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Drug discovery by identifying protein targets
In the field of drug discovery, reverse pharmacology also known as target-based drug discovery (TDD), a hypothesis is first made that modulation of the
Reverse_pharmacology
Drug discovery by phenotypic screening
see if they have the desired effect. This approach is known as "reverse pharmacology" or "target based drug discovery" (TDD). However, recent statistical
Classical_pharmacology
Vaccine development via genomics to find antigens
Reverse vaccinology is an improvement of vaccinology that employs bioinformatics and reverse pharmacology practices, pioneered by Rino Rappuoli and first
Reverse_vaccinology
Integral of drug concentration in blood plasma over time
points in time and the trapezoidal rule is used to estimate AUC. In pharmacology, the area under the plot of plasma concentration of a drug versus time
Area under the curve (pharmacokinetics)
Area_under_the_curve_(pharmacokinetics)
Pharmaceutical discovery procedure
which are hypothesized to be disease-modifying in a process known as reverse pharmacology. Hits from these screens are then tested in cells and then in animals
Drug_discovery
Half maximal inhibitory concentration
IC50 is commonly used as a measure of antagonist drug potency in pharmacological research. IC50 is comparable to other measures of potency, such as
IC50
Theoretical drug measure in pharmacology
In pharmacology, the volume of distribution ( V D {\displaystyle V_{D}} , also known as apparent volume of distribution or volume of dilution) is the theoretical
Volume_of_distribution
Substance used to diagnose, cure, treat, or prevent disease
which are hypothesized to be disease-modifying in a process known as reverse pharmacology. Hits from these screens are then tested in cells and then in animals
Medication
Observation about the discovery of new drugs
shifted from whole-animal classical pharmacology testing methods (phenotypic screening) to reverse pharmacology target-approaches that result in the
Eroom's_law
Measure of organism response to stimulus
relationships modelled by dose response curves are used extensively in pharmacology and drug development. In particular, the shape of a drug's dose–response
Dose–response_relationship
properties (forward pharmacology) or target directed assays to identify their biological target and mechanism of action (reverse pharmacology). Venoms are naturally
Venoms_in_medicine
Study of traditional medicine practiced in ethnic groups
as a starting point in drug discovery, specifically those using reverse pharmacological techniques. Ethnopharmacology is a related field which studies
Ethnomedicine
Species of plant
Falquet; Chiaka Diakite; Sergio Giani; Drissa Diallo (2011). "A "reverse pharmacology" approach for developing an anti-malarial phytomedicine". Malaria
Argemone_mexicana
Indian Ayurvedic physician and Sanskrit scholar (1877–1945)
depression, among others. Their research also laid the foundation for reverse pharmacology in India. Sen also worked tirelessly for the welfare of his community
Gananath_Sen
Molecular biologist
orphan receptors to discover new neurotransmitters referred to as reverse pharmacology. Utilizing this strategy, he was the first to identify a novel neuropeptide
Olivier_Civelli
Neuropeptide chemical compound
inhibit N/OFQ receptor function. Nociceptin is the first example of reverse pharmacology; the NOP receptor was discovered before the endogenous ligand which
Nociceptin
Biochemical analysis procedure
J.C.; Inglese, J. (2025). "A general assay platform to study protein pharmacology using ligand-dependent structural dynamics". Nat Commun. 16 (1) 4342
Structural Dynamics Response Assay
Structural_Dynamics_Response_Assay
Biochemical analysis procedure
removal of unbound reagents. Ligand binding assays are used primarily in pharmacology for various demands. Specifically, despite the human body's endogenous
Ligand_binding_assay
Molecular dynamics software package
MDynaMix Ascalaph Designer BOSS (molecular mechanics) CHARMM GROMACS Reverse Pharmacology OPLS Yasara Folding@home Amber 2023 Reference Manual Weiner, Paul
AMBER
Part of an organism targeted by a ligand or drug to affect behavior
intervention, is the first step in the discovery of a medicine using the reverse pharmacology approach. Potential drug targets are not necessarily disease causing
Biological_target
Drug discovery technique
screening High throughput biology IC50 / EC50 Laboratory automation Reverse pharmacology Synthetic genetic array Virtual high throughput screening Yeast two-hybrid
High-throughput_screening
Chemical compound
sphingosine 1-phosphate receptor agonists as immunomodulators based on reverse pharmacology". Perspectives in Medicinal Chemistry. 1 1177391X0700100002: 11–23
Fingolimod
Type of medical testing in drug discovery
see if they have the desired effect. This approach is known as "reverse pharmacology" or "target based drug discovery" (TDD). However recent statistical
Phenotypic_screening
Prediction method in molecular modeling
likely to bind to protein target of interest (see virtual screening). Reverse pharmacology routinely uses docking for target identification. lead optimization
Docking_(molecular)
Italian immunologist (born 1952)
genomic approach to vaccine development known as reverse vaccinology, a subsection of reverse pharmacology. Rappuoli joined Chiron as head of European vaccines
Rino_Rappuoli
Pharmacological phenomenon
Reverse tolerance or drug sensitization is a pharmacological phenomenon describing subjects' increased reaction (positive or negative) to a drug following
Reverse_tolerance
Techniques used to study protein–small molecule interactions
a disease phenotype, as opposed to target-based drug discovery (reverse pharmacology), in which lead compounds are designed to interact with predetermined
Chemoproteomics
Invention of new medications based on knowledge of a biological target
insufficient for effective intervention. Rational drug design (also called reverse pharmacology) begins with a hypothesis that modulation of a specific biological
Drug_design
Drug class
sphingosine 1-phosphate receptor agonists as immunomodulators based on reverse pharmacology". Perspectives in Medicinal Chemistry. 1: 11–23. doi:10.1177/1177391X0700100002
Sphingosine-1-phosphate receptor modulator
Sphingosine-1-phosphate_receptor_modulator
Collection of chemicals
chemical libraries are often used in target based drug discovery (reverse pharmacology). Among the compound libraries should be annotated the Fragment Compound
Chemical_library
American pharmacologist (born 1981)
Drug Administration. She was previously director of the department of pharmacology and molecular sciences at Johns Hopkins University School of Medicine
Namandjé_Bumpus
Protein with a receptor structure but with unidentified ligand
orphans. However, with modern molecular biology techniques such as reverse pharmacology, screening of cDNA libraries, and whole genome sequencing, receptors
Orphan_receptor
Field of study
Its role in interindividual differences in drug response". Clinical Pharmacology & Therapeutics. 85 (4): 426–430. doi:10.1038/clpt.2009.2. PMID 19242404
Pharmacoepigenetics
Pharmacodynamics and pharmacokinetics of ethanol
The pharmacology of ethanol involves both pharmacodynamics (how it affects the body) and pharmacokinetics (how the body processes it). In the body, ethanol
Pharmacology_of_ethanol
Type of receptor ligand or drug that blocks a biological response
include alpha blockers, beta blockers, and calcium channel blockers. In pharmacology, antagonists have affinity but no efficacy for their cognate receptors
Receptor_antagonist
Belgian bioengineer and molecular biologist
Peter; Ballet, Steven; Steyaert, Jan (2018-05-04). "Nanobody-Enabled Reverse Pharmacology on G-Protein-Coupled Receptors". Angewandte Chemie International
Jan_Steyaert
Antiretroviral medication
Clercq E (January 1994). "HIV resistance to reverse transcriptase inhibitors". Biochemical Pharmacology. 47 (2): 155–169. doi:10.1016/0006-2952(94)90001-9
Zidovudine
Pharmacology of the antiparkinsonian and antidepressant selegiline
The pharmacology of selegiline pertains to the pharmacodynamic and pharmacokinetic properties of the antiparkinsonian and antidepressant selegiline (L-deprenyl)
Pharmacology_of_selegiline
Movement of a drug into the bloodstream or lymph
Clinical Pharmacology". MSD Manual Professional Edition. Retrieved 2020-03-28. Kaplan Pharmacology 2010, page 6, Absorption Kaplan Pharmacology 2010, Video
Absorption_(pharmacology)
Multinational Life science company
cellular targets; this came to be known as target-based screening (i.e. reverse pharmacology). The multi-target approach entails the understanding that, although
Persomics
Reduced reaction to a drug following repeated use
Drug tolerance or drug insensitivity is a pharmacological concept describing subjects' reduced reaction to a drug following its repeated use. Drug tolerance
Drug_tolerance
"Pharmacomicrobiomics: The Impact of Human Microbiome Variations on Systems Pharmacology and Personalized Therapeutics". OMICS: A Journal of Integrative Biology
Pharmacomicrobiomics
2004.02.028, PMID 15183338 Kakuda, T.N. (2010), "Pharmacology of nucleoside and nucleotide Reverse transcriptase inhibitor - induced mitochondrial toxicity"
Discovery and development of nucleoside and nucleotide reverse-transcriptase inhibitors
Discovery_and_development_of_nucleoside_and_nucleotide_reverse-transcriptase_inhibitors
Opioid receptor antagonist
name Narcan among others, is an opioid antagonist, a medication used to reverse or reduce the effects of opioids. Naloxone is commonly used to restore
Naloxone
Reverse transport, or transporter reversal, is a phenomenon in which the substrates of a membrane transport protein are moved in the opposite direction
Reverse_transport
Pharmaceutical compound
The pharmacology of cyproterone acetate (CPA) concerns the pharmacology (pharmacodynamics, pharmacokinetics, and routes of administration) of the steroidal
Pharmacology of cyproterone acetate
Pharmacology_of_cyproterone_acetate
Chemical compound
four months than those not given the supplement. Mitoquinone was able to reverse the early signs of diabetes-related heart failure over the course of the
Mitoquinone_mesylate
Opioid antagonist
(April 2021). "Methocinnamox Reverses and Prevents Fentanyl-Induced Ventilatory Depression in Rats". The Journal of Pharmacology and Experimental Therapeutics
Methocinnamox
Pharmaceutical compound
The pharmacology of bicalutamide is the study of the pharmacodynamic and pharmacokinetic properties of the nonsteroidal antiandrogen (NSAA) bicalutamide
Pharmacology_of_bicalutamide
Agent in biochemistry
In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of
Inverse_agonist
GABA receptor antagonist drug and benzodiazepine antidote
flumazenil is primarily used to treat benzodiazepine overdoses and to help reverse anesthesia. Administration of flumazenil by sublingual lozenge and topical
Flumazenil
Pharmaceutical compound
despite cessation of dosing. The pro-erectile effects of volufralin can be reversed by a melanocortin MC4 receptor antagonist in rodents. Volufralin is a semisynthetic
Volufralin
Chemical compound
heparins (LMWH), and unfractionated heparin). Ciraparantag significantly reverses anticoagulation induced by a therapeutic dose of edoxaban within 10 minutes
Ciraparantag
Mood-stabilizing psychiatric medication
partially reverses telomere shortening in these patients and also increases mitochondrial function, although how lithium produces these pharmacological effects
Lithium_(medication)
Chemical compound
pharmacokinetics: formulation on its absorption". Journal of Clinical Pharmacology. 52 (9): 1343–1349. doi:10.1177/0091270011414575. PMID 21903894. "Meclizine
Meclizine
Adenosine A2A receptor antagonist for Parkinson's disease
A2A antagonist Lu AA47070 reverses the motor and motivational effects produced by dopamine D2 receptor blockade". Pharmacology, Biochemistry, and Behavior
Lu_AA47070
Indian independence activist, politician, social reformer, journalist and writer
practice. This practice has been recently fulfilled by the use of Reverse Pharmacology in Ayurveda. Babubhai died on 12 December 1979, in Mumbai. His 50-year
Babubhai_P._Vaidya
Pharmaceutical compound
UC Davis. Retrieved 2026-05-12. JRT - Isomer Design LSD-Inspired Drug Reverses Psychosis Brain Damage Without Hallucinations - Neuroscience News Scientists
JRT_(drug)
TrkA and TrkB positive modulator
than at the TrkA, TrkB, and TrkC. In animals, ACD856 has been found to reverse scopolamine- and dizocilpine (MK-801)-induced memory impairment, to improve
ACD856
Chemical compound
analgesic properties. It was introduced in 1954 and was used as an antidote to reverse opioid overdose and in a challenge test to determine opioid dependence
Nalorphine
Chemical compound
Federal Trade Commission for deceptive advertising implying that TA-65 can reverse aging and repair DNA damage. Its mode of action is purported to be the
Cycloastragenol
Alpha-adrenergic agonist
treating resistant hypertension. Clonidine is used as a non-stimulant pharmacological treatment for ADHD and is USFDA-approved in its extended-release formulation
Clonidine
Class of psychoactive drugs that produce empathic experiences
of MDMA were first described in the 1970s. Entactogens as a unique pharmacological class depending on induction of serotonin release was established in
Entactogen
Pharmaceutical compound
Nguyen MM, Kuang RR, Nguyen C, Huynh E, et al. (October 2021). "SPG302 Reverses Synaptic and Cognitive Deficits Without Altering Amyloid or Tau Pathology
Tazbentetol
Non-depolarizing neuromuscular blocker
(March 2007). "Sugammadex: another milestone in clinical neuromuscular pharmacology". Anesthesia and Analgesia. 104 (3): 575–581. doi:10.1213/01.ane.0000244594
Rocuronium_bromide
Sedating antihistamine
September 2023. "promazine | Ligand Activity Charts | IUPHAR/BPS Guide to PHARMACOLOGY". Guidetopharmacology.org. Retrieved 18 May 2023. Möller HJ, Müller WE
Promethazine
Chemical compound
Pregnenolone 16α-carbonitrile Proadifen Progesterone Quingestrone Reserpine Reverse triiodothyronine Rifampicin Rifaximin Rimexolone Riodipine Ritonavir Simvastatin
Clotrimazole
Atypical opioid drug
substitution of conventional opioids like morphine with SR-17018 can reverse analgesic tolerance and suppress withdrawal symptoms in rodents. However
SR-17018
Drug class
facilitate the reverse transport of monoamine neurotransmitters at said transporters, leading to non-exocytotic monoamine release. This reverse-transport is
Norepinephrine–dopamine releasing agent
Norepinephrine–dopamine_releasing_agent
Pharmaceutical compound
indicating lack of sedation, and its effects in neuropathic pain models were reversed by a centrally active oxytocin receptor antagonist but not by a peripherally
LIT-002
Chemical compound
the latter being the isomer with the pharmacologic effect as an alpha 2- adrenergic agonist. Effects can be reversed using atipamezole. It was developed
Medetomidine
Belgian physician (1926–2003)
with a postdoctoral degree in pharmacology at the same university in 1956, and studied at the Institute of Pharmacology of the University of Cologne.
Paul_Janssen
Class of antiviral drugs used to treat HIV/AIDS and hepatitis C
known as "Crix belly", after indinavir (Crixivan). The Proteolysis Map Reverse-transcriptase inhibitor Discovery and development of NS5A inhibitors Discovery
Protease inhibitor (pharmacology)
Protease_inhibitor_(pharmacology)
Biochemical interaction through which a drug produces its pharmacological effect
In pharmacology, the term mechanism of action (MOA) refers to the specific biochemical interaction through which a drug substance produces its pharmacological
Mechanism_of_action
Class of acetylcholinesterase inhibitors
the treatment of myasthenia gravis, while neostigmine is also used to reverse non-depolarizing neuromuscular blockade after surgery. Rivastigmine is
Stigmine
Pharmaceutical compound
et al. (January 2023). "Ephedrae Herba: A Review of Its Phytochemistry, Pharmacology, Clinical Application, and Alkaloid Toxicity". Molecules. 28 (2). Basel
Ephedroxane
Medical condition
substance abuse is necessary. There have been no controlled studies about pharmacological treatments of intermetamorphosis. However, both atypical and typical
Intermetamorphosis
Combination drug
ergot derivatives and strong CYP3A4 inhibitors, such as HIV protease or reverse transcriptase inhibitors, azole antifungals, or macrolide antibiotics,
Bellergal
Psychoactive drug, often called ecstasy
in 20,000 instances to 1 death in 50,000 instances. The purported pharmacological effects that may be prosocial include altered sensations, increased
MDMA
Triglyceride found in butter
HDAC inhibitor similarly to butyric acid. Tributyrin has been found to reverse gut microbiota dysbiosis and intestinal injury and inflammation induced
Tributyrin
Chemical compound
any significant advantage over existing triple-drug HIV therapies, and pharmacology studies showed that capravirine may interact with other HIV drugs. PubChem
Capravirine
Experimental cognitive enhancer
N, Papageorgiou C, Politis AM (July 2023). "A Systematic Review of Pharmacological Interventions for Apathy in Aging Neurocognitive Disorders". Brain
Pirepemat
Chemical compound
N, Grant L, Le Sommer S, Lees EK, Mody N, et al. (October 2017). "Pharmacological inhibition of protein tyrosine phosphatase 1B protects against atherosclerotic
Trodusquemine
Antidepressant medication
in blood pressure. In a study comparing 32 antidepressants of all pharmacological classes, mirtazapine was one of the antidepressants most likely to
Mirtazapine
Chemical compound
(2′-3′-dideoxycytidine, ddC), also called dideoxycytidine, is a nucleoside analog reverse-transcriptase inhibitor (NRTI) sold under the trade name Hivid. Zalcitabine
Zalcitabine
Type of enzyme
with trypsin, and peptides from it were separated from one another by reverse phase high performance liquid chromatography. The resulting fragments were
N-acyl phosphatidylethanolamine-specific phospholipase D
N-acyl_phosphatidylethanolamine-specific_phospholipase_D
the key effector of reverse cholesterol transport ATP-binding cassette A1 in monocytoid cells by niacin". Biochemical Pharmacology. 67 (3): 411–9. doi:10
Reverse_cholesterol_transport
Semi-synthetic opioid
Clark JD, Lameh J (January 2006). "Pharmacological profiles of opioid ligands at kappa opioid receptors". BMC Pharmacology. 6 (1) 3. doi:10.1186/1471-2210-6-3
Etorphine
Benzodiazepine analog drug
therefore increasing its pharmacological effects. Carbamazepine speeds up the metabolism of etizolam, resulting in reduced pharmacological effects. Cases of
Etizolam
Drug belonging to the tryptamine class
Substituted α-alkyltryptamine McKenna DJ, Towers GH (1984). "Biochemistry and pharmacology of tryptamines and beta-carbolines. A minireview". J Psychoactive Drugs
4-Methyl-α-methyltryptamine
TAAR1 agonist
RO5263397 at the mTAAR1. RO5263397 can partially and dose-dependently reverse the suppressive effects of RO5256390 on monoaminergic neuron firing in
RO5263397
Synthetic opioid pain medication
Ueta Y (March 2007). "Pharmacological aspects of the effects of tramadol on G-protein coupled receptors". Journal of Pharmacological Sciences. 103 (3): 253–260
Tramadol
Opioid analgesic compound
Metabolite in Human Plasma Increases Its Opioid Potency and Efficacy". ACS Pharmacology & Translational Science. 3 (6): 1063–1068. doi:10.1021/acsptsci.0c00075
Mitragynine_pseudoindoxyl
Glucocorticoid steroid (chemical compound)
with glucocorticosteroids. If HPA axis suppression occurs, it is often reversed shortly after discontinuation of treatment. Absorption of topical corticosteroids
Betamethasone_dipropionate
Chemical compound
"Behavioral pharmacology of abecarnil in baboons: self-injection, drug discrimination and physical dependence". Behavioural Pharmacology. 3 (5): 507–516
Abecarnil
Central nervous system stimulant
Docherty JR (June 2008). "Pharmacology of stimulants prohibited by the World Anti-Doping Agency (WADA)". British Journal of Pharmacology. 154 (3): 606–622. doi:10
Amphetamine
Medication used for spinal muscular atrophy
scheme closed to new people in November 2018. In May 2019, however, NICE reversed its stance and announced its decision to recommend nusinersen for use across
Nusinersen
Chemical compound
dependence involves considering the person's age, comorbidity and the pharmacological pathways of GHB. The mainstay of treatment for severe withdrawal is
Γ-Hydroxybutyric_acid
Opioid analgesic
is often employed in the treatment of postanesthetic shivering. The pharmacologic mechanism of this antishivering effect is not fully understood, but
Pethidine
Class of medications
pharmacokinetics. For many years the TCAs were the first choice for pharmacological treatment of major depression. Although they are still considered to
Tricyclic_antidepressant
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REVERSE PHARMACOLOGY
REVERSE PHARMACOLOGY
REVERSE PHARMACOLOGY
REVERSE PHARMACOLOGY
REVERSE PHARMACOLOGY
REVERSE PHARMACOLOGY
REVERSE PHARMACOLOGY
REVERSE PHARMACOLOGY
REVERSE PHARMACOLOGY
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