MA-VAL-ALA-PAB-OH is a usefully ACD-linker, which was reported in JACS 2020, 142, pp12890-12895.

(R)-4-Amino-3-hydroxybutyric acid, also known as (R)-GABOB, is a GABA receptor modulator. It binds to GABAA and GABAB receptors and inhibits GABA uptake in rat brain synaptosomes. (R)-4-amino-3-hydroxybutyric acid is also a GABAC receptor agonist that induces currents in a patch-clamp assay using Xenopus oocytes expressing the human receptor. In vivo, (R)-4-amino-3-hydroxybutyric acid inhibits electrical discharges in the amygdala in a cat model of N-amidinobenzamide-induced seizures.

ACHP is an IκB kinase inhibitor that inhibits DNA binding activity of NF-κB, blocks NF-κB pathway in multiple myeloma cell lines, and induces cell growth arrest and apoptosis. It also inhibits STAT3 signaling in NSCLC in vitro.

BD-AcAc2 is a ketone ester with anti-obesity and anticonvulsant activities. Oral administration of BD-AcAc2 reduces body weight, food intake, and whole animal adiposity in mice fed an isocaloric diet. BD-AcAc2 increases the seizure threshold and blood levels of β-hydroxybutyrate in a rat model of seizures induced by pentylenetetrazole.

AZD-2207 is a cannabinoid receptor CB1 antagonist and highly lipophilic compound for the treatment of type 2 diabetes mellitus and obesity.

Exametazime is a Diagnostic Aid (Regional Cerebral Perfusion Imaging). It is a radiopharmaceutical sold under the trade name Ceretec, and is used by nuclear medicine physicians for the detection of altered regional cerebral perfusion in stroke and other cerebrovascular diseases.

ORY1001, also known as RG-6016, is KDM1A inhibitor (IC50 <20nM) with high selectivity against related FAD dependent aminoxidases (MAO-A/B, IL4I1, KDM1B >100uM, SMOX 7uM). ORY-1001 does not inhibit non-related histone modifiers. Treatment of THP-1 (MLL-AF9) cells with ORY-1001, results in a time/dose dependent me2H3K4 accumulation at KDM1A target genes and concomitant induction of differentiation markers (EC50 me2H3K4 and FACS CD11b <1nM). ORY-1001 induces apoptosis in THP-1 and inhibits proliferation and colony formation of MV(4;11) (MLL-AF4) cells (EC50 <1nM).

AZD1446, also known as TC-6683, is a novel highly selective α4β2 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders. AZD1446 showed favorable pharmaceutical properties and in vivo efficacy in animal models has been identified as a potential treatment for cognitive deficits associated with psychiatric or neurological conditions and had been evaluated in phase 2 clinical trials as a treatment for Alzheimer's disease.

LDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2)

Benzovindiflupyr is a fungicide. It inhibits mitochondrial complex II, also known as succinate dehydrogenase (SDH; IC50 = 5.2 nM), and mycelial growth of S. sclerotiorum (EC50 = 0.011 µg/ml). Benzovindiflupyr (60 µg/ml) completely protects eggplant leaves from S. sclerotiorum infection. Formulations containing benzovindiflupyr have been used to control various fungal diseases in agriculture.

Bacteriochlorophyll a is a Bacteriochlorophyll from Rhodopseudomonas sphaeroides. The compounds of this class strongly absorb light at lambda=770-850 nm. This unique property opens new therapeutic opportunities due to deeper tissue penetration of light, thereby increasing the photodamage for tumor eradication.

CGS-20625 is an anxiolytic drug used in scientific research. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic. It produces anxiolytic and anticonvulsant effects, but with no sedative effects even at high doses, and no significant muscle relaxant effects. It is orally active in humans, but with relatively low bioavailability. CGS-20625 is a positive allosteric modulator at several GABAA receptors types. Due to its alicyclic moiety potency at γ1 subunit, containing receptor types is more pronounced for CGS-20625 compared to benzodiazepines. γ1 subunits are expressed at higher levels in the central amygdala.

Fluoxetine is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. It is used for the treatment of major depressive disorder, obsessive–compulsive disorder, bulimia nervosa, panic disorder, and premenstrual dysphoric disorder.

MTDIA, also known as MT-DADMe-ImmA, and Methylthio-DADMe-Immucillin A, is a MTAP inhibitor. Human 5'-methylthioadenosine phosphorylase (MTAP) is solely responsible for 5'-methylthioadenosine (MTA) metabolism to permit S-adenosylmethionine salvage. Transition-state (TS) analogues of MTAP are in development as anticancer candidates. TS analogues of MTAP incorporate a cationic nitrogen and a protonated 9-deazaadenine leaving group, which are mimics of the ribocation transition state. MT-ImmA and MT-DADMe-ImmA are two examples of these TS analogues.

AN-2898 ia a potent and selective PDE4 inhibitor potentially for the treatment of fungal infection. AN2898 inhibited phosphodiesterase 4 (PDE4) enzyme activity (IC50 0.060 μM) and the release of multiple cytokines including TNF-α (IC50 0.16 μM) from peripheral blood mononuclear cells (hPBMCs) stimulated by lipopolysaccharide (LPS) or phytohemag- glutinin.

Moxidectin is an anthelmintic drug which kills parasitic worms (helminths), and is used for the prevention and control of heartworm and intestinal worms. Moxidectin is a semisynthetic derivative of nemadectin which is produced by fermentation by Streptomyces cyano-griseus. This Streptomyces species was discovered in a soil sample from Australia in the late 1980s collected by an agronomist working for the American Cyanamid company.

Epetraborole, also known as GSK2251052 and AN3365, is a potent and selective leucyl-tRNA synthetase inhibitor. Epetraborole was in development for the treatment of infections caused by multidrug-resistant Gram-negative pathogens. GSK2251052 is a novel boron-containing antibiotic that inhibits bacterial leucyl tRNA synthetase. All Clostridium perfringens strains had GSK2251052 MICs of >32 μg/ml.

Gefapixant citrate is a P2X3 antagonist currently studied for use in the treatment of disorders associated with purinergic receptor activation.

Lanifibranor, also known as IVA-337, is a peroxisome proliferator-activated receptors (PPAR) agonist.

Pipequaline, also known as PK-8165, is an anxiolytic drug that was never marketed. It possesses a novel chemical structure that is not closely related to other drugs of this type. The drug has a similar pharmacological profile to the benzodiazepine family of drugs, but with mainly anxiolytic properties and very little sedative, amnestic or anticonvulsant effects, and so is classified as a nonbenzodiazepine anxiolytic. Pipequaline acts as a non-selective GABAA receptor partial agonist. While its profile of anxiolytic effects without sedation would appear to have potential medical applications, pipequaline has never been developed for medical use and is currently only used in scientific research.

Nifenalol, also known as INPEA, is a new beta-adrenergic receptor antagonist.

P552-02, also known as KM-003, PS 552-02, or 552-02, is a sodium channel blocker potentially for the treatment of cystic fibrosis.

AC-90179 is a high selective 5-hydroxytryptamine2A receptor inverse agonist. It is an atypical antipsychotic pharmaceutical. It has been shown to alleviate hallucinogen-induced vasocontriction and possible other harmful physical symptoms.

Bisbenzimide, also known as Pibenzimol, Hoechst 33258, is a cell-permeable, benzimidazole dye that binds to the minor groove of double stranded DNA with preference for adenine and thymine-rich sequences.

NSC 632839 is an Inhibitor of ubiquitin isopeptidase activity.

Topovale, also known as ARC-111, is a potent topoisomerase I inhibitor. ARC-111 inhibits hypoxia-mediated hypoxia-inducible factor-1alpha accumulation. ,ARC-111 exhibited low nM cytotoxicity against a panel of cancer cells. ARC-111 cytotoxicity as well as ARC-111-induced apoptosis was reduced >100-fold in CPT-resistant topoisomerase I (TOP1)-deficient P388/CPT45 cells as compared with P388 cells.

Dexamethasone phosphate disodium is a water-soluble form of the synthetic glucocorticoid dexamethasone.

AZD6538 is a novel mGluR5 negative allosteric modulators selected for clinical development.

AZD1386 is an orally available antagonist of the transient receptor potential channel TRPV1. Note: Structure of this product was from NIH/NCATS web page: https://drugs.ncats.io/drug/210323T9CP and drugbank web page: https://go.drugbank.com/drugs/DB15333.

Importazole is a small molecule inhibitor of the transport receptor importin-β. Importazole specifically inhibits the function of importin-β, likely by altering its interaction with RanGTP. Importazole is a valuable tool to evaluate the function of the importin-β/RanGTP pathway at specific stages during the cell cycle.