Afelimomab (MAK 195F) is an anti-tumor necrosis factor F(ab')2 monoclonal antibody fragment. Afelimomab can be used for the research of sepsis.

Aselizumab (HuDreg-55) is an humanized IgG4 mAb against L-selectin. However, L-selectin (CD62L) is a cell adhesion molecule expressed on circulating neutrophils. It regulates migrating cells to chemotaxis towards the site of injury. Aselizumab may be account for a high rate of infections and leucopenia after truma.

Nirsevimab (MEDI8897) is a recombinant monoclonal antibody against human respiratory syncytial virus (RSV). Nirsevimab has neutralizing activity against RSV A and RSV B viruses, with IC50 values of 5.42 ng/mL and 9.71 ng/mL, respectively. Nirsevimab can be used for research on respiratory infections.

Raxibacumab (ABthrax) is a human IgG1 monoclonal antibody against Bacillus anthracis protective antigen (PA). Raxibacumab blocks the toxin’s deleterious effects by preventing binding of the protective antigen component of the anthrax toxin to its receptors in host cells, thereby blocking the toxin’s deleterious effects. Raxibacumab can be used for anti-anthrax research.

Tesofensine (NS-2330) is a triple monoamine reuptake inhibitor inducing a potent inhibition of the re-uptake process in the synaptic cleft of the neurotransmitters dopamine (DA; IC50=6.5 nM), norepinephrine (NE;IC50=1.7 nM), and serotonin (5-HT;IC50=11 nM), and with potentials as an anti-obesity agent. Tesofensine is a CNS acting anti-obesity agent.

AC-7954 is a selective nonpeptidic urotensin receptor agonist (EC50: 300 nM at the human UII receptor).

PKCTheta-IN-2 (compound 14) is a potent and selective PKCθ inhibitor with an IC50 of 0.25 nM. PKCTheta-IN-2 shows good selectivity over a wide range of kinases, including the PKC subfamily (30 kinases). PKCTheta-IN-2 inhibits the IL-2 production in a mouse (IC50 of 682 nM).

Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor for the treatment of cancer.

Letrazuril is an anti-HIV agent.

ICI-204448 is a κ-opioid agonist with limited access to the CNS, ICI-204448 can displace the binding of the kappa-opioid ligand 3H-bremazocine from guinea pig cerebellum membranes.

CLK1-IN-3 (compound 10ad) is a potent and selective Clk1 inhibitor, with an IC50 of 5 nM and over 300-fold selectivity for Dyrk1A. CLK1-IN-3 also shows a relatively potent inhibition against Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 potently induces autophagy in vitro. CLK1-IN-3 can be used for acute liver injury (ALI) research.

cyt-PTPε Inhibitor-1 is a potent cytosolic protein tyrosine phosphatase epsilon (cyt-PTPε) inhibitor, binds to the catalytic domain of cyt-PTPε, blocks c-Src activation (dephosphorylation of c-Src), and exhibits anti-osteoclastic activity.

OXA-06 hydrochloride is an ATP-competitive ROCK inhibitor that blocks anchorage-dependent growth and invasion of non-small cell lung cancer cell lines. OXA-06 hydrochloride inhibits cofilin phosphorylation but does not stimulate apoptosis.

mPGES-1-IN-2 (compound III) is a benzimidazole-based mPGES-1 inhibitor that also inhibits adipophysin PGD synthase (I-PGDS) (5 μM, IR=60 %). mPGES-1-IN-2 reduces PGE2 production and tends to reduce levels of other prostaglandins. mPGES-1-IN-2 effectively inhibits acute inflammation in an air sac model stimulated by Carrageenan in mice.

CHK1-IN-3 is a Checkpoint Kinase 1 (CHK1) inhibitor with an IC50 of 0.4 nM.

Tariquidar dihydrochloride (XR9576 dihydrochloride) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1 nM).

SUCNR1-IN-2 (Statement 35) is a succinate/succinate receptor 1 inhibitor for the study of neurodegenerative diseases such as neuroinflammation.

ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect.

NTNCB (Compound 11) hydrochloride is a potent and selective neuropeptide Y Y5 (NPY Y5) receptor antagonist with a Ki of 8 nM against human Y5.

CCR6 inhibitor 1 is a potent and selective CCR6 inhibitor, with IC50s of 0.45 and 6 nM for monkey and human CCR6, much more selective at CCR6 over human CCR1 (IC50, > 30000 nM), and CCR7 (IC50, 9400 nM). CCR6 inhibitor 1 markedly blocks ERK phosphorylation. CCR6 inhibitor 1 is used in the research of autoimmune diseases and cancer.

Mebeverine acid (Mebeverine metabolite Mebeverine acid) is a secondary metabolite of Mebeverine. Mebeverine is an antispasmodic agent. Mebeverine acid is a valuable marker of oral exposure to Mebeverine.

HTMT (dimaleate) is a potent histamine H1 and H2 receptor agonist. HTMT (dimaleate) is 4 x 104 times more active than histamine in H2-mediated effects in natural suppressor cells.

ATC0175 is a novel nonpeptidic and orally active melanin-concentrating hormone receptor 1 (MCHR1) antagonist.

Bevenopran is a peripheral μ-opioid receptor antagonist.

Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α.

Zatolmilast (BPN14770) is a selective phosphodiesterase 4D (PDE4D) allosteric inhibitor with IC50s of 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3, respectively.

BB-22 is a third generation SPICE/K2 cannabinoid wih dopamine (DA) stimulant properties. BB-22 shows affinity to CB1 receptors with a Ki value of 0.11 nM and an EC50 value of 2.9 nM. BB-22 also stimulates CB1-induced [35S]GTPγS binding.