Tafluprost ethyl amide is a prostaglandin derivative. Tafluprost ethyl amide is capable of intraocular pressure (IOP) reduction and influencing eyelash growth. Tafluprost ethyl amide can be used in antiglaucoma ophthalmic compositions or cosmetics.

SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM, 100-fold more selective for ALK5 than p38 MAPK and other kinases.

Mc-Val-Cit-PABC-PNP is a cathepsin cleavable ADC peptide linker. For example, FDA approved drug, brentuximab vedotin, adopts this linker.

SBI-797812 is an orally active nicotinamide phosphoribosyltransferase (NAMPT) activator. SBI-797812 shifts NAMPT to NMN formation, increases NAMPT affinity for ATP, stabilizes phosphorylated NAMPT, promotes consumption of the pyrophosphate by-product, and blunts feedback inhibition by NAD+. SBI-797812 increases intracellular nicotinamide mononucleotide (NMN) and elevates liver NAD+ in mice.

ABC294640 is an orally available, aryladamantane compound and selective inhibitor of sphingosine kinase-2 (SK2) with potential antineoplastic activity.

ACBI3 is a selective, potent and in vivo active pan-KRAS PROTAC degrader, potently degrades 13 out of 17 of the most prevalent oncogenic KRAS alleles (DC50=3.9 nM in GP2d cells).

Cbl-b-IN-10 (Compound 463) is a casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl inhibitor with IC50s of 6.0 nM and 3.5 nM, respectively.

TEAD activator Q2 (Quinolinol Q2) is a small molecule activator of TEAD with EC50 of 2.6 uM in TEAD dual-luciferase reporter (DLR) assays, inhibits TEAD-palmitate interaction with IC50 of 1.7 uM.

SW106 is a potent, selective, competitive PTH/PTH-related peptide receptor (PPR) antagonist with IC50 of 0.99 uM.

CH5447240 is a novel potent, selective, orally active hPTHR1 agonist with EC20 of 3.0 nM and EC50 of 12 nM.

Naltriben is a highly selective δ2 opioid receptor antagonist.Naltriben (NTB) has been used to differentiate the subtypes of delta opioid receptors, delta1 and delta2. NTB displaced the specific binding of [3H]DAMGO with Ki value of 19.79 +/- 1.12 nM in rat cortex membranes. Specific binding of [3H]diprenorphine ([3H]DIP) was inhibited by NTB with Ki value of 82.75 +/- 6.32 nM in the presence of DAMGO and DPDPE. Naltriben enhanced the MAPK/ERK signaling pathway, but not the PI3k/Akt pathway. Therefore, potentiated TRPM7 activity contributes to the devastating migratory and invasive characteristics of GBM.

Novel pendrin inhibitor, attenuating airway hyperresponsiveness and mucin expression in experimental murine asthma

DRAinh-A250 is a specific inhibitor of Cl-/anion exchanger SLC26A3 (DRA), fully and reversibly inhibits SLC26A3-mediated Cl- exchange with HCO3-, I-, and thiocyanate (SCN-) with IC50 of ~0.2 uM.

PAT1inh-A0030 is a potent and selective SLC26A6 (putative anion transporter 1, PAT1) inhibitor with IC50 of 1.0 uM, shows no activity on relevant ion transporters/channels (SLC26A3, SLC26A4, SLC26A9, CFTR, TMEM16A).

1PBC is a small molecule blocker of calcium-activated chloride channel TMEM16A, blocks TMEM16A completely with an IC50 of 4 uM at zero mV and saturating Ca2+ concentration (2 uM).

Survodutide (BI 456906) is a potent, selective glucagon receptor/GLP-1 receptor (GCGR/GLP-1R) dual agonist with EC50s of 0.52 nM and 0.33 nM in CHO-K1 cells, respectively. Survodutide, a 29-amino-acid peptide, is a potent acylated peptide containing a C18 fatty acid. Survodutide has robust anti-obesity efficacy achieved by increasing energy expenditure and decreasing food intake.

Pasireotide (SOM230), a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity. At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Pasireotide acetate) usually boasts enhanced water solubility and stability.

Albiglutide is a glucagon-like peptide-1 agonist (GLP-1 agonist).

Semaglutide acetate, a long-acting GLP-1 analogue, is a glucagon-like peptide-1 (GLP-1) receptor agonist. Semaglutide acetate has the potential for type 2 diabetes treatment.

TMinh-23 is (Compound 10bm) is a potent, selective inhibitor of transmembrane protein 16A (TMEM16A or ANO1, DOG1, ORAOV2, TAOS-2) with IC50 of 30 nM in short-circuit current assays, weakly inhibits TMEM16B (IC50=400 nM, 13 -fold selectivity).

NSC74429 is a CNS-active, small molecule PHLPP inhibitor with IC50 of <5 uM, shows neuroprotective activity in primary rat cortical neurons in STS assay.

Compound 12f (LPA1 antagonist) is a potent and highly selective LPA1 antagonist with IC50 of 16.0 nM (cAMP assay) and 18.4 nM (calcium mobilization assay), respectively.

R1-ICR-5 is a highly selective and efficacious PROTAC degrader of both human and murine RIPK1.

A-910 is a orally bioavailable, highly potent and selective dual MerTK/Axl inhibitor with IC50 of 0.3 nM/0.8 nM. A-910 exhibits favorable oral bioavailability, exceptional kinome selectivity, and significantly improved in MerTK Ba/F3 xenograft tumor model.

Compound 13 (MET inhibitor) is a selective, potent, and mutant-active MET inhibitor with a MET D1228N cell line IC50 of 23 nM and shows good efficacy in the MET-D1228N Type I resistance mutation model.

Arvanil is a CB1 and TRPV1 agonist. It increases lung tidal volume, diaphragm activity, mean arterial blood pressure and inhibits lymphocyte proliferation.

Palvanil is a capsaicin analogue, shows strong desensitizing capability against the TRPV1 receptor. Palvanil shows anti-nociceptive and anti-inflammation effects.

CB31 is a highly potent and orally bioavailable PD-L1 inhibitor with IC50 of 0.2 nM (PD-1/PD-L1 alphs) and EC50 of 15 nM (NFAT), with high passive permeability, good metabolic stability and favorable oral PK. CB31 targets both the surface and intracellular PD-L1, reducing tumor size and killing cells in a 3D spheroid model.

AZ'3137 is an orally bioavailable androgen receptor (AR) degrader that recruit the Cereblon (CRBN) E3 ligase with DC50 of 22 nM (LNCaP) and 92 nM (LNCaP L720H), respectively.

CID-2858522 is a selectively inhibits protein kinase C (PKC)-induced activation of the NF-κB pathway (IC50 < 0.1 μM for PMA-stimulated IL-8 production).