SKF-96365 is a selective TRPC channel blocker. SKF-96365 activates cytoprotective autophagy to delay apoptosis in colorectal cancer cells through inhibition of the calcium/CaMKIIγ/AKT-mediated pathway. SKF-96365 strongly inhibits voltage-gated sodium current in rat ventricular myocytes. SKF 96365 inhibits glioblastoma cell growth by enhancing reverse mode of the Na(+) /Ca(2+) exchanger and increasing intracellular Ca(2+). SKF-96365 attenuates toxin-induced neuronal injury through opposite regulatory effects on Homer1a and Homer1b/c in cultured rat mesencephalic cells.

ROS-IN-1 is a mitochondrial ROS inhibitor.

LSD1-IN-23 is a competitive/non-competitive mixed inhibitor of lysine specific demethylase 1 (LSD1)

Omadacycline, also known as PTK 0796 and Amadacyclin, is a novel first-in-class aminomethylcycline with potent activity against important skin and pneumonia pathogens, including community-acquired methicillin-resistant Staphylococcus aureus (MRSA), β-hemolytic streptococci, penicillin-resistant Streptococcus pneumoniae, Haemophilus influenzae, and Legionella. Omadacycline is active against strains expressing the two main forms of tetracycline resistance (efflux and ribosomal protection). The primary effect of omadacycline is on bacterial protein synthesis, inhibiting protein synthesis with a potency greater than that of tetracycline. The binding site for omadacycline is similar to that for tetracycline.

MAO-B-IN-22 (compound 6h) is a potent MAO-B inhibitor

Normetanephrine is a metabolite of norepinephrine created by action of catechol-O-methyl transferase on norepinephrine. It is excreted in the urine and found in certain tissues. It is a marker for catecholamine-secreting tumors such as pheochromocytoma.

PNU282987 is a drug that acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors. In animal studies, it shows nootropic effects, and derivatives may be useful in the treatment of schizophrenia, although PNU-282,987 is not suitable for use in humans because of excessive inhibition of the hERG antitarget.

KSK68 is a Histamine H3 and Sigma‑1 Receptor Ligand, which may be useful in the Treatment of Nociceptive and Neuropathic Pain

KSK94 is a high-affinity histamine H3 receptor antagonist.

MK-212 is a 5HT2C-receptor agonist. A dose-dependent the effect of 5HT2C-receptor agonist MK-212 on mouse behavior was demonstrated. Intraperitoneal injection of MK-212 in high doses (0.5 and 1.0 mg/kg) increased blood level of corticosterone in mice and reduced their motor activity. In low doses of 0.1 and 0.2 mg/kg, the agonist reduced anxiety, but had no effect on motor activity. It is hypothesized that low doses of MK-212 exhibited anxiolytic activity in mice.

TRK-IN-22 (compound 11) is a TRK inhibitor.

DRI-C21041 is a CD40/CD40L interaction inhibitor

Nacubactam, also known as RG-6080, FPI-1459, and OP-0595, is a beta-lactamase inhibitor used for treating bacterial infections.

α-Glucosidase-IN-22 (compound 7i), a benzimidazole, is a potent α-glucosidase inhibitor.

SID-852843 is a WNV NS2B-NS3 proteinase inhibitor.

CYP1B1-IN-4 is a 2,4-diarylthiazole compound with selectively CYP1B1 inhibition.

4-PPBP is a σ ligand and selective non-competitive antagonist at recombinant NR1a/2B NMDA receptors expressed in Xenopus oocytes. 4-PPBP protects against newborn excitotoxic brain injury by stabilizing the mitochondrial membrane potential in vitro and inhibiting microglial activation in vivo. 4-PPBP modulates neuronal nitric oxide synthase/postsynaptic density-95 coupling mechanisms and protects against neonatal ischemic degeneration of striatal neurons.

PROTAC MDM2 Degrader-2 is a MDM2 degrader based on PROTAC technology.

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.

LY 235959 is a competitive NMDA receptor antagonist.

PARP-1-IN-4 is a PARP-1 inhibitor.

Beloxepin, also known as ADL-6906; ORG-4428, is an oral dual selective serotonin and norepinephrine uptake inhibitor.

CDK8-IN-12 is an orally active, potent CDK8 inhibitor.

PDCD4-IN-1(compound 20031600) is a PDCD4 inhibitor.

LY 43578 is an aromatase inhibitor.

HT-61, also known as HY-50A, is a pyrroloquinolone antibiotic potentially for the treatment of staphylococcal infections. HT61 was effective at reducing biofilm viability and was associated with increased expression of cell wall stress and division proteins, confirming its potential as a treatment for S. aureus biofilm infections. HT61 enhances the effect of tobramycin against Pseudomonas aeruginosa in vitro and in vivo.

VU0364572 TFA is an orally active and selective allosteric agonist of the M1 muscarinic receptor.

SHP099 is a potent, selective, orally bioavailable, and efficacious SHP2 inhibitor with IC50 =0.07 μM and p-ERK modulation in cells IC50 = 0.250 μM. SHP099 exhibits dose-dependent pathway inhibition and antitumor activity in xenograft models. SHP2 is a nonreceptor protein tyrosine phosphatase (PTP) encoded by the PTPN11 gene involved in cell growth and differentiation via the MAPK signaling pathway. SHP2 also purportedly plays an important role in the programmed cell death pathway (PD-1/PD-L1). Because it is an oncoprotein associated with multiple cancer-related diseases, as well as a potential immunomodulator, controlling SHP2 activity is of significant therapeutic interest.

VU0364572 free base is an orally active and selective allosteric agonist of the M1 muscarinic receptor.

Tubulin inhibitor 32 is a potent and orally active tubulin inhibitor.