PF-152 is a potent, highly selective and orally bioavailable MMP13 inhibitor with Ki of 1.5 nM, with no activity against MMP3 (Ki>10 uM).

Oridonin (Cmpd-5, NSC 250682) is a natural ent-kaurane diterpenoid from Rabdosia rubescens identified as a first-in-class small-molecule inhibitor that directly binds β-arrestin1 and β-arrestin2 with high nanomolar to low micromolar affinity. Oridonin broadly suppresses β-arrestin recruitment, receptor desensitization, internalization, and downstream ERK signaling across multiple GPCR families, and abrogates T-cell chemotaxis.

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.

​​GB1107​​ is a novel small-molecule inhibitor specifically designed to target galectin-3 (Gal-3), demonstrating high binding affinity and oral bioavailability.

HOIPIN-1 (JTP-0819958, HOIP inhibitor-1) is a chemical inhibitor of linear ubiquitin chain assembly complex (LUBAC, IC50=2.8 uM), specifically generates Met1-linked linear ubiquitin chains through the ubiquitin ligase activity in HOIP, and activates the N

PSMA-617, also know as vipivotide tetraxetan, is a ligand used to make 177Lu-PSMA-617, which is a radioactive molecule to fight cancer. PSMA617 possesses a small peptide, which was designed to target prostate-specific membrane antigen (PSMA). PSMA617 demonstrates high radiolytic stability for at least 72 h. PSMA617 has high inhibition potency (equilibrium dissociation constant Ki=2.34±2.94 nM on LNCaP; Ki=0.37±0.21 nM enzymatically determined). 177 Lu-PSMA-617 offers a potential additional life-prolonging treatment option for men with mCRPC.

SPI-21 (Spt5-Pol II inhibitor 21) is a small-molecule inhibitor of Spt5-Pol II with IC50 of 25.2 uM.

Asimadoline HCl is a κ-opioid receptor agonist potentially for the treatment of pruritus. Asimadoline has also been shown to be used in the treatment of irritable bowel syndrome.

GYS32661 is a potent, small-molecule inhibitor of RAC1 and its isoform RAC1B, specifically designed to target the Sonic Hedgehog (Shh) signaling pathway in cancers like medulloblastoma and colorectal carcinoma. Distinguishing itself from other RAC1 inhibitors, GYS32661 exhibits exceptional blood-brain barrier (BBB) permeability with an approximately 50% brain-to-plasma ratio, making it a premier candidate for treating CNS-related malignancies. It functions by disrupting the activation of RAC1 (IC50 ≈ 1.18 μM), subsequently reducing the expression of downstream transcription factors GLI1 and GLI2, which effectively halts tumor proliferation and metastasis. In preclinical in vivo models, the compound has demonstrated significant anti-tumor efficacy and a favorable safety profile without systemic toxicity. Due to its hydrophobic nature, it is typically formulated in a vehicle of DMSO, PEG300, and saline for administration. As a non-toxic clinical candidate, GYS32661 represents a promising therapeutic strategy for overcoming chemoresistance and improving survival rates in Shh-driven pediatric and adult tumors.

Sodium taurocholate is a GPBAR1 protein agonist potentially for the treatment of type 2 diabetes and obesity in rats.

An orally active anabolic-androgenic steroid and a 19-nortestosterone derivative that has been widely used in scientific research as a hot ligand in androgen receptor (AR) ligand binding assays (LBAs) and as a photoaffinity label for the AR..

DOTA-ADIBO is a Click Chemistry intermidate used for antibody-drug conjugates..

T025 is as an orally available and potent inhibitor of Cdc2‐like kinases (CLKs) with an IC50s of 0.93 nM, 1 nM, 14 nM, 1.5 nM for CLK1, CLK2, CLK3, DYRK1B respectively. It exhibits anti‐tumor efficacy and can be used in MYC‐driven cancer research.

Vicadrostat (compound 29 A) is a potent and selective inhibitor of aldosterone synthase(CYP11B2) with an IC50 of 16 nM. It exhibits potential in renal disease, diabetic nephropathy, cardiovascular diseases and fibrotic disorder research.

Barbadin is a small molecule that selectively inhibits the β-arrestin/β2-adaptin interaction (IC50=19.1/15.6 uM for β-arrestin1/2) without effect on the formation of receptor/β-arrestin complexes.

QD325 is a potent redox modulator that induces Nrf2-mediated oxidative stress and unfolded protein responses in PDAC cells (IC50=0.9 uM).

IDE-1 induces definitive endoderm formation in mouse and human embryonic stem cells (ESCs) (EC50 = 125 nM).

LUF6000 is a potent, selective, positive allosteric modulator (enhancer) of human A3 adenosine receptor, enhance Emax but without affecting agonist potency.

tri-GalNAc-COOH is an asialoglycoprotein receptor (ASGPR) ligand that can be used for LYsosome TArgeting Chimera (LYTAC) research.

tri-GalNAc-COOH acetylation is the acetylated and modified form of tri-GalNAc-COOH. tri-GalNAc-COOH acetylation can be used for the synthesis of LYTAC.

A novel and irreversible inhibitor of mutant K-ras G12C..

ENOblock(AP-III-a4) is a novel small molecule which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity (IC50=0.576 uM); inhibit cancer cell metastasis in vivo.

BMS-986122 is a potent positive allosteric modulator of μ-opioid receptor, significantly increases the inhibition of forskolin-stimulated adenylyl cyclase activity produced by an EC10 (30 pM) concentration of endomorphin-I in CHO-μ cells..

YY-20394 is a novel PI3K inhibitor suppresses tumor progression by immune modulation.

Dorzolamide is a carbonic anhydrase inhibitor. It is an anti-glaucoma agent, and acts by decreasing the production of aqueous humour. It is administered as a topical ophthalmic in the form of a 2% solution.

IM176OUT05 is a novel, and safe small molecule that improves the acquisition and maintenance of stem cell pluripotency, inhibits electron transport chain (ETC) in the A549 lung carcinoma cell line with IC50 of 3.2 uM.

AM4113 is a cannabinoid receptor 1 (CB1)-selective antagonist.

CGP-77675 is a potent and selective Src family kinase (SFK) inhibitor. CGP-77675 inhibited phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50: 5-20 and 40 nM, respectively). The dual inhibition of Src and GSK-3 signaling by CGP 77675 and CHIR 99021 was found to maintain mouse embryonic stem cell (mESC) self-renewal and pluripotency marker expression as efficiently as the dual inhibition of MAPK and GSK-3 by PD 0325901 and CHIR 99021.

K252c is a staurosporine analog and inhibitor of PKC and PKA. It inhibits proliferation of human cytomegalovirus and induces apoptosis in cancer cells.

CCT 365623 (CCT365623) hydrochloride is a potent, orally active small molecule inhibitor of lysyl oxidase (LOX) with IC50 of 0.89 uM.