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ANTITARGET

Antitarget

Concept in pharmacology

In pharmacology, an antitarget (or off-target) is a receptor, enzyme, or other biological target that, when affected by a drug, causes undesirable side-effects

Antitarget

KCNH2

Mammalian protein found in humans

called torsades de pointes). This has made hERG inhibition an important antitarget that must be avoided during drug development. hERG has also been associated

KCNH2

PNU-282,987

Chemical compound

suitable for use in humans because of excessive inhibition of the hERG antitarget. PNU-282987 has been shown to initiate signaling that leads to adult neurogeneis

PNU-282,987

Trazodone

Antidepressant medication

2165/00003088-198510030-00002. PMID 2861928. S2CID 21305772. Vaz RJ, Klabunde T (2008). Antitargets: Prediction and Prevention of Drug Side Effects. John Wiley & Sons. pp

Trazodone

Guanfacine

Medication used for high blood pressure and ADHD

memory in aged monkeys). Activation of the 5-HT2B receptor is a well-known antitarget and is associated with cardiac valvulopathy. However, not all 5-HT2B receptor

Guanfacine

List of modafinil analogues and derivatives

(hERG) that can lead to heart problems (potent inhibition of the hERG antitarget and predicted cardiotoxicity). Adrafinil (Olmifon, CRL-40028, N-hydroxymodafinil)

List of modafinil analogues and derivatives

List_of_modafinil_analogues_and_derivatives

Tabernanthalog

Pharmaceutical compound

receptor. Tabernanthalog was found to be 100-fold less potent at the hERG antitarget compared to ibogaine, and hence is thought to have a much lower potential

Tabernanthalog

JJC8-088

Cocaine-like dopamine reuptake inhibitor derived from modafinil

sigma σ1 receptor (Ki = 41.6 nM). The drug has high affinity for the hERG antitarget (IC50Tooltip half-maximal inhibitory concentration = 130 nM) and could

JJC8-088

Off-target activity

Drug biological activity

in women. Metformin also causes off-target activity.[citation needed] Antitarget Mohammadi E, Benfeitas R, Turkez H, Boren J, Nielsen J, Uhlen M, Mardinoglu

Off-target activity

Off-target_activity

Drug design

Invention of new medications based on knowledge of a biological target

affect any other important "off-target" molecules (often referred to as antitargets) since drug interactions with off-target molecules may lead to undesirable

Drug design

Drug_design

Quinidine

Antiarrythmic medication

Proarrhythmic Effects Thereof". In Urban L, Patel V, Vaz RJ (eds.). Antitargets and Drug Safety. Wiley. pp. 303–. ISBN 978-3-527-67367-4. Archer SL,

Quinidine

Drug discovery

Pharmaceutical discovery procedure

candidate based on its safety, specificity of effect, and efficacy of doses. Antitarget Bioinformatics Biomedical informatics Cheminformatics Drug discovery hit

Drug discovery

Drug_discovery

Ibogalog

Class of chemical compounds

addition, the compounds have dramatically reduced potency at the hERG antitarget compared to ibogaine, which confers much less cardiotoxicity. Ibogalogs

Ibogalog

N-Bn-THAZ

Pharmaceutical compound

numerous other targets, notably including the serotonin 5-HT2B receptor antitarget. The drug has been found to produce pro-cognitive-like effects in rodents

N-Bn-THAZ

Para-Aminoblebbistatin

Chemical compound

Guedes RC, Stevens CV, García-Sosa AT (2018). "Recovering Actives in Multi-Antitarget and Target Design of Analogs of the Myosin II Inhibitor Blebbistatin"

Para-Aminoblebbistatin

Dirty drug

Informal term for a drug that binds to many different molecular targets or receptors

try to make new drugs as selective as possible to minimise binding to antitargets and hence reduce the occurrence of side effects and risk of adverse reactions

Dirty drug

Dirty_drug

JJC8-016

Abandoned drug

abandoned following findings that it interacts with high affinity at the hERG antitarget (IC50Tooltip half-maximal inhibitory concentration = 60 nM) and thereby

JJC8-016

Matched molecular pair analysis

M. H.; Sefton, C. E.; Wood, D. J. (2012). "Prospective prediction of antitarget activity by matched molecular pairs analysis". Mol. Inform. 31 (5): 365–368

Matched molecular pair analysis

Matched_molecular_pair_analysis

Pseudokinase

Catalytically-deficient pseudoenzyme

variety of diseases, which has made them potential drug targets and antitargets. Pseudokinases are made up of an evolutionary mixture of eukaryotic protein

Pseudokinase

Gerhard Ecker

Austrian medicinal chemist

substrate properties. Around 2010 he extended the studies also on other antitargets, such as the hERG potassium channel, as well as on the serotonin transporter

Gerhard Ecker

Gerhard_Ecker