FLX475 is a potent CCR4 antagonist that blocks regulatory T cells that interfere with effective antitumor immune responses and has antitumor activity.

Atrasentan is designed to block the action of endothelin-1; for treating metastatic hormone-refractory prostate cancer.

Arazasetron is an antiemetic which acts as a 5-HT3 receptor antagonist, pKi = 9.27. It is used in the management of nausea and vomiting induced by cancer chemotherapy (such as cisplatin chemotherapy). Azasetron hydrochloride is given in a usual dose of 10 mg once daily by mouth or intravenously. It is approved for marketing in Japan, and marketed exclusively by Torii Pharmaceutical Co., Ltd. under the trade names "Serotone I.V. Injection 10 mg" and "Serotone Tablets 10 mg".

JNJ-54175446 is a potent and selective brain penetrant P2X7 receptor antagonist, with pIC50s of 8.46 and 8.81 for hP2X7 receptor and rP2X7 receptor, respectively.

4BAB (compound 29) is an irreversible glyoxalase I (GLO1) inhibitor. 4BAB has anticancer effects.

Dalcetrapib (JTT-705) is a rhCETP inhibitor with IC50 of 0.2 μM.

Zidesamtinib (NVL-520) is a potent, selective, orally active and brain-penetrant inhibitor of diverse ROS1 fusions and resistance mutations, with IC50s of 0.7 and 7.9 nM for wild-type ROS1 and ROS1 G2032R, respectively, and spares TRK inhibition. Zidesamtinib can be used for the research of cancer.

FR179642 is a key intermediate in the synthesis of the echinocandin antifungal Micafungin. FR179642 is the cyclic peptide nucleus of the echinocandin-like antifungal lipopeptide FR901379.

A highly potent, subtype-selective melanin concentrating hormone receptor 1 (MCHR1) inhibitor with Ki of 17 nM, without inhibitory activity for MCHR2 at 10 uM.

AT-127 is a novel potent, selective nociceptin/orphanin FQ receptor (NOP receptor) agonist with Ki of 1.18 nM.

GpTx-1 is a potent, selective, 34-residue peptide antagonist of Nav1.7 sodium channel with IC50 of 10 nM, displays 20- and 1000- fold selectivity over NaV1.4 and NaV1.5..

GX-674 is a potent, selective Nav1.7 inhibitor with IC50 of 0.1 nM.

JTE-852 is a novel potent, selective, ATP-competitive Syk kinase inhibitor with IC50 of 1.25/1.28 nM for human/rat Syk, respectively.

LSP4–2022 is a novel potent, selective, brain-penetrant mGluR4 agonist with EC50 of 0.11 uM in cell-based assays.

MCL0129 is a selective, potent melanocortin-4 receptor (MC4R) antagonist with Ki of 7.9 nM, without affinity for MC1 and MC3.

PF-05198007 is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 9 nM, no significant activity against Nav1.5 (IC50>10 uM).

Poloppin is a cell-active, small molecule inhibitor of protein-protein interaction via the Polo-box domain (PBD) of the mitotic Polo-like kinase (PLK) with IC50 of 26.9 uM (PLK1) in FP assays.

SR-16507 is a potent full agonist of ORL1 receptor (NOP receptor) and partial agonist of mu-opioid receptor with Ki of 5.22 nM and 1.07 nM, respectively.

An orally available, brain penetrant p75NTR ligand that blocks p75-mediated cell death, also increases proliferation and survival of hippocampal neural progenitors.

D-GsMTx4, a spider peptide, is the D-enantiomer of GsMTx4 (HY-P1410). D-GsMTx4 inhibits the mechanosensitive ion channel Piezo2. D-GsMTx4 can be used for research of mechanical stress.

Difamilast (OPA-15406) is a novel potent, selective phosphodiesterase IV (PDE4) inhibitor with preference for PDE4B (IC50=11.2 nM).

DX600 is a potent and selective peptide inhibitor of angiotensin-converting enzyme 2 (ACE2; Kis = 2.8, 200, and 1,200 nM for recombinant, human, and murine ACE2, respectively).

MSC2360844 is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. MSC2360844 shows highly selective against a panel of 278 additional kinases.

Niraparib, also know as MK-4827, is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. MK4827 inhibits PARP activity, enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. The PARP family of proteins detect and repair single strand DNA breaks by the base-excision repair (BER) pathway.

ALG1001 (Risuteganib, ALG-1001) is a first-in-class, RGD class oligopeptide that inhibits integrin receptors (αvβ3, αvβ5, and α5β1) associated with angiogenesis; ALG1001 inhibits an integrin-mediated pathway of the vitreoretinal interface, connecting the posterior aspect of the vitreous with the internal limiting membrane of the retina. In blocking this pathway, ALG-1001 helps to achieve vitreous breakdown and separation from the retina.

SNS-314 is a synthetic small molecule Aurora kinase (AK) inhibitor with potential antineoplastic activity. Aurora kinase inhibitor SNS-314 selectively binds to and inhibits AKs A and B, which may result in the inhibition of cellular division and proliferation in tumor cells that overexpress AKs. AKs are serine-threonine kinases that play essential roles in mitotic checkpoint control during mitosis.

UNC-2025 is a potent and orally bioavailable dual MER/FLT3 inhibitor with IC50 of 0.74 nM and 0.8 nM, respectively, about 20-fold selectivity over Axl and Tyro3.

Gepotidacin (GSK2140944) is a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor.

Seladelpar sodium salt (MBX-8025) is an orally active, potent and specific PPARδ agonist with an EC50 of 2 nM, showing more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively.

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.