YK-009 is a novel ionizable lipid for mRNA delivery. Comparisons of YK009-LNP-mRNA and commercial MC3-LNP-mRNA showed that YK009-LNP-mRNA vaccines had good biodistribution patterns, favorable tissue clearance, and high delivery efficiency. Furthermore, our study proved that YK009-LNP-Omicron mRNA could trigger a robust immune response and immune protection against the SARS-CoV-2 Omicron variant.

Lipidoid S14 is a novel lipidoid for siRNA delivery.Lipidoid-polymer hybrid nanoparticle (FS14-NP) can efficiently deliver siRNA against IL-1β (siIL-1β) to macrophages and effectively suppress the pathogenesis of experimental arthritis induced by collagen antibody (CAIA mice). FS14-NP/siIL-1β achieved approximately 70% and 90% gene-silencing efficiency in the RAW 264.7 cell line and intraperitoneal macrophages, respectively. Intravenous administration of FS14-NP/siRNA led to rapid accumulation of siRNA in macrophages within the arthritic joints. Furthermore, FS14-NP/siIL-1β treatment lowered the expression of pro-inflammatory cytokines in arthritic joints and dramatically attenuated ankle swelling, bone erosion, and cartilage destruction.

Pyr01 is a targeted activator of cell kill (TACK) and shows more than 300-fold more potent than doravirine and also retains reverse transcriptase (RT) inhibition activity within about 3-fold of doravirine.

Lipid 8 iLNPs were used to deliver CRISPR-Cas9 mRNA and sgRNA which targeted to the PLK1 gene. The safety and excellent intracerebral diffusion performance of lipid 8 iLNPs ensured that the survival of murine glioblastoma multiforme (GBM) mice was extended. The median survival was extended by approximately 50% and the overall survival was increased by 30%. The treatment of metastatic adenocarcinoma was executed by the EGFRtargeted lipid 8 iLNPs. These iLNPs possessed the ability of tumor targeting, which could increase the accumulation of CRISPR-Cas9 mRNA and sgRNA within the tumor cells. After a single intraperitoneal administration,
80% PLK1 gene was edited and the overall survival of mice with high-grade ovarian cancer malignant ascites was enhanced by
80% . These results demonstrate the clinical potential of CRISPR-Cas9 gene editing system can be delivered by iLNPs for treating tumors, and provide new ideas for tumor gene therapy.

FX-909（FX 909） is a first-in-class inverse agonist of the peroxisome proliferator-activated receptor gamma (PPARG) lineage transcription factor with EC50 of 1 nM and shows >2000-fold selectivity for PPARG over PPARA/PPARD - acting through a mechanism that promotes a repressive conformation of PPARG.

BAY-2965501 is a first-in-class a diacylglycerol kinase zeta (DGKζ, lipid kinase) inhibitor with IC50 of 27 nM/35 nM (human/mouse) and shows >20-fold selectivity for DGKζ over other DGK isotypes. BAY-2965501 blocks DGKζ in T-cells to activate them

ARV-766 is an orally active and potent proteolysis targeting chimera (PROTAC) protein degrader. ARV-766 degrades wild-type androgen receptor (AR) but also relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations[1].

M3913 is an antitumor compound.

TNG260 is a CoREST-selective deacetylase inhibitor and shows 500-fold selectivity for the CoREST complex over the other HDAC1-containing complexes, NuRD and Sin3.

ZW251 is an antibody drug conjugate (ADC) consisting of a topoisomerase l inhibitor payload conjugated to an antibody targeting Glypican-3(GPC3).

MRT-2359 a potent, selective and orally bioavailable GSPT1-directed molecular glue degrader (MGD).

RMC-6291 is a potent covalent inhibitor of KRASG12C(ON) that forms a tri-complex within tumor cells between KRASG12C(ON) and cyclophilin A (CypA). RMC-6291 overcomes limitations of first-generation KRASG12C(OFF) inhibitors in preclinical models by directly targeting the active form of this important oncogenic driver.

DT-109 is a glycine-based tripeptide (Gly-Gly-Leu) that lowers steatohepatitis and hepatic fibrosis via induction of fatty acid (FA) degradation and antioxidant defense through de novo glutathione (GSH) biosynthesis.

Camlipixant (BLU-5937) a potent, selective, non-competitive and orally active P2X3 homotrimeric receptor antagonist with an IC50 of 25 nM against hP2X3 homotrimeric. Camlipixant shows potent anti-tussive effect and no taste alteration. Camlipixant can be used for the research of unexplained, refractory chronic cough.

UCM1306 is a potent and orally active human dopamine D1 receptor allosteric modulator (PAM). UCM-1306 increases the endogenous dopamine (DA) maximal effect both in human and mouse D1 receptors. UCM-1306 is not only for improving motor symptoms but also for addressing the key comorbid cognitive impairment associated with long-term Parkinson’s disease (PD).

MS023 hydrochloride is a potent, selective and cell-active inhibitor of human type I protein arginine methyltransferases (PRMT), with IC50 values of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.

SU056 is an inhibitor of Y box binding protein 1 (YB-1) with IC50 of 1.73 μM in Sk0V3 cells.

Usp22i-S02(USP22-IN-1, compound S02) is a potent inhibitor of ubiquitin specific peptidase 22 (USP22). It showed anticancer activity by suppressing Foxp3 expression in T-regulatory cells.

Zuranolone(SAGE-217, CS-2797) is an orally active and potent neuroactive steroid and positive allosteric modulator of the GABAA receptor, with EC50s of 296 nM for α1β2γ2 receptor.

LNP023 is a highly potent factor B (FB) inhibitor with an IC50 value of 10 nM. LNP023 shows direct, reversible, and high-affinity binding to human FB (KD=7.9 nM).

8-Azaadenosine is a potent ADAR1 inhibitor and an A-to-I editing inhibitor. 8-Azaadenosine blocks RNA editing and inhibits proliferation, 3D growth, invasion, and migration in thyroid cancer cells.

AL-A12 is an ionizable cationic amino lipid that has been used in the formation of lipid nanoparticles (LNPs).1 LNPs containing AL-A12 and encapsulating minicircle DNA that encodes for GFP have been used to induce GFP expression in Huh7 cells.

D-Lin-MC4-DMA(MC4) is a cationic lipid that has been synthesized for Lipid nanoparticles (LNPs) to deliver the siRNA.

D-Lin-MC2-DMA(MC2) is a cationic lipid that has been synthesized for Lipid nanoparticles (LNPs) to deliver the siRNA.

WAY-299801 is an antiacterial agent. WAY-299801 showed interesting in vitro antimycobacterial activity against some strains of Mycobacterium and clin. isolates of M. tuberculosis.

DSG-PEG2000 is used for liposome preparation. DSG-PEG, MW 2,000 has become known for lipid nanoparticle (LNP) preparation for siRNA (small interfering RNA) delivery research. .

WAY-313013 is a p38a Mitogen-Activated Protein Kinase inhibitor.

WAY-640810 is a chemical agent which may alter the lifespan of a eukaryotic organism.

AD-57, also known as KIRA 1, is an IRE1 inhibitor for cancer inflammation autoimmune disease therapy.

DCFH, also known as 2',7'-dichlorodihydrofluorescein, is a fluororescent agent. It is a key chemcial for the dichlorofluorescin (DCFH) oxidation assay.

HHS-0701, a sulfur-triazole exchange (SuTEx) ligand, is a potent tyrosine-reactive prostaglandin reductase 2 (PTGR2) inhibitor. HHS-0701 blocks PTGR2 metabolism of the lipid substrate 15-Keto-PGE2.

Moracin C is a phenolic compound isolated from Artocarpus heterophyllus. Moracin C suppresses Lipopolysaccharide-Activated Inflammatory Responses in Murine Raw264.7 Macrophages.

BDTX-1535 is a potent, selective, brain penetrant and irreversible MasterKey inhibitor of EGFR mutations that expressed in glioblastoma multiforme (GBM) and intrinsic and acquired resistance EGFR mutations in non-small cell lung cancer (NSCLC).

NSC321039, also known as hMAO-B-IN-4, is a selective, reversible and blood–brain barrier (BBB) penetrable human monoamine oxidase-B (hMAO-B) inhibitor with an IC50 value of 0.067 μM.

WAY-658513 is a multiple kinase inhbitor. WAY658513 was shown to inhibit ROCK I, ERK2, GSK3, and PKA with Ki <1 μM.

RXN00442, also known as EGFR-IN-11, is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI). This compound was first reported in Eur J Med Chem.

WAY-299838 is a useful chemical agent for chemical synthesis of hypoxia-inducible factor-1 inhibitor.

HUN39963, also known as LDH-IN-2 is an inhibitor of glycolate oxidase. This compound was first reported in J Med Chem.

ZVN26391, also known as NLRP3-IN-10, is a IL-1β inhibitor for the treatment of inflammation and inflammation-related disease (neurogenic inflammation, Alzheimer disease, etc.).

CUN11141, also known as BRD4 Inhibitor-20, is a potent orally active bromodomain protein 4 (BRD4) inhibitor. It can be used for the research of kinds of cancer, such as colon cancer.

GSK3β Inhibitor II, also known as KIN 001-042, also known as GSK-3β Inhibitor II, is a GSK-3β inhibitor.

VUN28691, also known as p38α inhibitor 3, is a p38α inhibitor for treatment of p38-α kinase-mediated conditions.

DUN51106, also known as USP8-IN-3, is a deubiquitinase USP8 inhibitor (IC50 = 4.0 μM) for treatment of malignant tumors.

DKI5, also known as (E)-N’-benzylidenehydrazinecarbothiohydrazide, is a LOX-1 inhibitor with an IC50 value of 22.5 μM. DKI5 strongly inhibits lipid peroxidation.

J 3-54 , also known as LSD1-IN-24, is a selective LSD1 inhibitor with IC50 = 0.247 μM. VUN34592 can mediate the expression of PD-L1, enhance T cell killing response, and can be used in cancer research.

CAY10462 is the hydrochloride salt of CAY10434 and selective inhibitor of the 20-HETE synthase CYP4A11 exhibiting an IC50 of 8.8 nM when tested in human renal microsomes.4 CAY10434 is nearly 200 times less potent as an inhibitor of 1A, 1C, and 3A CYP450.

ThioLox is a competitive 15-lipoxygenase-1 (15-LOX-1) inhibitor. ThioLox shows anti-inflammatory and neuroprotective properties.

Pomalidomide-piperazine is an active compound that can be used to synthesis the E3 ligand for PROTAC.

BRD-K56819078 is a small-molecule senolytics and significantly decreases senescent cell burden and mRNA expression of senescence-associated genes in the kidneys of aged mices.

RM133-3 is an ionizable lipid for potent functional mRNA delivery in vivo. The LPN formulation RM133-3-21, is found to be roughly 4.5 times more potent than DLin-MC3-DMA.

FTX-6746 is an orally active PPARG inhibitor. FTX-6746 shows potent tumor inhibition in mouse xenograft models.

1,2-Distearoyl-sn-glycero-3-phosphorylglycerol is used as a component of a loposomal delivery system that coordinates the release of irinotecan and floxuridine in vivo. It is also used to encapsulate anthracyclines and deliver them to tumors.DSPG has a high transition temperature and has therefore found much use in liposomal drug delivery systems.

CFT8634 is an oral activity degrader targeting BRD9 extracted from patent WO2021178920A1 compound 174. CFT8634 can be used for the research of synovial sarcoma and SMARCB1-deleted solid tumors.

BAY-7081 is a Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor with very good aqueous solubility.

CFT1946 is an orally active and selective target ligand for BRAF kinase.

KT-474 is a highly active and selective, orally bioavailable IRAK4 degrader being developed for the treatment of toll-like receptor (TLR)/interleukin-1 receptor (IL-1R)-driven immune-inflammatory diseases.

MK-8189 is a potent, orally active and selective PDE10A inhibitor with a Ki value of 29 pM. MK-8189 can be used in research of schizophrenia.

CEE321 is a potent pan JAK inhibitor in enzyme and cellular assays (IC50 = 54 nM). CEE321 potently inhibited biomarkers relevant to atopic dermatitis.

CZS-241 is a Potent, Selective, and Orally Available Polo- Like Kinase 4 Inhibitor for the Treatment of Chronic Myeloid Leukemia.

AK-2292 is a Potent and Selective STAT5 PROTAC Degrader with Strong Antitumor Activity In Vivo in Acute Myeloid Leukemia.

BI 3231 is a potent and selective hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13) inhibitor, with IC50s of 1 and 13 nM for hHSD17B13 and mHSD17B13, respectively.

BAY-805 is a potent and selective USP21 inhibitor. BAY-805 is a non-covalent inhibitor with low nanomolar affinity for USP21 and high selectivity over other DUB targets as well as kinases, proteases, and other common off-targets.

BGB-8035 is a Highly Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase (BTK IC50 = 1.1 nM)for B‑Cell Malignancies and Autoimmune Diseases.

IPG7236 is a CCR8 antagonist that through the modulation of regulatory T-cells and cytotoxic T (CD8+ T) cells, displays anticancer effects. IPG7236 is currently undergoing Phase 1 clinical trials in the treatment of advanced solid tumors.

BAY6096, a potent, selective, and highly water-soluble α2B antagonist with IC50 = 14 nM.

A2A receptor antagonist 1 is an antagonist of both adenosine A2A receptor and A1 receptor with Kis of 4 and 264 nM, respectively.

Lipid 10 is a novel ionizable cationic lipid be used for delivery of therapeutic RNA to the Bone Marrow in Multiple Myeloma Using CD38-Targeted with Lipid 10-LNP.

YCT529 is a potent, selective and orally active RAR-α inhibitor.

LP0200 is the prodrug of the oral allosteric IL-17A inactivator.

GLPG2534 is an IRAK4 inhibitor for use as a therapeutic for inflammatory skin diseases.

TP0473292 is an adamantane carboxylic acid ester prodrug of TP0178894, a metabotropic glutamate 2 and 3 receptor antagonist for use as an antidepressant. TP0473292 has undergone phase 1 clinical trials for treatment of depression.

Overview. A common route of resistance to tuberculosis involves Mtb erm37 expression, which expresses an RNA methyltransferase that methylates the A2058 position of the 23S ribosome RNA, hindering macrolide antibiotic binding.

QR-6401 is a highly potent and selective macrocyclic CDK2 inhibitor with IV50 of 0.37 nM. QR-6401 exhibits good selectivity against other closely related kinases, such as CDK1, CDK4, CDK6, CDK9 and GSK3β. QR-6401 demonstrates robust antitumor efficacy in an OVCAR3 ovarian cancer xenograft model via oral administration.

BDM2(Newly disclosed HIV-1 antiretroviral) is the first integrase-LEDGF/p75 allosteric HIV-1 inhibitor to clear Ph.

A protein-protein interaction inhibitor for a challenging-to-drug master transcription factor.

LY3154885 is a Human Dopamine D1 Receptor Positive Allosteric Modulator (D1 PAM EC50 = 11.7 nM) with an Improved Nonclinical Drug−Drug Interaction Risk Profile.

AZ13824374 is a highly potent and selective ATAD2 inhibitor which shows cellular target engagement and antiproliferative activity in a range of breast cancer models.

MAP855 is a novel highly potent and selective MEK1/2 kinase inhibitor with equipotent inhibition of WT and mutant MEK1/2, whose drug-like properties allow further investigation in the mutant MEK setting upon BRAF/MEK therapy.

”Compound 53” (University of Texas Southwestern Medical Center) is a stimulator of interferon (IFN) genes (STING) agonist.

TXA6101 is an FtsZ inhibitor that is associated with potent activity against clinical isolates of methicillin-resistant Staphylococcus aureus (MRSA) that are resistant to current standard-of-care antibiotics.

“compound 4e” (Chiesi Farmaceutici) is an inhaled p38α/β mitogen-activated protein kinase (MAPK) inhibitor being developed for lung inflammatory diseases.

MAGLi 432 is a novel, reversible monoacylglycerol lipase (MAGL) inhibitor.

HHS-166 shows dose-dependent inhibition of arsenite-induced stress granule (SG) formation, and liganded G3BP1 Y40 in the NTF2 dimerization domain of this essential nucleating protein for SG regulation.

AHL-030 is a potent and selective EDC3-targeted ligands. AHL-030 is also an stress granules (SGs) enhancer and results in a 2-fold increase in SGs per arsenite-treated cell.

MK-0159 is a CD38 enzymatic inhibitor. Mice treated with MK-0159 show strong protection from myocardial damage upon cardiac I/R injury compared to those treated with NAD+ precursors (nicotinamide riboside) or another CD38 inhibitor.

RP-6306 is a PKMYT1 inhibitor extracted from patent WO2021195781A1 compound 182. RP-6306 can be used for the research of cancer.

Dalzanemdor (SAGE-718) is a N-methyl-D-aspartate (NMDA) receptor positive allosteric modulator.

BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC50= 5 nM. BI-4142 showed efficacy against HER2 exon 20 insertion-driven tumors, while preserving EGFR wt signaling.

GST-HG131 is a specific inbihitor of hepatitis B virus (HBV) surface antigen, belongs to dihydrobenzopyridooxazepine (DBP) series. GST-HG131 exhibits excellent and specific HBV antigens inhibition with EC50 of 28.2 nM (HBsAg) and 16.0 nM (HBeAg), respectively, but also it is safety for animal.

AZD-1656 is a glucokinase (GK) activator potentially for the treatment of type 2 diabetes and obesity.

JNJ-64264681 is a covalent, irreversible BTK inhibitor with potent whole blood activity and exceptional kinome selectivity. JNJ-64264681 demonstrated excellent oral efficacy in both cancer and autoimmune models with sustained in vivo target coverage amenable to once daily dosing and has advanced into human clinical studies to investigate safety and pharmacokinetics.

AN15368 (AN 15368) is a small molecule prodrug activated by parasite carboxypeptidases to yield a compound that targets the messenger RNA processing pathway in Trypanosoma cruzi (T. cruzi), exhibits potent in vitro activity against T.

Sirpiglenastat (DRP-104) is a broad acting glutamine antagonist. Sirpiglenastat has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response.

ENT-01 shows promise in the treatment of constipation in those with Parkinson's disease (PD) by preventing or reducing the formation of αS aggregates that form in enteric neurons. ENT-01 has undergone Phase 2b clinical trials to evaluate the safety and efficacy of the orally administered drug for the alleviation of constipation in those with PD.

compound 27, is a potent (13 nM) CNS-penetrant compound that reduces very long chain fatty acid (VLCFA) levels in the CNS, which are believed to be pathological in the rare disease adrenoleukodystrophy (ALD). The starting point came from an HTS on compounds from an internal collection.

“Compound 14d” (Shionogi & Co.) is a highly potent, dose-dependent adenosine monophosphate activated protein kinase (AMPK) activator being investigated for its blood-glucose-lowering effects.

BI685509 is a soluble guanylate cyclase (sGC) activator taken orally, with potential to treat diabetic and kidney diseases. In both rat and human platelets, BI685509 was found to restore/enhance cGMP, but had no effect on the functionality of nitric oxide pathways. BI685509 is currently undergoing phase 2 trials for the treatment of diabetic nephropathy, with the aim of improving kidney function.

DN-1289 is a potent and selective dual DLK/LZK inhibitor. DN1289 demonstrated excellent in vivo plasma half-life across species and is anticipated to freely penetrate the central nervous system with no brain impairment based on in vivo rodent pharmacokinetic studies and human in vitro transporter data. Proximal target engagement and disease relevant pathway biomarkers were also favorably regulated in an in vivo model of amyotrophic lateral sclerosis.

“Compound 6” (Novartis) is a first-in-class YAP-TEAD protein-protein inhibitor. The TEAD transcription factor and its coactivator YAP and WWTR1/TAZ of the Hippo pathway are responsible for directly regulating the expression of genes involved in cell proliferation and organ size.

Overcoming FGFR mutation resistance and FGFR1-mediated hyperphosphatemia toxicity through isoform-selective FGFR2/3 inhibition. “Compound 29” is an ATP-competitive fibroblast growth factor receptor (FGFR) 2/3 inhibitor with subnanomolar potency.

BI-3231 is a novel potent and selective HSD17B13 inhibitor with IC50 of 1 nM and Ki of 0.7 nM, respectively. BI-3231 is a valuable chemical probe to further elucidate the biological function of HSD17B13.

OICR-8268 is a small molecule ligands that target DCAF1 and shows the highest affinity for binding to the DCAF1 WDR domain with SPR KD of 38 nM. OICR-8268 is an excellent tool compound to enable the development of next-generation DCAF1 ligands toward cancer therapeutics.

PUM00199, also known as PARP10-IN-3, is a selective mono‐ADP‐ribosyltransferase PARP10 inhibitor with an IC50 of 480 nM for human PARP10.

KR-32568 is an inhibitor of the sodium-hydrogen exchanger isoform-1 (NHE-1; IC50 = 230 nM). It restores cardiac contractile function ex vivo in an isolated ischemic rat heart model when used at a concentration of 10 μM.

TCS 46b is an orally active, subtype-selective GluN1A/GluN2B NMDA receptor antagonist

SBS is a useful probe and tool molecule for detecting amyloid deposits in systemic amyloidosis in vitro and in vivo. SBS can be used for detecting amyloid fibrils in autopsy and biopsy samples from patients with localized amyloidosis, such as familial prion disease, and systemic amyloidosis, such as familial amyloidotic polyneuropathy, amyloid A (AA) amyloidosis, light chain (AL) amyloidosis, and dialysis-related amyloidosis.

SJ3149 is a uniquely potent and selective CK1α degrader with DC50 of 3.7 nM. SJ3149 shows high activity across a range of acute leukemia (AL) cell lines derived from different hematologic neoplasms, such as B-cell and T-cell acute lymphoblastic leukemia. SJ3149 activity shows a strong correlation with wild-type TP53 expression.SJ3149 (SJ-3149) is uniquely potent and selective CK1α degrader with DC50 of 3.7 nM and Dmax 95% in MOLM-13 cells, potently inhibits the viability of MOLM-13 cells with IC50 of 13 nM. SJ 3149 shows a broad antiproliferative profile on a panel of AML and ALL cell lines with IC50 values in a single digit nanomolar range, and even sub-nanomolar activity. SJ-3149 also potently inhibited the viability of multiple cell lines derived from solid tumors, including breast, soft tissue, and tumors of the male and female reproductive system, with several cell lines being inhibited more potently than MOLM-13. SJ3149 also inhibits several TP53-altered cell lines, such as BT-20 and KU812.

UCL-TRO-1938 is a small-molecule activator of the PI3Kα isoform with EC50 of 60 μM. UCL-TRO-1938 activats PI3Kα but not PI3Kβ or PI3Kδ and effectively boosts endogenous protective and regenerative signalling.

MIC1 is a set of multi-charged lipids with four tertiary amino nitrogen atoms (4N4T) which could be constructed and applied to form novel lipid nanoparticles. 4N4T-LNPs based on MIC1 exhibit much higher mRNA translation efficiency than the approved SM-102-LNPs. 4N4T-LNPs are successfully applied to DS mRNA vaccine and the vaccines worked well against SARS-CoV-2 and its variants, including Delta and Omicron.

MIC2 is a set of multi-charged lipids with four tertiary amino nitrogen atoms (4N4T) which could be constructed and applied to form novel lipid nanoparticles. 4N4T-LNPs based on MIC2 exhibit much higher mRNA translation efficiency than the approved SM-102-LNPs. 4N4T-LNPs are successfully applied to DS mRNA vaccine and the vaccines worked well against SARS-CoV-2 and its variants, including Delta and Omicron.

NFAT:AP-1 inhibitor-10 is a novel inhibitor of the NFAT:AP-1:DNA interaction on the ARRE-2 element, binding to DNA in a sequence-selective manner and inhibiting the transcription of the Il2 gene and several other cyclosporin A-sensitive cytokine genes important for the effector immune response.

GNE-8505 is a DLK inhibitor (IC50 = 10nM).

CDK2-IN-3 (compound 3) is a potent and selective CDK2 inhibitor with an 50 of 60 nM.

VU0652835 is a metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC50 of 81 nM.

PF-4211 is a potent D1 receptor agonist.

Pseudouridimycin (PUM), an antibiotic, is a selective bacterial RNA polymerase (RNAP) inhibitor. Pseudouridimycin is a C-nucleoside analogue that is effective against both Gram-negative and Gram-positive bacteria.

HMG499 is a potent and selective HMG-CoA reductase inhibitor.

SGL5213 is a potent, oral active and low-absorbable sodium-dependent glucose cotransporter 1 (SGLT1) inhibitor, with IC50 values of 29 nM and 20 nM for hSGLT1 and hSGLT2, respectively. SGL5213 has potential to treat type 2 diabetes treatment.

(S)-DO271 is an inactive control for the α/β-hydrolase domain-containing protein 12 (ABHD12) inhibitor DO264.

JNJ-64326067 is a potent and selective binder to aggregated tau with a favorable pharmacokinetic profile and no apparent off-target binding. This was confirmed in rat and monkey positron emission tomography studies using [18F]-JNJ-64326067.