​​RO5263397​​ is a novel, orally active trace amine-associated receptor 1 (TAAR1) agonist demonstrating high potency and species-specific activity.

PF-00562271 is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 with IC50 of 1.5 nM and 14 nM, respectively.

ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4), is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization.

A competitive inhibitor of HMG-CoA reductase that acts as a lipid-lowering agent for prevention of events associated with cardiovascular disease..

Novel inhibitor of CYLD and USP-family deubiquitinating enzymes, increasing the polyubiquitination of NEMO and RIP1, enhancing NF-κB activation and promoting NF-κB signaling

Antibiotic, inhibiting the first step in the N-linked glycosylation in eukaryotes and inducing ER stress to activate the unfolded protein response (UPR)

ICA135 (ICA-135, ICA 135) is a broad-spectrum inhibitor against human enteroviruses that inhibits Coxsackievirus A10 (CV-A10) replication in RD cells with IC50 of 1.446 uM.

NCGC00131308 is a small molecule inhibitor that effectively disrupts IQGAP1-Cdc42 interaction in breast cancer cells, shows EC50 of 4.47 uM in biochemical HTRF assays.

Vanzacaftor is a modulator of cystic fibrosis transmembrane conductance regulator (CFTR) for treating cystic fibrosis.

ZHAWOC8697 is a small molecule dual inhibitor of sentrin-specific protease SENP1 and SENP2 with IC50 of 8.6 and 2.3 uM, respectively, a valuable tool for the study of SUMOylation processes.

PF-06273340 is a highly potent, kinases elective, well-tolerated pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, Trk C, respectively.

EB1 is the inhibitor of kinases MNK with IC50s of 0.69 μM (MNK1) and 9.4 μM (MNK2). EB1 selectively inhibits the growth of cancer cells, but not normal cells. EB1 also increases cell apoptosis and suppresses eIF4E phosphorylation.

Dabigatran etexilate mesylate (BIBR 1048MS) serves as the ​orally bioavailable prodrug of the active anticoagulant dabigatran. Following absorption, this precursor compound undergoes ​enzymatic conversion to release dabigatran - a highly ​selective, reversible direct thrombin inhibitor (DTI) with exceptional potency (Ki = ​4.5 nM).

BL5923 (BL-5923) is a potent, highly specific, orally available inhibitor of CCR1 with IC50 of 20.4 and 22.8 nM for human and mouse CCR1, resepctively.

MK-6240 Precursor (6e) serves as a key intermediate in the synthesis of ​**[18F]-MK-6240**, a highly selective ​tau-targeting PET imaging agent. The radiolabeled compound, ​**[18F]-MK-6240**, is specifically designed for detecting ​neurofibrillary tangles (NFTs)—a hallmark pathology of ​Alzheimer’s disease and other tauopathies.

EB-PSMA-617 is an Evans blue-modified prostate-specific membrane antigen (PSMA) 617 ligand for making 177Lu-EB-PSMA, which is potential useful for Metastatic Castration-Resistant Prostate Cancer.

HC-258 is a Covalent Acrylamide TEAD Inhibitor That Reduces Gene Expression and Cell Migration. HC-258 reduces the CTGF, CYR61, AXL, and NF2 transcript levels and inhibits the migration of MDA-MB-231 breast cancer cells. Co-crystallization with hTEAD2 confirmed that HC-258 binds within TEAD’s PA pocket, where it forms a covalent bond with its cysteine.

Oligopeptide-10, also known as granactive oligopeptide-10, is a synthetic bio-active peptide composed of 15 amino acids. it can help manage acne-causing bacteria, both on its own and in conjunction with anti-acne superstar exfoliant salicylic acid.

XPW1 is a potent and selective CDK9 inhibitor with excellent anti-ccRCC activity and low toxicity.

FDW028 is a potent and highly selective small-molecule inhibitor of fucosyltransferase 8 (FUT8) with binding KD value of 5.486 uM, displays no affinity against other FUTs, shows potent anti-CRC activities.

GLPG3667 is an oral, reversible, and selective tyrosine kinase 2 (TYK2) inhibitor. It is being developed to treat inflammatory and auto-immune diseases. Biochemical assays showed that GLPG3667 displayed nanomolar potency on TYK2 with a selectivity over other JAK kinases >3-fold. In human PBMC, GLPG3667 showed comparable potency on the IFNα and IL-23 pathways (around 50 nM). Selectivity for TYK2 on the IFNα pathway was >14-fold and >19-fold toward the IL-2 and GM-CSF pathways in human PBMC and whole blood, respectively. Dermal ear inflammation in a mouse model of psoriasis driven by IL-23 was prevented by GLPG3667 with a minimal effective dose of 3 mg/kg given orally once daily. This effect was associated with a decrease in neutrophil infiltration and STAT3 phosphorylation at sites of inflammation. In healthy HV, GLPG3667 completely inhibited IFNα-induced STAT1 and STAT3 phosphorylation but did not impact IL-2- and GM-CSF-induced STAT5 phosphorylation.

ZH8667 is a trace amine-associated receptor 1 (TAAR1)–Gs agonist.

ML162 is a covalent inhibitor that specifically targets ​glutathione peroxidase 4 (GPX4), a key regulator of ferroptosis. This compound exhibits ​selective cytotoxicity against cancer cell lines harboring ​mutant RAS oncogenes, making it a promising candidate for precision oncology.

A83B4C63 is a highly potent small-molecule inhibitor targeting the DNA repair enzyme polynucleotide kinase 3'-phosphatase (PNKP), exhibiting strong binding affinity with a ​Kd of 80 nM. Due to its limited aqueous solubility, A83B4C63 was formulated into ​nano-encapsulated carriers, enhancing its therapeutic potential—particularly in ​PTEN-deficient colorectal cancer (CRC).

Furamidine dihydrochloride (NSC 305831) tyrosyl-DNA phosphodiesterase (Tdp1), also is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with IC50 of 9.4 uM.

Pyrinuron is an inhibitor of NAMPT and NMNAT2.Pyrinuron is used as a model compound in studies of urea derivatives and their reactivity.Research has explored the effects of this compound on insulin-producing beta cells, providing insights into diabetes mechanisms.Although not used therapeutically, this compound’s ability to selectively destroy beta cells has implications for understanding and potentially treating type 1 diabetes.

Mifepristone (RU-486) is a potent steroidal antagonist exhibiting subnanomolar affinity for progesterone receptors (PR IC₅₀ = 0.2 nM) and nanomolar activity against glucocorticoid receptors (GR IC₅₀ = 2.6 nM). This dual-receptor modulator competitively blocks endogenous hormone binding while inducing distinct conformational changes that prevent coactivator recruitment, demonstrating differential antagonism between PR and GR signaling pathways.

XEN-602 represents a breakthrough in DMT1 pharmacology as a picomolar-range inhibitor of divalent metal transporter 1 (SLC11A2), demonstrating unprecedented selectivity for manganese transport blockade (IC₅₀ = 300 pM in HEK293 cells). This structurally optimized small molecule achieves complete suppression of DMT1-mediated Mn²⁺ uptake while maintaining exceptional target specificity, as evidenced by minimal interference with other metal transporters. Its unmatched potency enables precise interrogation of DMT1's physiological roles and therapeutic exploration for manganese dysregulation disorders.

GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.

DOCK5-IN-C21 functions as an allosteric inhibitor targeting the guanine nucleotide exchange factor DOCK5, effectively modulating its activity through a non-competitive mechanism.