E-64 is a natural, potent, and irreversible inhibitor of cysteine proteases; IC50 values for inhibiting cathepsins K, S, and L, in vitro, are 1.4, 4.1, and 2.5 nM, respectively.

Nemorubicin, also known as PNU152243A, is a doxorubicin derivative that differs significantly from its parent drug in terms of spectrum of antitumor activity, metabolism and toxicity profile. The drug is active on tumors resistant to alkylating agents, topoisomerase II inhibitors and platinum derivatives. It works primarily through topoisomerase I inhibition. Of note, Nemorubicin is active in cells with upregulation of the nucleotide excision repair (NER) pathway, where current therapies fail. Nemorubicin is biotransformed in the liver into cytotoxic metabolites that may further contribute to render this drug highly active against primary liver tumors or liver metastases.

Tazobactam inhibits the action of bacterial β-lactamases, especially those belonging to the SHV-1 and TEM groups. It is commonly used as its sodium salt, tazobactam sodium. Tazobactam is combined with the extended spectrum β-lactam antibiotic piperacillin in the drug piperacillin/tazobactam, one of the preferred antibiotic treatments for nosocomial pneumonia caused by Pseudomonas aeruginosa.[medical citation needed] Tazobactam broadens the spectrum of piperacillin by making it effective against organisms that express β-lactamase and would normally degrade piperacillin. Tazobactam is derived from the penicillin nucleus and is a penicillinic acid sulfone.

Rimegepant (BMS-927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki value of 0.027 nM.

Puromycin Dihydrochloride is an antibiotic. It inhibits protein synthesis by binding to RNA. Puromycin Dihydrochloride has antimicrobial, antitrypanosomal, and antineoplastic properties.

Puromycin is an aminoglycoside antibiotic isolated from the bacterium Streptomyces alboniger. It is a protein synthesis inhibitor.

Perhexiline maleate (WSM 3978G) is a prophylactic antianginal agent that inhibits carnitine palmitoyltransferase (CPT1/CPT2).

MS2734 is a bisubstrate Nicotinamide N-methyltransferase (NNMT) with IC50 of 14 uM, Kd of 2.7 uM..

JPH203 (KYT-0353) is a potent, selective L-type amino acid transporter 1 (LAT1, SLC7A5) inhibitor with IC50 of 60 nM (leucine uptake inhibition), but not LAT2.

Golotimod (SCV-07), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function.

Ertapenem is a carbapenem antibiotic marketed by Merck as Invanz.

MIN-101 (Roluperidone, CYR-101, MT-210) is a higly potent 5-HT2A and sigma 2 receptor antagonist, with no direct dopamine affinities, for treatment of negative symptoms in schizophrenia..

TAK-599 is a highly promising parenteral cephalosporin targeted for MRSA infection.

Finasteride is a medication used for the treatment of benign prostatic hyperplasia (BPH) and male pattern baldness (MPB). It is a type II and type III 5α-reductase inhibitor; 5α-reductase, an enzyme, converts testosterone to dihydrotestosterone (DHT).

Cefozopran (SCE-2787) is a new parenteral cephalosporin, against experimental infections in mice.

Liothyronine sodium (T3 Sodium sal) is the most potent form of thyroid hormone used to treat hypothyroidism and myxedema coma.

γ-L-Glutamyl-L-alanine, composed of gamma-glutamate and alanine, is a proteolytic breakdown product of larger proteins.

γ-Glu-Phe (γ-Glutamylphenylalanine) is synthesized by Bacillus amyloliquefaciens (GBA) and Aspergillus oryzae (GAO). γ-Glu-Phe or the post-enzymatic reaction mixture enhances the umami intensity of commercial soy sauce and model chicken broth.

Dexketoprofen works by blocking the action of a substance in the body called cyclo-oxygenase. It belongs to a class of medicines called non-steroidal anti-inflammatory drugs (NSAIDs).

L-AP4 is a selective group III metabotropic glutamate receptor agonist..

LY2794193 is a highly potent and selective mGlu3 receptor agonist with Ki of 0.93 nM and EC50 of 47 nM, >100-fold selectivity over mGlu2 receptor..

Highly selective group II mGlu receptor agonist (EC50 values are 2.69 and 4.48 nM for hmGlu2 and hmGlu3 respectively) that displays > 80-fold selectivity over group I and group III receptors.

Semax is a synthetic peptide analog of adrenocorticotropic hormone

Pirmenol inhibits IK.ACh by blocking muscarinic receptors. The IC50 of Pirmenol for inhibition of Carbachol-induced IK.ACh is 0.1 μM.

Nelarabine (Arranon, 506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.

Bufalin inhibits steroid receptor coactivator 1 (SRC-1) and SRC-3 at doses as low as 5 nM, promotes the degradation of SRC-3 protein, and inhibits cancer cell growth both in vitro and in vivo.

Streptomycin (Agrept) is an effective antibiotic against M. tuberculosis, is used for the research of tuberculosis (TB). Streptomycin also is a bacteriocidal agent that can be used for the research of a number of bacterial infections. Streptomycin can bind strongly to nucleic acids, interferes and blocks protein synthesis while permitting continued RNA and DNA synthesis. Streptomycin, as a common antibiotic used in culture media, also is a blocker of stretch-activated and mechanosensitive ion channels in neurons and cardiac myocytes .

Pogostemon (patchouli) leaves and their extracted oils are used in perfumes and in traditional medicine to relieve sunstroke, stop vomiting, and increase appetite.

Lurbinectedin (PM01183) is a new DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively.

Ademetionine, also known as AdoMet; MSI-195; SAMe, S-adenosylmethionine, is a PDE4B inhibitor potentially for treatment of primary biliary cirrhosis and major depressive disorder. Ademetionine is a ubiquitous metabolite present in all cells and biological fluids, and serves as a methyl donor in a multitude of different methylation reactions involving proteins, phospholipids, catecholamines and DNA. Pharmaceutical preparations of some stable salts of SAMe are available for parenteral and oral use in humans, and have been shown to increase plasma and cerebrospinal fluid SAMe concentrations.