Page last updated: 2024-12-11

selamectin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

selamectin: a broad-spectrum endectocide; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9578507
CHEMBL ID1908325
CHEBI ID177562
SCHEMBL ID120105
MeSH IDM0371163
PubMed CID122198140
MeSH IDM0371163

Synonyms (59)

Synonym
CHEBI:177562
(1r,4s,5's,6r,6's,8r,10e,12s,13s,14e,16e,20r,21z,24s)-6'-cyclohexyl-24-hydroxy-21-hydroxyimino-12-[(2r,4s,5s,6s)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetrae
D05813
selamectin (usan/inn)
NCGC00095066-01
25-cyclohexyl-25-de(1-methylpropyl)-5-deoxy-22 23-dihydro-5-(hydroxyimino)-avermectin b1 monosaccharide
(2ae,4e,5's,6s,6's,7s,8e,11r,13r,15s,17ar,20ar,20bs)-6'-cyclohexyl-7-((2,6-dideoxy-3-o-methyl-alpha-l-arabino-hexopyranosyl)oxy)-3',4',5',6,6',7,10,11,14,15,20a,20b-dodecahydro-20b-hydroxy-5',6,8,19-tetramethylspiro(11,15-methano-2h,13h,17h-furo(4,3,2-pq)
25-cyclohexyl-4'-o-de(2,6-dideoxy-3-o-methyl-alpha-l-arabino-hexopyranosyl)-5-demethoxy-25-de(1-methylpropyl)-22,23-dihydro-5-(hydroxyimino)-avermectin a1a
uk-124,114
revolution (antibiotic)
a2669owx9n ,
unii-a2669owx9n
selamectin [usan:inn:ban]
nsc 758615
avermectin a1a, 25-cyclohexyl-4'-o-de(2,6-dideoxy-3-o-methyl-alpha-l-arabino-hexopyranosyl)-5-demethoxy-25-de(1-methylpropyl)-22,23-dihydro-5-(hydroxyimino)-, (5z)-
uk 124114
revolution
tox21_111408
cas-165108-07-6
dtxcid4025903
dtxsid6045903 ,
uk-124114
CHEMBL1908325
selamectin [usp-rs]
selamectin component of stronghold
selamectin [green book]
stronghold component selamectin
selamectin [mart.]
selamectin [mi]
avermectin a1a, 25-cyclohexyl-4'-o-de(2,6-dideoxy-3-o-methyl-.alpha.-l-arabino-hexopyranosyl)-5-demethoxy-25-de(1-methylpropyl)-22,23-dihydro-5(hydroxyimino)-, (5z)-
selamectin [usan]
selamectin [ema epar veterinary]
stronghold plus component selamectin
avermectin a1a, 25-cyclohexyl-4'-o-de(2,6-dideoxy-3-o-methyl-.alpha.-l-arabino-hexopyranosyl)-5-demethoxy-25-de(1-methylpropyl)-22,23-dihydro-5-(hydroxyimino)-
selamectin component of stronghold plus
selamectin [usp monograph]
selamectin [inn]
SCHEMBL120105
CS-7778
AKOS026749796
J-014423
mfcd31621085
HY-107212
DB11459
EX-A3581
bdbm50588192
selarid
selamectine
revolt
senergy
selamectin (usp monograph)
selaspot
avermectin a1a, 25-cyclohexyl-4'-o-de(2,6-dideoxy-3-o-methyl-alpha-l-arabino-hexopyranosyl)-5-demethoxy-25-de(1-methylpropyl)-22,23-dihydro-5(hydroxyimino)-, (5z)-
selamectin (ema epar veterinary)
selamectin (usp-rs)
selamectina
selamectinum
selamectin (mart.)
selamectin

Research Excerpts

Toxicity

Selamectin was shown to be safe and highly effective in the control of naturally acquired flea infestations on dogs and cats presented as veterinary patients in Europe. Similarly, selamectin had no adverse effects on reproduction in adult male and female dogs.

ExcerptReferenceRelevance
" Selamectin was shown to be safe and highly effective in the control of naturally acquired flea infestations on dogs and cats presented as veterinary patients in Europe."( Efficacy and safety of selamectin against fleas on dogs and cats presented as veterinary patients in Europe.
Benchaoui, HA; Clemence, RG; Clements, PJ; Jernigan, AD; Jones, RL; Rowan, TG; Shanks, DJ; Smith, DG; Sture, GH; Watson, P, 2000
)
0.31
" There were no serious adverse events."( Efficacy and safety of selamectin against fleas and heartworms in dogs and cats presented as veterinary patients in North America.
Boy, MG; Jernigan, AD; Novotny, MJ; Rowan, TG; Six, RH; Smothers, CD; Thomas, CA, 2000
)
0.31
" Thus, selamectin was safe and effective against ear mites in dogs and cats and sarcoptic mange in dogs when used in field (veterinary patient) studies in dogs and cats of a wide variety of ages and breeds."( Efficacy and safety of selamectin against Sarcoptes scabiei on dogs and Otodectes cynotis on dogs and cats presented as veterinary patients.
Behan, S; Benchaoui, HA; Boy, MG; Clemence, RG; Clements, PJ; Jernigan, AD; Rowan, TG; Six, RH; Thomas, CA; Watson, P, 2000
)
0.31
" These studies have shown that monthly topical administration of selamectin is safe and highly effective in the treatment of naturally acquired ascarid and hookworm infections in cats."( Efficacy and safety of selamectin against gastrointestinal nematodes in cats presented as veterinary patients.
Benchaoui, HA; Boy, MG; Clemence, RG; Jernigan, AD; Rowan, TG; Six, RH; Smith, DG; Sture, GH; Thomas, CA; Watson, P, 2000
)
0.31
" Similarly, selamectin had no adverse effects on reproduction in adult male and female dogs."( Safety of selamectin in dogs.
Ehrhart, JC; Evans, EI; Godin, CS; Jernigan, AD; Krautmann, MJ; McCall, JW; Novotny, MJ; Rowan, TG; Sun, F, 2000
)
0.31
" Similarly, selamectin had no adverse effect on reproduction in adult male and female cats."( Safety of selamectin in cats.
De Keulenaer, K; Evans, EI; Godin, CS; Jernigan, AD; Krautmann, MJ; McCall, JW; Novotny, MJ; Rowan, TG; Wang, C, 2000
)
0.31
" No adverse reactions associated with selamectin treatment were observed."( Efficacy and safety of topical administration of selamectin for treatment of ear mite infestation in rabbits.
Hair, JA; McTier, TL; Thompson, L; Walstrom, DJ, 2003
)
0.32
" No adverse events attributable to treatment with the test articles were observed during the study."( Safety of imidacloprid plus moxidectin topical solution applied to cats heavily infected with adult heartworms (Dirofilaria immitis).
Arther, RG; Atkins, C; Ciszewski, DK; Davis, WL; Ensley, SM; Settje, TL, 2005
)
0.33
" Only three mild, possibly drug-related adverse reactions were observed among alI treated animals (two in the imidacloprid/moxidectin group, one in the selamectin group)."( Efficacy and safety of imidacloprid 10% plus moxidectin 2.5% spot-on in the treatment of sarcoptic mange and otoacariosis in dogs: results af a European field study.
Dumont, P; Heine, J; Hellmann, K; Krieger, K, 2005
)
0.33
"To determine pharmacokinetics, efficacy, and adverse effects of topically administered selamectin in flea-infested rabbits."( Pharmacokinetics, efficacy, and adverse effects of selamectin following topical administration in flea-infested rabbits.
Carpenter, JW; Dryden, MW; Kukanich, B, 2012
)
0.38
" No adverse effects were detected."( Pharmacokinetics, efficacy, and adverse effects of selamectin following topical administration in flea-infested rabbits.
Carpenter, JW; Dryden, MW; Kukanich, B, 2012
)
0.38
" No adverse reactions were observed in any of the treated animals."( Comparison of efficacy, safety, and convenience of selamectin versus ivermectin for treatment of Trixacarus caviae mange in pet guinea pigs (Cavia porcellus).
Bdolah-Abram, T; Eshar, D, 2012
)
0.38
"The most common adverse event was vomiting (14."( Safety and efficacy of spinosad chewable tablets for treatment of flea infestations of cats.
Kee, EA; Paarlberg, TE; Snyder, DE; Trout, CM; Wiseman, S, 2013
)
0.39
" No serious adverse events associated with either product were observed during the study."( Clinical evaluation of the safety and efficacy of 10% imidacloprid + 2.5% moxidectin topical solution for the treatment of ear mite (Otodectes cynotis) infestations in dogs.
Arther, RG; Davis, WL; Jacobsen, JA; Lewis, VA; Settje, TL, 2015
)
0.42
" There were no treatment-related adverse events in either study."( Efficacy and safety of a new topical formulation containing selamectin and sarolaner in the prevention of heartworm disease and the treatment of roundworm infection in cats presented as veterinary patients in Japan.
Fujii, T; Maeder, S; Naito, M; Rugg, D; Yonetake, W, 2019
)
0.51
"Drug-associated adverse events cause approximately 30 billion dollars a year of added health care expense, along with negative health outcomes including patient death."( Making Sense of Pharmacovigilance and Drug Adverse Event Reporting: Comparative Similarity Association Analysis Using AI Machine Learning Algorithms in Dogs and Cats.
Amini, M; Goligerdian, A; Jaberi-Douraki, M; Mazloom, R; Riviere, J; Staley, J; Wyckoff, GJ; Xu, X, 2019
)
0.51
"0 mg/kg sarolaner was safe and highly effective against natural infestations of fleas under a range of geographical conditions, representative of both tropical and subtropical regions of Australia."( Safety and efficacy of a new spot-on formulation of selamectin plus sarolaner in the treatment and control of naturally occurring flea infestations in cats presented as veterinary patients in Australia.
Bruellke, N; Graham, K; Hodge, A; Packianathan, R; Pittorino, M, 2020
)
0.56

Pharmacokinetics

There were no selamectin-related adverse effects and no sex differences in pharmacokinetic parameters. Mean terminal half-life and maximum plasma concentrations of selamECTin were 0.

ExcerptReferenceRelevance
" There were no selamectin-related adverse effects and no sex differences in pharmacokinetic parameters."( Pharmacokinetics of selamectin following intravenous, oral and topical administration in cats and dogs.
Castledine, J; Jernigan, AD; Rowan, TG; Sarasola, P; Smith, DG; Walker, DK, 2002
)
0.31
"Some pharmacokinetic parameters of selamectin were determined in male (n = 5) and female (n = 5) Beagle dogs following a topical application at a dose rate of 6 mg/kg."( Pharmacokinetics of selamectin in dogs after topical application.
Alvinerie, M; Cadiergues, MC; Derlon, AL; Dupuy, J; Franc, M; Sutra, JF, 2004
)
0.32
" Pharmacokinetic parameters were determined."( Pharmacokinetics, efficacy, and adverse effects of selamectin following topical administration in flea-infested rabbits.
Carpenter, JW; Dryden, MW; Kukanich, B, 2012
)
0.38
"Twenty-one healthy helmeted guineafowl (Numida meleagris) housed at the Oklahoma City Zoo were used to evaluate the pharmacokinetic parameters of topical selamectin."( Pharmacokinetics of selamectin in helmeted guineafowl (Numida meleagris) after topical administration.
Cole, G; D'Agostino, J; Hahn, A; Kukanich, B, 2014
)
0.4

Bioavailability

ExcerptReferenceRelevance
"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

Dosage Studied

P purpose-bred shorthaired cats and Beagles were randomly allocated to treatment with either selamectin at a minimum dosage of 6mgkg(-1) or the negative control treatment (vehicle only) Selamectin was applied topically in a single spot to the skin on each animal's back at the base of the neck.

ExcerptRelevanceReference
" One treatment consisted of the inert formulation ingredients (vehicle) administered as a negative control, and the other three treatments consisted of a single topical dosage of 3, 6, or 9mgkg(-1) of selamectin."( Dose selection of selamectin for efficacy against adult fleas (Ctenocephalides felis felis) on dogs and cats.
Bishop, BF; Evans, NA; Giles, CJ; Gration, KA; Holbert, MS; Jernigan, AD; McTier, TL; Rowan, TG; Smothers, CD, 2000
)
0.31
" Animals were randomly allocated to treatment with either selamectin at a minimum dosage of 6mgkg(-1) in the commercial formulation or one of two negative-controls (0."( Evaluation of the effects of selamectin against adult and immature stages of fleas (Ctenocephalides felis felis) on dogs and cats.
Blagburn, BL; Holbert, MS; Jernigan, AD; Jones, RL; McTier, TL; Murphy, MG; Rowan, TG; Shanks, DJ; Smith, DG; Wang, C, 2000
)
0.31
" Purpose-bred shorthaired cats and Beagles were randomly allocated to treatment with either selamectin at a minimum dosage of 6mgkg(-1) of body weight in the commercial formulation or the negative control treatment (vehicle only), and housed in controlled simulated home environments capable of supporting the flea life cycle."( Efficacy of selamectin in the treatment and prevention of flea (Ctenocephalides felis felis) infestations on dogs and cats housed in simulated home environments.
Jernigan, AD; Jones, RL; Murphy, MG; Rowan, TG; Shanks, DJ; Smith, DG; Watson, P, 2000
)
0.31
" Animals were allocated randomly in a 2:1 ratio to one of two treatments: either selamectin alone at a minimum dosage of 6mgkg(-1) or fenthion at recommended dose rates."( Efficacy and safety of selamectin against fleas on dogs and cats presented as veterinary patients in Europe.
Benchaoui, HA; Clemence, RG; Clements, PJ; Jernigan, AD; Jones, RL; Rowan, TG; Shanks, DJ; Smith, DG; Sture, GH; Watson, P, 2000
)
0.31
" In all studies selamectin was applied topically, once per month, in unit doses providing a minimum dosage of 6mgkg(-1)."( Efficacy and safety of selamectin against fleas and heartworms in dogs and cats presented as veterinary patients in North America.
Boy, MG; Jernigan, AD; Novotny, MJ; Rowan, TG; Six, RH; Smothers, CD; Thomas, CA, 2000
)
0.31
" Selamectin was applied topically in a single spot to the skin on each animal's back at the base of the neck in front of the scapulae as a unit dose that provided at least the minimum recommended dosage of 6mgkg(-1) (range, 6-12mgkg(-1))."( Efficacy of selamectin in the prevention of adult heartworm (Dirofilaria immitis) infection in dogs in northern Italy.
Clemence, RG; Genchi, C; Jernigan, AD; Rowan, TG; Sarasola, P; Shanks, DJ; Smith, DG, 2000
)
0.31
" Cats were treated topically with unit doses providing a minimum dosage of 6mgkg(-1) selamectin at 30 days PI."( Prevention of experimentally induced heartworm (Dirofilaria immitis) infections in dogs and cats with a single topical application of selamectin.
Dickin, SK; Genchi, C; Jernigan, AD; McCall, JW; McTier, TL; Pengo, G; Rowan, TG; Shanks, DJ; Six, RH; Thomas, CA; Watson, P, 2000
)
0.31
" In four controlled and masked studies conducted in the USA and Europe, animals were allocated randomly to treatment with either selamectin at a minimum dosage of 6mgkg(-1) (range, 6-12."( The efficacy of selamectin in the treatment of naturally acquired aural infestations of otodectes cynotis on dogs and cats.
Bowman, DD; Genchi, C; Hair, JA; Jernigan, AD; McTier, TL; Pengo, G; Rowan, TG; Shanks, DJ; Smith, DG; Smothers, CD; Thomas, CA; Watson, P, 2000
)
0.31
" Unit doses of selamectin (providing a minimum dosage of 6mgkg(-1)) were administered topically to the skin in a single spot at monthly intervals."( Efficacy and safety of selamectin against gastrointestinal nematodes in cats presented as veterinary patients.
Benchaoui, HA; Boy, MG; Clemence, RG; Jernigan, AD; Rowan, TG; Six, RH; Smith, DG; Sture, GH; Thomas, CA; Watson, P, 2000
)
0.31
" Unit doses of the commercial formulation of selamectin were administered to the dams to provide at least the minimum recommended dosage of 6mgkg(-1) (range, 6-12mgkg(-1))."( Efficacy of selamectin administered topically to pregnant and lactating female dogs in the treatment and prevention of adult roundworm (Toxocara canis) infections and flea (Ctenocephalides felis felis) infestations in the dams and their pups.
Clements, PJ; Jernigan, AD; Maitland, TP; McLoughlin, A; Murphy, MG; Payne-Johnson, M; Rowan, TG; Shanks, DJ; Sherington, J, 2000
)
0.31
" Selamectin was supplied in unit dose tubes designed to deliver a minimum dosage of 6mgkg(-1)."( Efficacy of selamectin against experimentally induced tick (Rhipicephalus sanguineus and Dermacentor variabilis) infestations on dogs.
Chieffo, C; Hair, JA; Jernigan, AD; Krautmann, MJ; McTier, TL; Rowan, TG; Thomas, CA; Wang, C; Young, DR, 2000
)
0.31
" Studies were designed to measure the safety of selamectin at the recommended dosage range of 6-12mgkg(-1) of body weight."( Safety of selamectin in dogs.
Ehrhart, JC; Evans, EI; Godin, CS; Jernigan, AD; Krautmann, MJ; McCall, JW; Novotny, MJ; Rowan, TG; Sun, F, 2000
)
0.31
" Studies were designed to measure the safety of selamectin at the recommended dosage range of 6-12mgkg(-1) of body weight."( Safety of selamectin in cats.
De Keulenaer, K; Evans, EI; Godin, CS; Jernigan, AD; Krautmann, MJ; McCall, JW; Novotny, MJ; Rowan, TG; Wang, C, 2000
)
0.31
" Selamectin was administered topically in a single spot to the skin of each animal's back at the base of the neck in front of the scapulae at a minimum dosage of 6mgkg(-1)."( Efficacy of selamectin administered topically in the treatment of feline otoacariosis.
Blot, C; Bourdoiseau, G; Kodjo, A; Reynaud, MC, 2003
)
0.32
" All Sarcoptes-infested dogs were topically treated twice (days 0 and 28) with the dosage recommended by the respective manufacturer (27 dogs with imidacloprid/moxidectin, 26 with selamectin)."( Efficacy and safety of imidacloprid 10% plus moxidectin 2.5% spot-on in the treatment of sarcoptic mange and otoacariosis in dogs: results af a European field study.
Dumont, P; Heine, J; Hellmann, K; Krieger, K, 2005
)
0.33
" Results suggested that topical administration at a dosage of 20 mg/kg every 7 days is efficacious for treatment of flea infestation in rabbits."( Pharmacokinetics, efficacy, and adverse effects of selamectin following topical administration in flea-infested rabbits.
Carpenter, JW; Dryden, MW; Kukanich, B, 2012
)
0.38
" The new spot-on formulation of selamectin and sarolaner was administered topically once a month for 3 consecutive months at a minimum dosage of 6 mg/kg selamectin (dose range 6-12 mg/kg) plus 1 mg/kg sarolaner (dose range 1-2 mg/kg)."( Safety and efficacy of a new spot-on formulation of selamectin plus sarolaner in the treatment and control of naturally occurring flea infestations in cats presented as veterinary patients in Australia.
Bruellke, N; Graham, K; Hodge, A; Packianathan, R; Pittorino, M, 2020
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
milbemycin
[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 Targets (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
67.9K proteinVaccinia virusPotency3.16230.00018.4406100.0000AID720580
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency33.49150.000323.4451159.6830AID743065; AID743067
Cellular tumor antigen p53Homo sapiens (human)Potency33.49150.002319.595674.0614AID651631
[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)
Genome polyproteinDengue virus 2 Thailand/16681/84Ki63.00005.80005.80005.8000AID1847507; AID1847535
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (124)

Processvia Protein(s)Taxonomy
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (34)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (19)

Processvia Protein(s)Taxonomy
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (19)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347161Confirmatory screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347169Tertiary RLuc qRT-PCR qHTS assay for Zika virus inhibitors2020Proceedings 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.
AID1347149Furin counterscreen qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347152Confirmatory screen NINDS AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347155Optimization screen NINDS Rhodamine qHTS for Zika virus inhibitors: Linked NS2B-NS3 protease assay2020Proceedings 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.
AID1347150Optimization screen NINDS AMC qHTS for Zika virus inhibitors: Linked NS2B-NS3 protease assay2020Proceedings 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.
AID1347168HepG2 cells viability qHTS for Zika virus inhibitors2020Proceedings 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.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347167Vero cells viability qHTS for Zika virus inhibitors2020Proceedings 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.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347153Confirmatory screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID60458One month protection against adult fleas after single topical application in dog2001Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
Perspectives in animal health: old targets and new opportunities.
AID1847507Inhibition of DENV2 NS2B-NS3 protease2021Bioorganic & medicinal chemistry, 11-01, Volume: 49A short survey of dengue protease inhibitor development in the past 6 years (2015-2020) with an emphasis on similarities between DENV and SARS-CoV-2 proteases.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1847535Binding affinity to DENV2 NS2B/NS3 protease assessed as inhibition constant2021Bioorganic & medicinal chemistry, 11-01, Volume: 49A short survey of dengue protease inhibitor development in the past 6 years (2015-2020) with an emphasis on similarities between DENV and SARS-CoV-2 proteases.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (156)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's82 (52.56)29.6817
2010's65 (41.67)24.3611
2020's9 (5.77)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%
Trials61 (39.61%)5.53%
Reviews3 (42.86%)6.00%
Reviews6 (3.90%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies10 (6.49%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other4 (57.14%)84.16%
Other77 (50.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (3)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Detection of Pulmonary Nodules: Comparison of Ultra-low-dose Chest CT (Approaching a Two Views Chest X-ray Radiation) and Standard Low Dose CT. A Monocentric, Prospective, Non-randomized, Comparative, Open-label Study With Blind Reading of the Judgment Cr [NCT03305978]150 participants (Actual)Interventional2017-09-26Completed
A Study Evaluating the Effect of the Number of Needle Revolutions Inside the Node on the Diagnostic Yield of EBUS-TBNA in Sarcoidosis [NCT02875756]Phase 2/Phase 3150 participants (Actual)Interventional2016-08-31Completed
Impact of Fast Gantry Rotation Cardiac CT Angiography on Coronary Motion Artifacts in the Absence of β-Blocker Premedication in Patients Undergoing Aortic Stenosis Workup: a Single-centre Randomized Controlled Trial [NCT05709652]124 participants (Anticipated)Interventional2023-03-01Not yet recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]