DJ4 (ROCK inhibitor DJ4) is a potent, selective, ATP-competitive inhibitor of ROCK1/2 and MRCKα/β with IC50 of 5/50 nM and 10/100 nM, respectively.

BDT001 is a first-in-class, non-competitive FLT3 negative allosteric modulator, effectively prevents extracellular cytokine FL binding to FLT3 with IC50 of 11 uM.

K284 is a selective small molecule inhibitor of chitinase 3 like1 (CHI3L1) with strong binding affinity (Kd=-9.7 kcal·mol-1), inhibits lung metastasis by blocking IL-13Rα2-mediated JNK-AP-1 signals.

(R)-SKBG-1 is a covalent small molecule ligand of RNA-binding protein NONO, engages NONO Cys145 and suppress an array of cancer-relevant genes and impair cancer cell proliferation.

BAY-598 is a selective inhibitor of SMYD2.

DB213 (RG-501) is a small molecule stimulator of HIV-1 frameshifting and inhibitor of viral replication.

INT-777 is a semisynthetic bile acid that acts as an agonist of TGR5 (EC50 = 0.82 μM). INT-777 mitigates inflammatory response in human endometriotic stromal cells: A therapeutic implication for endometriosis.

ABT-702 is a potent non-nucleoside adenosine kinase inhibitor (IC50 = 1.7 nM), selective over other sites of adenosine interaction (A1, A2A and A3 receptors, adenosine transporter and adenosine deaminase).

NCP26 is a potent, ATP-competitive prolyl-tRNA synthetase (ProRS, PRS) inhibitor, inhibits recombinant human ProRS in the presence of 100 μM proline with KD of 0.35 nM in TR-FRET assays.

PXS-4748 (PXS4748) is a potent, selective and irreversible pan-lysyl oxidase (pan-LOX) inhibitor with IC50 of 2.0 uM and 3.2/0.6/1.4/0.2 uM for bovine (aorta) LOX and rh LOXL1/2/3/4, respectively.

Alprostadil(Caverject) is a prostanoid receptor ligand, with Kis of 1.1 nM, 2.1 nM, 10 nM, 33 nM and 36 nM for mouse EP3, EP4, EP2, IP and EP1, respectively. Prostaglandin E1 induces vasodilation and inhibits platelet aggregation. Prostaglandin E1 can be used as a vasodilator for the research of peripheral vascular diseases.

CPAG-1 (PGRMC2 activator CPAG-1) is a small-molecule activator of PGRMC2. CPAG-1 treatment had no effect on weight or food intake but treated mice had reduced fasting glycemia and insulin levels. CPAG-1 decreased Rev-Erbα protein in BAT of CPAG-1-treated mice. CPAG-1 also significantly increased labile heme in the nucleus of brown adipocytes from CPAG-1-treated mice within 4 days of treatment.

BRD5814 is a potent, selective, highly brain penetrant β-arrestin biased dopamine D2 receptor (D2R) antagonist with Ki of 0.27 uM.

ZINC 39395747 is a novel potent derivative of propylthiouracil that functions as a cell-active inhibitor of cytochrome b5 reductase 3 (CYB5R3) with IC50 of 9.14 uM.

Diarylpropionitrile (DPN) is a non-steroidal estrogen receptor β(ERβ) selective ligand, demonstrates the neuroprotective effects against 10 0M Aβ1-42-induced oxidative stress and inflammation in primary rat cortical cell culture.

NC-001 (NC 001, NC001, az-NC-001) is a potent, specific, cell-permeable inhibitor of immunoproteasome caspase-like sites (β1i and β1), does not correlate with inhibition of chymotrypsin-like sites..

VTI-1002 is a potent and specific inhibitor of human (K i = 4.4 ± 2.0 nM) and murine (IC 50 = 179 ± 18 nM) GzmB, with minimal activity (IC 50 > 300 nM) against Cathepsin-G, neutrophil elastase and caspases (−3, −4, −5, −7, −8 and −9). In addition to its high specificity for GzmB, VTI-1002 is retained in murine skin for up to 24 hours and exhibits minimal toxicity in vivo with no observed adverse effects after 30 consecutive days of systemic administration in mice [31]. VTI-1002-mediated GzmB inhibition was first reported to augment type I collagen fibrillogenesis and improve tensile strength in a murine diabetic burn model, notably by preventing decorin cleavage and dermal fibrillar collagen network disorganization.

USP10-IN-3 is a HBX19818 analog, potent and selective USP10 inhibitor, but does not inhibit USP7 (IC50>100 uM).

Orlistat is a drug designed to treat obesity. Orlistat's primary function is preventing the absorption of fats from the human diet by acting as a lipase inhibitor, thereby reducing caloric intake. Orlistat is intended for use in conjunction with a healthcare provider-supervised reduced-calorie diet.

TP-1454 is an activator of PKM2 with AC50 of 10 Nm in biochemical assays.TP-1454 modulates tumor-immune responses by destabilizing T-regulatory cells.

YE-120 is an agonist of G protein-coupled receptor 35 (GPR35).

PAFAH inhibitor P11 (P11) is a potent, selective platelet-activating factor acetylhydrolases PAFAH1b2 and PAFAH1b3 inhibitor with IC50 of 40 nM and 900 nM respectively.

Inflachromene (ICM) is a microglial inhibitor with anti-inflammatory effects, directly binds high mobility group protein 1 (HMGB1) and HMGB2 and reduces their cytoplasmic accumulation in microglial cells.

Befiradol (F13640, NLX 112) is a highly potent, selective 5-HT1A receptor agonist with Ki of 2.7 nM.

TL4-12 is a potent MAP4K2 (GCK) inhibitor that inhibits IL-1 and TGFβ-induced p38 MAPK phosphorylation, in vitro.

Dibenzo[a,i]pyrene is a polycyclic aromatic hydrocarbon (PAH) with potent carcinogenic activity. Dibenzo[a,i]pyrene was shown to induce DNA adduction, tumorigenicity as well as Ki-ras oncogene mutations in strain A/J mouse lung. Dibenzo[a,i]pyrene has been shown to be present in cigarette smoke condensate and in automobile exhaust gas in small quantities.

R121919 is a potent small-molecule CRF1 receptor antagonist with a Ki of 2 to 5 nM for the CRF1 receptor and over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types.

20-O-Acetylingenol-3-angelate is a diterpene ester that has been found in E. peplus and a derivative of ingenol-3-angelate

L557-0155 is a small molecule inhibitor of VSIG-8, prevents VSIG-8 binding to VISTA, promotes cytokine production and cell proliferation in PBMCs and suppresses melanoma growth.

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.