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).

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.

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.

ReACp53 is a cell-penetrating peptide,designed to inhibit p53 amyloid formation.

MBX-4132 a trans translation inhibitor by binding to the bacterial ribosome.

KDOAM25 is a selective inihbitor of the KDM5 family histone demethylases JARID1A, JARID1B, JARID1C and JARID1D with IC50 values < 60 nM.

DBPR114 is a quinazoline-based multi-kinase inhibitor for the treatment of acute myeloid leukemia and other solid tumors.

N-Acetyl lysyltyrosylcysteine amide is a potent, reversible, specific, and non-toxic tripeptide inhibitor of myeloperoxidase (MPO). N-Acetyl lysyltyrosylcysteine amide effectively inhibits MPO generation of toxic oxidants in vivo. N-Acetyl lysyltyrosylcysteine amide reduces neuronal damage and preserves brain tissue and neurological function in the stroked brain. N-Acetyl lysyltyrosylcysteine amide inhibits MPO-dependent hypochlorous acid (HOCl) generation, protein nitration, and LDL oxidation.

PCNA-I1 is an inhibitor of proliferating cell nuclear antigen (PCNA) that binds to PCNA trimers (Kd = 0.41 µM) and dose-dependently reduces the level of PCNA associated with chromatin in PC3 cells.

Selective estrogen receptor modulator (SERM), inhibiting mammalian PLD (PLD1 and PLD2)

KY-04031 is a PAK4 inhibitor with IC50 of 0.79 uM, a basic building block in designing novel imidazo[4,5-b]pyridine-based PAK4 inhibitors..

RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation.

Naxillin is the first non-auxin-like molecule that promotes root branching, activates a subset of auxin-induced transcripts, including AUX/IAA, SAUR and PIN families; induces auxin response in the basal meristem; represents a valuable tool to further decipher the molecular networks involved in lateral root branching.

DFP00173 (DFP-00173) is a potent and selective aquaporin-3 (AQP3) inhibitor, inhibits glycerol permeability in erythrocytes with IC50 of 0.2 uM..

4-Allylcatechol (4-Allylpyrocatechol, Hydroxychavicol) is an intermediate to synthetic safrole.

AG-636 is an orally available inhibitor of dihydroorotate dehydrogenase (DHODH) with potential antineoplastic activity.

ON1231320 is a potent selective inhibitor of Polo like kinase 2 (PLK2).

Abiraterone acetate is an FDA approved drug, and is an orally active acetate ester of the steroidal compound abiraterone with antiandrogen activity. Abiraterone acetate was approved by the U.S. Food and Drug Administration (FDA) in April 2011. Abiraterone inhibits the enzymatic activity of steroid 17alpha-monooxygenase (17alpha-hydrolase/C17,20 lyase complex), a member of the cytochrome p450 family that catalyzes the 17alpha-hydroxylation of steroid intermediates involved in testosterone synthesis. Administration of this agent may suppress testosterone production by both the testes and the adrenals to castrate-range levels. FDA Approval this drug in May 2011.

SBI-477 is a chemical probe that coordinately inhibits triacylglyceride (TAG) synthesis and enhances basal glucose uptake in human skeletal myocytes with EC50 of 100 nM and 1 uM, respectively.

AZ10606120 is a potent, specific P2X7 receptor antagonist with Kd of 1.4 and 19 nM at human and rat P2X7 receptors respectively.

GLS4 (Morphothiadin) is a potent inhibitor of HBV capsid assembly, inhibits HBV replication (EC50=62.24 nM) and reduces HBV-DNA levels in HepG.2.2.15 cells (IC50=14 nM), shows efficacy against ADV-resistant HBV mutations.