features of different anthelmintic drugs, their availability in host tissues, accumulation within target helminths and resulting therapeutic efficacy." | ( Host pharmacokinetics and drug accumulation of anthelmintics within target helminth parasites of ruminants. Alvarez, L; Lanusse, C; Lifschitz, A, 2017) | 0.46 |
Excerpt | Reference | Relevance |
---|---|---|
"The strategic use of moxidectin or closantel in combination with levamisole (LEV) to control gastrointestinal nematodes of sheep in the highlands of central Kenya was examined." | ( Strategic use of moxidectin or closantel in combination with levamisole in the control of nematodes of sheep in the highlands of central Kenya. Gichigi, MN; Maingi, N; Munyua, WK, 2002) | 0.88 |
Excerpt | Reference | Relevance |
---|---|---|
"Closantel was reasonably well absorbed in sheep and cattle." | ( The metabolism and fate of closantel (Flukiver) in sheep and cattle. Heykants, J; Meuldermans, W; Michiels, M, 1987) | 2.01 |
"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 |
Six simple, accurate, reproducible, and selective derivative spectrophotometric and chemometric methods have been developed. Lower concentrations of both ivermectin and closantel were not as effective in reducing larval growth.
Excerpt | Relevance | Reference |
---|---|---|
" Dose-response experiments showed that lower concentrations of both ivermectin and closantel were not as effective in reducing larval growth." | ( Reduced growth of Lucilia cuprina larvae fed serum from sheep treated with anthelmintics. East, IJ; Eisemann, CH; Kerlin, RL, 1992) | 0.51 |
" In the latter case, control was achieved by dosing either the ewes in the early part of the grazing season, or the lambs from June onwards." | ( Effectiveness of strategic anthelmintic dosing in controlling Haemonchus contortus infections in sheep in the United Kingdom. Hunt, KR; Quick, JM; Taylor, MA; Wilson, CA, 1991) | 0.28 |
" Independently of the dosing scheme and route of administration, the maximum daily intake by the consumer was always below the acceptable daily intake within 4 weeks after the last dose." | ( The metabolism and fate of closantel (Flukiver) in sheep and cattle. Heykants, J; Meuldermans, W; Michiels, M, 1987) | 0.57 |
" The rats were dosed orally with closantel at 20 mg kg-1 at two, four, six, eight and 10 weeks; the sheep at 10 mg kg-1 at eight, 10 and 12 weeks after artificial infection." | ( Flukicidal action of closantel against immature and mature Fasciola hepatica in experimentally infected rats and sheep. Deckers, W; Lauwers, H; Maes, L; Vanparijs, O, 1988) | 0.88 |
"Two controlled tests were conducted in equine foals and yearlings to determine the optimal oral dosage and the duration of activity of closantel for the prevention of Gasterophilus spp larval infections." | ( Activity of closantel in the prevention of Gasterophilus and Strongylus vulgaris larval infections in equine foals and yearlings. Guerrero, J; Michael, BF; Newcomb, K; Seibert, BP, 1985) | 0.85 |
" Repeated oral dosing was without effects up to 40 mg/kg in rats and dogs except for focal swelling of the epididymis in male rats at 40 mg/kg due to formation of spermatic granulomas." | ( Toxicological properties of closantel. Hérin, V; Marsboom, R; Van Cauteren, H; Vandenberghe, J; Vanparys, P, 1985) | 0.56 |
" In the 2nd and 3rd experiments, groups of 10 or 12 sheep were treated to confirm the efficacy of the previously determined optimal dosage of 15 mg/kg." | ( Activity of closantel against experimentally induced Fascioloides magna infection in sheep. Conboy, GA; Newcomb, KM; Schlotthauer, JC; Seibert, BP; Stromberg, BE, 1985) | 0.65 |
" While the unselected substrain appeared to show only slight increased resistance to the residual effect of closantel drenched at a dosage rate of 5 mg/kg, there was a dramatic increase in resistance after one selection." | ( Slight resistance to the residual effect of closantel in a field strain of Haemonchus contortus which showed an increased resistance after one selection in the laboratory. Alves, RM; Gerber, HM; Van Wyk, JA, 1982) | 0.74 |
" The largest dosage of closantel (12." | ( Pilot trials on the treatment of Dermatobia hominis infections in cattle with closantel. Chaia, G; Chiari, L; da Silva, DC; Guerrero, J, 1981) | 0.8 |
" Two groups were dosed with single therapeutic doses of closantel and tetramisole and the third group was given a low-level medication with albendazole through feed pellets for 30 days." | ( Comparative anthelmintic activity of strategic sustained low-level administration of albendazole in feed pellets compared to single doses of closantel and tetramisole against natural ovine parasitic gastroenteritis. Bhagwan, PS; Khan, FA; Sanyal, PK; Singh, D; Swarnkar, CP, 1999) | 0.75 |
"Six simple, accurate, reproducible, and selective derivative spectrophotometric and chemometric methods have been developed and validated for the determination of levamisole HCl (Lev) either alone or in combination with closantel sodium (Clo) in the pharmaceutical dosage form." | ( Comparative Study of Univariate Spectrophotometry and Multivariate Calibration for the Determination of Levamisole Hydrochloride and Closantel Sodium in a Binary Mixture. Abdel-Aziz, O; Ahmed, N; El Kosasy, AM; Hussien, EM, 2016) | 0.82 |
" This case alerts us about the destructive effect of this drug on humans even in low dosage which necessitates preventive efforts to reduce the chance of this morbid side effect." | ( Closantel; a veterinary drug with potential severe morbidity in humans. Abrishami, M; Inanlou, B; Mansouri, MR; Masarat, H; Mirshahi, A; Pakrah, AR; Soleimani, M; Tabatabaei, SA, 2016) | 1.88 |
" This report could be useful in anticipating the possibility of a further improvement based on a dose-response relationship." | ( Case report: restored vision after ocular Closantel intoxication and blindness. Khalili, MR; Zareei, A, 2021) | 0.89 |
Class | Description |
---|---|
nitrile | A compound having the structure RC#N; thus a C-substituted derivative of hydrocyanic acid, HC#N. In systematic nomenclature, the suffix nitrile denotes the triply bound #N atom, not the carbon atom attached to it. |
phenols | Organic aromatic compounds having one or more hydroxy groups attached to a benzene or other arene ring. |
organoiodine compound | An organoiodine compound is a compound containing at least one carbon-iodine bond. |
monocarboxylic acid amide | A carboxamide derived from a monocarboxylic acid. |
aromatic amide | An amide in which the amide linkage is bonded directly to an aromatic system. |
monochlorobenzenes | Any member of the class of chlorobenzenes containing a mono- or poly-substituted benzene ring in which only one substituent is chlorine. |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 17.7828 | 0.0040 | 23.8416 | 100.0000 | AID485290 |
Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 1.7783 | 0.0447 | 17.8581 | 100.0000 | AID485341 |
Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 50.1187 | 0.6310 | 35.7641 | 100.0000 | AID504339 |
Luciferase | Photinus pyralis (common eastern firefly) | Potency | 40.5334 | 0.0072 | 15.7588 | 89.3584 | AID624030 |
glp-1 receptor, partial | Homo sapiens (human) | Potency | 12.5893 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
phosphopantetheinyl transferase | Bacillus subtilis | Potency | 63.0957 | 0.1413 | 37.9142 | 100.0000 | AID1490 |
hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 21.3138 | 3.1890 | 29.8841 | 59.4836 | AID1224846 |
RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 29.8493 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
USP1 protein, partial | Homo sapiens (human) | Potency | 50.1187 | 0.0316 | 37.5844 | 354.8130 | AID504865; AID743255 |
TDP1 protein | Homo sapiens (human) | Potency | 21.4372 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
GLI family zinc finger 3 | Homo sapiens (human) | Potency | 23.8675 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
TSHR protein | Homo sapiens (human) | Potency | 2.1331 | 0.3381 | 19.0466 | 37.9330 | AID602292 |
AR protein | Homo sapiens (human) | Potency | 24.2903 | 0.0002 | 21.2231 | 8,912.5098 | AID743035; AID743042 |
Smad3 | Homo sapiens (human) | Potency | 7.0795 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
PINK1 | Homo sapiens (human) | Potency | 14.1254 | 2.8184 | 18.8959 | 44.6684 | AID624263 |
estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 21.1317 | 0.0006 | 57.9133 | 22,387.1992 | AID1259378 |
progesterone receptor | Homo sapiens (human) | Potency | 29.8493 | 0.0004 | 17.9460 | 75.1148 | AID1346795 |
regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 79.4328 | 0.5318 | 15.4358 | 37.6858 | AID504845 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 1.7377 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 31.0634 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159553; AID1159555 |
retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 7.4371 | 0.0008 | 17.5051 | 59.3239 | AID1159527; AID1159531 |
estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 30.2949 | 0.0015 | 30.6073 | 15,848.9004 | AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403 |
farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 24.2239 | 0.3758 | 27.4851 | 61.6524 | AID743217; AID743220 |
pregnane X nuclear receptor | Homo sapiens (human) | Potency | 33.4915 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982 |
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 22.3406 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID1259248; AID743069; AID743075; AID743078; AID743079; AID743080; AID743091 |
G | Vesicular stomatitis virus | Potency | 21.8761 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 10.9640 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
Parkin | Homo sapiens (human) | Potency | 14.1254 | 0.8199 | 14.8306 | 44.6684 | AID624263 |
bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 44.6684 | 0.7079 | 36.9043 | 89.1251 | AID504333 |
peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 20.8647 | 0.0010 | 24.5048 | 61.6448 | AID743212; AID743215 |
vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 33.4889 | 0.0237 | 23.2282 | 63.5986 | AID743222 |
IDH1 | Homo sapiens (human) | Potency | 20.5962 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 8.3186 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 26.6032 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 8.4852 | 19.7391 | 45.9784 | 64.9432 | AID1159509 |
nuclear receptor subfamily 1, group I, member 2 | Rattus norvegicus (Norway rat) | Potency | 35.4813 | 0.1000 | 9.1916 | 31.6228 | AID1346983 |
Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 25.1189 | 0.5406 | 17.6392 | 96.1227 | AID2528 |
vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 25.1189 | 0.3548 | 28.0659 | 89.1251 | AID504847 |
thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 57.7315 | 0.0100 | 39.5371 | 1,122.0200 | AID1469; AID1479 |
nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 20.5962 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
transcriptional regulator ERG isoform 3 | Homo sapiens (human) | Potency | 11.2202 | 0.7943 | 21.2757 | 50.1187 | AID624246 |
thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 23.0868 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
heat shock protein beta-1 | Homo sapiens (human) | Potency | 4.2160 | 0.0420 | 27.3789 | 61.6448 | AID743210 |
flap endonuclease 1 | Homo sapiens (human) | Potency | 28.1838 | 0.1337 | 25.4129 | 89.1251 | AID588795 |
serine/threonine-protein kinase PLK1 | Homo sapiens (human) | Potency | 18.8876 | 0.1683 | 16.4040 | 67.0158 | AID720504 |
histone-lysine N-methyltransferase 2A isoform 2 precursor | Homo sapiens (human) | Potency | 89.1251 | 0.0103 | 23.8567 | 63.0957 | AID2662 |
nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 15.4086 | 0.0006 | 27.2152 | 1,122.0200 | AID743202; AID743219 |
DNA polymerase eta isoform 1 | Homo sapiens (human) | Potency | 50.1187 | 0.1000 | 28.9256 | 213.3130 | AID588591 |
DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 15.8489 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 22.3872 | 0.0079 | 8.2332 | 1,122.0200 | AID2546 |
lethal(3)malignant brain tumor-like protein 1 isoform I | Homo sapiens (human) | Potency | 39.8107 | 0.0752 | 15.2253 | 39.8107 | AID485360 |
geminin | Homo sapiens (human) | Potency | 14.7328 | 0.0046 | 11.3741 | 33.4983 | AID624296; AID624297 |
DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 89.1251 | 0.0316 | 22.3146 | 100.0000 | AID588579 |
peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 40.5334 | 0.0056 | 12.3677 | 36.1254 | AID624032 |
histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 14.2528 | 0.2512 | 15.8432 | 39.8107 | AID504327; AID588347 |
Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 23.7101 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) | Potency | 50.1187 | 6.3096 | 60.2008 | 112.2020 | AID720709 |
Interferon beta | Homo sapiens (human) | Potency | 21.8761 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 21.8761 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 8.4199 | 0.0023 | 19.5956 | 74.0614 | AID651631; AID720552 |
Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 23.7101 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 25.1772 | 0.0096 | 10.5250 | 35.4813 | AID1479145; AID1479148 |
Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 28.1838 | 1.9953 | 25.5327 | 50.1187 | AID624288 |
Rap guanine nucleotide exchange factor 4 | Homo sapiens (human) | Potency | 50.1187 | 3.9811 | 46.7448 | 112.2020 | AID720708 |
Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 21.8761 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 26.6032 | 0.0119 | 17.9420 | 71.5630 | AID651632 |
Ataxin-2 | Homo sapiens (human) | Potency | 26.6032 | 0.0119 | 12.2221 | 68.7989 | AID651632 |
cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 21.8761 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
[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) |
---|---|---|---|---|---|---|---|
SUMO-1 | Homo sapiens (human) | IC50 (µMol) | 36.5950 | 0.6470 | 7.4947 | 15.9000 | AID624382; AID624383 |
hexokinase | Trypanosoma brucei brucei TREU927 | IC50 (µMol) | 25.0000 | 0.2008 | 4.6024 | 22.3780 | AID2230 |
Solute carrier family 22 member 1 | Homo sapiens (human) | IC50 (µMol) | 3.0000 | 0.2100 | 5.5537 | 10.0000 | AID1442001 |
Long-chain-fatty-acid--AMP ligase FadD32 | Mycobacterium tuberculosis H37Rv | IC50 (µMol) | 7.7000 | 7.7000 | 7.7000 | 7.7000 | AID1854972 |
Epidermal growth factor receptor | Homo sapiens (human) | IC50 (µMol) | 0.5640 | 0.0000 | 0.5369 | 10.0000 | AID625184 |
Receptor tyrosine-protein kinase erbB-2 | Homo sapiens (human) | IC50 (µMol) | 2.4680 | 0.0001 | 0.5453 | 10.0000 | AID625186 |
Tyrosine-protein kinase Lck | Homo sapiens (human) | IC50 (µMol) | 1.2490 | 0.0002 | 1.3173 | 10.0000 | AID625187 |
Tyrosine-protein kinase Fyn | Homo sapiens (human) | IC50 (µMol) | 0.9390 | 0.0002 | 1.6789 | 8.6800 | AID625185 |
Sporulation initiation phosphotransferase F | Bacillus subtilis subsp. subtilis str. 168 | IC50 (µMol) | 3.8000 | 3.8000 | 3.8000 | 3.8000 | AID40629 |
Neutrophil elastase | Homo sapiens (human) | IC50 (µMol) | 25.0000 | 0.0063 | 2.0734 | 22.3780 | AID2230 |
Cytochrome P450 3A4 | Homo sapiens (human) | IC50 (µMol) | 5.0000 | 0.0001 | 1.7536 | 10.0000 | AID625251 |
Adenosine receptor A3 | Homo sapiens (human) | IC50 (µMol) | 0.0960 | 0.0000 | 1.8940 | 8.5470 | AID625196 |
Adenosine receptor A3 | Homo sapiens (human) | Ki | 0.0540 | 0.0000 | 0.9306 | 10.0000 | AID625196 |
60 kDa heat shock protein, mitochondrial | Homo sapiens (human) | IC50 (µMol) | 2.6500 | 0.1700 | 4.5590 | 10.0000 | AID1423480; AID1594139 |
Cytochrome P450 2C9 | Homo sapiens (human) | IC50 (µMol) | 2.0000 | 0.0000 | 2.8005 | 10.0000 | AID625248 |
Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0960 | 0.0002 | 1.8742 | 10.0000 | AID625196 |
Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.0540 | 0.0001 | 0.9490 | 10.0000 | AID625196 |
Sporulation kinase A | Bacillus subtilis subsp. subtilis str. 168 | IC50 (µMol) | 3.8000 | 3.8000 | 3.8000 | 3.8000 | AID40629 |
Alpha-2B adrenergic receptor | Homo sapiens (human) | IC50 (µMol) | 1.8000 | 0.0000 | 1.2380 | 8.1590 | AID625202 |
Alpha-2B adrenergic receptor | Homo sapiens (human) | Ki | 0.8219 | 0.0002 | 0.7257 | 10.0000 | AID625202 |
Alpha-2C adrenergic receptor | Homo sapiens (human) | IC50 (µMol) | 7.1000 | 0.0000 | 1.4725 | 7.8980 | AID625203 |
Alpha-2C adrenergic receptor | Homo sapiens (human) | Ki | 1.0000 | 0.0003 | 0.4834 | 10.0000 | AID625203 |
Acetylcholinesterase | Homo sapiens (human) | IC50 (µMol) | 2.9510 | 0.0000 | 0.9332 | 10.0000 | AID625193 |
Thromboxane-A synthase | Homo sapiens (human) | IC50 (µMol) | 0.0640 | 0.0009 | 1.2304 | 10.0000 | AID625229 |
Mitogen-activated protein kinase 1 | Homo sapiens (human) | IC50 (µMol) | 1.4280 | 0.0003 | 1.6878 | 9.2000 | AID625181 |
Prostaglandin G/H synthase 2 | Homo sapiens (human) | IC50 (µMol) | 1.8390 | 0.0001 | 0.9950 | 10.0000 | AID625244 |
Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0960 | 0.0000 | 1.8194 | 10.0000 | AID625196 |
Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.0540 | 0.0000 | 0.9650 | 10.0000 | AID625196 |
10 kDa heat shock protein, mitochondrial | Homo sapiens (human) | IC50 (µMol) | 2.6500 | 0.1700 | 4.5590 | 10.0000 | AID1423480; AID1594139 |
Sodium-dependent dopamine transporter | Homo sapiens (human) | IC50 (µMol) | 4.8000 | 0.0007 | 1.8419 | 46.0000 | AID625256 |
Sodium-dependent dopamine transporter | Homo sapiens (human) | Ki | 3.8000 | 0.0002 | 1.1115 | 8.0280 | AID625256 |
Mitogen-activated protein kinase 14 | Homo sapiens (human) | IC50 (µMol) | 0.6560 | 0.0001 | 0.7266 | 7.8000 | AID625182 |
Thiosulfate sulfurtransferase | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.0600 | 3.9631 | 9.7000 | AID1423472; AID1594135 |
Chitinase | Onchocerca volvulus | IC50 (µMol) | 1.6000 | 0.3400 | 1.1800 | 1.6000 | AID1158751; AID606510 |
Chitinase | Onchocerca volvulus | Ki | 0.4690 | 0.1300 | 0.3560 | 0.4700 | AID1158753; AID606510 |
60 kDa chaperonin | Escherichia coli | IC50 (µMol) | 1.9750 | 0.0390 | 3.5552 | 9.8000 | AID1423469; AID1423470; AID1594140; AID1594141 |
10 kDa chaperonin | Escherichia coli | IC50 (µMol) | 1.9750 | 0.0390 | 3.5552 | 9.8000 | AID1423469; AID1423470; AID1594140; AID1594141 |
NAD-dependent protein deacylase sirtuin-5, mitochondrial | Homo sapiens (human) | IC50 (µMol) | 2.7000 | 0.1000 | 3.3800 | 6.6000 | AID1742983 |
[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) |
---|---|---|---|---|---|---|---|
Chain A, BCL-2-RELATED PROTEIN A1 | Homo sapiens (human) | EC50 (µMol) | 350.0000 | 8.0570 | 121.1218 | 338.0000 | AID2765 |
streptokinase A precursor | Streptococcus pyogenes M1 GAS | EC50 (µMol) | 0.0820 | 0.0600 | 8.9128 | 130.5170 | AID1902 |
bcl-2-like protein 11 isoform 1 | Homo sapiens (human) | EC50 (µMol) | 350.0000 | 8.0570 | 121.1218 | 338.0000 | AID2765 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1423472 | Inhibition of refolded rhodanese (unknown origin) preincubated with Escherichia coli GroEL/GroES for 60 mins in absence of compound followed by compound addition by spectrometric analysis | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
AID1594137 | Inhibition of ATPase activity of Escherichia coli GroEL expressed in Escherichia coliDH5alpha incubated for 60 mins using ATP by spectrometric analysis | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9 | HSP60/10 chaperonin systems are inhibited by a variety of approved drugs, natural products, and known bioactive molecules. |
AID1594145 | Inhibition of Escherichia coli GroEL expressed in Escherichia coli DH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured rhodanese refolding by measuring rhodanese enzyme activity | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9 | HSP60/10 chaperonin systems are inhibited by a variety of approved drugs, natural products, and known bioactive molecules. |
AID1423481 | Cytotoxicity against human THLE3 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue reporter assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
AID606510 | Inhibition of Onchocerca volvulus L3 larvae chitinase using 4-methylumbelliferyl-N,N',N''-beta-chitotrioside as a profluorescent substrate after 10 mins by fluorometric analysis | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Design, synthesis, and biological activities of closantel analogues: structural promiscuity and its impact on Onchocerca volvulus. |
AID1423470 | Inhibition of Escherichia coli GroEL expressed in Escherichia coli DH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured rhodanese refolding after 45 mins by spectrometric analysis | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
AID1594134 | Inhibition of native soluble pig heart MDH assessed as reduction in MDH enzyme activity using sodium mesoxalate as substrate and NADH by malachite green dye based spectrometric analysis | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9 | HSP60/10 chaperonin systems are inhibited by a variety of approved drugs, natural products, and known bioactive molecules. |
AID66747 | Percentage of specific activity relative to untreated control at a concentration allowing 80% growth. | 1998 | Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16 | Substituted salicylanilides as inhibitors of two-component regulatory systems in bacteria. |
AID1423471 | Antibacterial activity against Staphylococcus aureus ATCC 25923 after 6 to 8 hrs by bacterial proliferation assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
AID1423479 | Antibacterial activity against Enterobacter cloacae subsp. cloacae ATCC 13047 after 24 hrs by bacterial proliferation assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
AID606515 | Antiparasitic activity against Onchocerca volvulus assessed as inhibition of L3 to L4 larval molting at 100 uM after 6 days by using inverted microscopic analysis | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Design, synthesis, and biological activities of closantel analogues: structural promiscuity and its impact on Onchocerca volvulus. |
AID66750 | Activity of the VanS/VanR TCS in Enterococcus faecalis OC3364; Not Tested | 1998 | Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16 | Substituted salicylanilides as inhibitors of two-component regulatory systems in bacteria. |
AID1158766 | Toxicity in Caenorhabditis elegans | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
AID1423475 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC BAA-44 after 6 to 8 hrs by bacterial proliferation assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
AID1423478 | Antibacterial activity against Pseudomonas aeruginosa ATCC 10145 after 24 hrs by bacterial proliferation assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
AID1158761 | Drug metabolism in Caenorhabditis elegans assessed as 5-iodo closantel formation after 12 hrs by LC/MS analysis | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
AID1594140 | Inhibition of Escherichia coli GroEL expressed in Escherichia coli DH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured rhodanese refolding by measuring rhodanese enzyme activity | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9 | HSP60/10 chaperonin systems are inhibited by a variety of approved drugs, natural products, and known bioactive molecules. |
AID1423473 | Inhibition of refolded MDH (unknown origin) preincubated with Escherichia coli GroEL/GroES for 45 mins in absence of compound followed by compound addition and measured for 20 to 35 mins by spectrometric analysis | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
AID741324 | Induction of internalization of Frizzled1-GFP (unknown origin) expressed in human U2OS cells at 12.5 uM after 6 hrs by confocal microscopy | 2013 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7 | Small molecule modulators of Wnt/β-catenin signaling. |
AID195261 | Uncoupler concentration that reduced the respiratory control index by 50% of coupled rat liver mitochondria | 1998 | Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7 | Synthesis and endectocidal activity of novel 1-(arylsulfonyl)-1-[(trifluoromethyl)sulfonyl]methane derivatives. |
AID606520 | Antiparasitic activity against Onchocerca ochengi assessed as effect on microfilarial mobility at 10 ug/ml measured every 24 hrs for 120 hrs by inverted microscopic analysis | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Design, synthesis, and biological activities of closantel analogues: structural promiscuity and its impact on Onchocerca volvulus. |
AID1423482 | Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue reporter assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
AID68415 | Minimum inhibitory activity against Enterococcus faecium OC3312. | 1998 | Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16 | Substituted salicylanilides as inhibitors of two-component regulatory systems in bacteria. |
AID1594144 | Inhibition of Escherichia coli GroEL expressed in Escherichia coliDH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured soluble pig heart MDH refolding by measuring MDH enzyme acti | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9 | HSP60/10 chaperonin systems are inhibited by a variety of approved drugs, natural products, and known bioactive molecules. |
AID1423480 | Inhibition of human N-terminal octa-His-tagged HSP60 expressed in Escherichia coli Rosetta(DE3) pLysS/human HSP10 expressed in Escherichia coli Rosetta(DE3) assessed as reduction in HSP60/HSP10-mediated denatured MDH refolding after 40 to 60 mins by spect | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
AID1594141 | Inhibition of Escherichia coli GroEL expressed in Escherichia coliDH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured soluble pig heart MDH refolding by measuring MDH enzyme acti | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9 | HSP60/10 chaperonin systems are inhibited by a variety of approved drugs, natural products, and known bioactive molecules. |
AID1423474 | Antibacterial activity against Enterococcus faecium ATCC 19434 after 24 hrs by bacterial proliferation assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
AID1158760 | Drug metabolism in Caenorhabditis elegans assessed as 3-iodo closantel formation after 12 hrs by LC/MS analysis | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
AID1158763 | Drug metabolism in Caenorhabditis elegans assessed as glycosylated metabolite formation after 12 hrs by LC/MS analysis | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
AID1423476 | Antibacterial activity against Klebsiella pneumoniae ATCC 13883 after 6 to 8 hrs by bacterial proliferation assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
AID1158753 | Competitive inhibition of Onchocerca volvulus L3 larvae chitinase using 20 uM 4-methylumbelliferyl-N,N',N''-beta-chitotrioside as substrate after 10 mins by microplate reader analysis | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
AID1442001 | Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1). |
AID1158751 | Inhibition of Onchocerca volvulus L3 larvae chitinase using 20 uM 4-methylumbelliferyl-N,N',N''-beta-chitotrioside as substrate after 10 mins by microplate reader analysis | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
AID1158757 | Protonophoric activity in human HEK293T/17 cells assessed as mitochondrial membrane depolarization at 50 uM for 30 mins by TMRE dye based fluorescence spectrometry | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
AID207670 | Minimum inhibitory activity against Staphylococcus aureus ATCC 29213. | 1998 | Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16 | Substituted salicylanilides as inhibitors of two-component regulatory systems in bacteria. |
AID1423469 | Inhibition of Escherichia coli GroEL expressed in Escherichia coli DH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured MDH refolding after 20 to 40 mins by spectrometric analysis | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
AID1742983 | Inhibition of SIRT5 (unknown origin) | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Identification of the subtype-selective Sirt5 inhibitor balsalazide through systematic SAR analysis and rationalization via theoretical investigations. |
AID1158762 | Drug metabolism in Caenorhabditis elegans assessed as sulfated metabolite formation after 12 hrs by LC/MS analysis | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
AID1854973 | Binding affinity to Mycobacterium tuberculosis FAAL32 assessed as change in melting temperature at 5 uM by NanoDSF assay | 2022 | Bioorganic & medicinal chemistry, 10-01, Volume: 71 | Drug screening approach against mycobacterial fatty acyl-AMP ligase FAAL32 renews the interest of the salicylanilide pharmacophore in the fight against tuberculosis. |
AID1423477 | Antibacterial activity against Acinetobacter baumannii ATCC 19606 after 24 hrs by bacterial proliferation assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
AID1158758 | Protonophoric activity in human HEK293T/17 cells assessed as mitochondrial membrane depolarization at 50 uM for 30 mins by TMRE dye based flow cytometry | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
AID1854972 | Inhibition of Mycobacterium tuberculosis FAAL32 using AMPC12 as substrate incubated for 50 mins and measured by spectrophotometric assay | 2022 | Bioorganic & medicinal chemistry, 10-01, Volume: 71 | Drug screening approach against mycobacterial fatty acyl-AMP ligase FAAL32 renews the interest of the salicylanilide pharmacophore in the fight against tuberculosis. |
AID606516 | Antiparasitic activity against Onchocerca volvulus assessed as larval toxicity at 100 uM after 6 days by using inverted microscopic analysis | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Design, synthesis, and biological activities of closantel analogues: structural promiscuity and its impact on Onchocerca volvulus. |
AID1594139 | Inhibition of human N-terminal octa-His-tagged HSP60 expressed in Escherichia coli Rosetta(DE3) pLysS/human HSP10 expressed in Escherichia coli Rosetta(DE3) assessed as reduction in HSP60/HSP10-mediated denatured MDH refolding by measuring MDH enzyme acti | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9 | HSP60/10 chaperonin systems are inhibited by a variety of approved drugs, natural products, and known bioactive molecules. |
AID1158759 | Drug accumulation in Caenorhabditis elegans at 10 uM after 6 hrs by LC-MS analysis | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
AID1854971 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv incubated for 24 hrs and measured by MTT assay | 2022 | Bioorganic & medicinal chemistry, 10-01, Volume: 71 | Drug screening approach against mycobacterial fatty acyl-AMP ligase FAAL32 renews the interest of the salicylanilide pharmacophore in the fight against tuberculosis. |
AID207672 | Minimum inhibitory activity against methicillin resistant Staphylococcus aureus (MRSA) OC2089. | 1998 | Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16 | Substituted salicylanilides as inhibitors of two-component regulatory systems in bacteria. |
AID40629 | Inhibition of autophosphorylation of the two-component signal transduction system kinase was measured using the KinA/Spo0F regulatory system of Bacillus subtilis. | 1998 | Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16 | Substituted salicylanilides as inhibitors of two-component regulatory systems in bacteria. |
AID1594135 | Inhibition of native rhodanese (unknown origin) assessed as reduction in rhodanese enzyme activity after 45 mins by Fe(SCN)3 dye based spectrometric analysis | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9 | HSP60/10 chaperonin systems are inhibited by a variety of approved drugs, natural products, and known bioactive molecules. |
AID293136 | Parasiticidal activity against Haemonchus contortus McMaster | 2007 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4 | Discovery of (Z)-2-phenyl-3-(1H-pyrrol-2-yl)acrylonitrile derivatives active against Haemonchus contortus and Ctenocephalides felis (cat flea). |
AID67728 | Minimum inhibitory activity against Enterococcus faecalis OC3041. | 1998 | Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16 | Substituted salicylanilides as inhibitors of two-component regulatory systems in bacteria. |
AID606519 | Antiparasitic activity against Onchocerca ochengi assessed as effect on microfilarial mobility at 5 ug/ml measured every 24 hrs for 120 hrs by inverted microscopic analysis | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Design, synthesis, and biological activities of closantel analogues: structural promiscuity and its impact on Onchocerca volvulus. |
AID1158764 | Drug metabolism in Caenorhabditis elegans assessed as glucordinated metabolite formation after 12 hrs by LC/MS analysis | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. 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. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. 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. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. 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. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
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. |
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. |
AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 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. |
AID1347153 | Confirmatory 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. |
AID1347163 | 384 well plate NINDS AMC confirmatory 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. |
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. |
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. |
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. |
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. |
AID1347167 | Vero cells viability 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. |
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. |
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. |
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. |
AID1347149 | Furin counterscreen 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. |
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. |
AID1347157 | Confirmatory screen GU Rhodamine qHTS for Zika virus inhibitors qHTS | 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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1347152 | Confirmatory screen NINDS 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. |
AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
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. |
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. |
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. |
AID1347161 | Confirmatory 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. |
AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
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. |
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. |
AID1347169 | Tertiary RLuc qRT-PCR qHTS assay 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. |
AID1347168 | HepG2 cells viability 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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 30 (14.78) | 18.7374 |
1990's | 60 (29.56) | 18.2507 |
2000's | 24 (11.82) | 29.6817 |
2010's | 65 (32.02) | 24.3611 |
2020's | 24 (11.82) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (54.22) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 18 (8.65%) | 5.53% |
Reviews | 3 (1.44%) | 6.00% |
Case Studies | 10 (4.81%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 177 (85.10%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |