Capadenoson is a selective agonist of adenosine-A1 receptor.

CSRM617 (CSRM-617) is a small-molecule inhibitor of the transcription factor ONECUT2 (OC2) with Kd of 7.43 uM in SPR assays, binds to OC2-HOX domain directly.

UT-143 is a selective androgen receptor irreversible covalent antagonist and inhibits AR transactivation with IC50 of 150 nM. UT-143 covalently and selectively binds to C406 and C327 in the AF-1 region and inhibits PCa cell proliferation and tumor growth.

CYN 154806 is a potent and selective somatostatin sst2 receptor antagonist. pIC50 values are 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively.

BTdCPU is an activator of HRI. The eIF2-alpha kinase HRI is a novel therapeutic target in multiple myeloma. Combination therapy with rapamycin, an mTOR inhibitor, and BTdCPU, an activator of HRI, demonstrated additive effects on apoptosis in dex-resistant cells. Thus, specific activation of the eIF2α kinase HRI is a novel therapeutic target in MM that can augment current treatment strategies.

BLU-945(BLU945,BLU 945) is a highly potent and selective EGFR+/T790M/C797S (IC50 of 0.5 nM) and EGFR+/T790M (IC50 of 0.4 nM) inhibitor with >900-fold selectivity over EGFR WT (IC50 of 736.3 nM).

NSC243928(NSC-243928 ) is a small molecule that potently inhibit ovarian cancer stem-like cells (CSC) growth with GI50 of 0.83 uM, which os consistent with cell death/apoptosis..

Tinlorafenib (PF-07284890) (compound 10) is an orally active BRAF kinase inhibitor, with IC50s of 4.25 and 2.7 nM for BRAFV600E/V600K respectively. Tinlorafenib demonstrates CNS penetration and can be used in the research of BRAF-associated malignant and benign tumors of the CNS as well as extracranial malignancies[1].

Centanamycin alkylates the A-T-rich minor groove of the DNA and thereby blocks DNA replication. Centanamycin potently inhibits replication of human cytomegalovirus (HCMV), mouse CMV (MCMV), and herpes simplex virus-2 (HSV-2) in vitro. Centanamycin-attenuated whole virion MCMV elicits a robust serum neutralizing antibody response and protects the mice from live-virus challenge.

NFAT Transcription Factor Regulator is an IL-2 synthesis inhibitor with an IC50 of 182 nM.

A potent, specific and nonlipid agonist of LPA2 receptor with EC50 of 3.3 uM, does not activate any of the other LPA GPCRs (>10 uM).

SB-328437 is a potent, selective non-peptide CCR3 antagonist with an IC50 of 4.5 nM.

PKR-IN-C51(compound 51) is an ATP-competitive double-stranded RNA-activated protein kinase (PKR) inhibitor with an IC50 of 9 μM. PKR-IN-C51 inhibits intracellular PKR activation in a dose-dependent manner in primary mouse macrophages[1].

PQM130, a Feruloyl-Donepezil Hybrid compound with brain penatration, is a multitarget drug candidate against the neurotoxicity induced by Aβ1-42 oligomer (AβO) and shows anti-inflammatory activity. PQM130 acts as a neuroprotective compound for anti-AD drug development[1].

Olvanil (NE-19550)is an agonist of transient receptor potential vanilloid type 1 (TRPV1) channels with an EC50 of 0.7 nM.Analgesic[1].

Dexpramipexole 2Hcl(KNS-760704), also known as R-(+)-Pramipexole, is a neuroprotective agent and weak non-ergoline dopamine agonist. IC50 Value:Target: Dopamine ReceptorDexpramipexole has been found to have neuroprotective effects and is being investigated for treatment of amyotrophic lateral sclerosis (ALS). Dexpramipexole reduces mitochondrial reactive oxygen species (ROS) production, inhibits the activation of apoptotic pathways, and increase cell survival in response to a variety of neurotoxins and β-amyloid neurotoxicity. Compared to the S-(-) isomer, Dexpramipexole has much lower dopamine agonist activity.

BETd-260 (ZBC260, BETd260) is a novel PROTAC BET degrader that tether HJB97 to a ligand for the E3 ubiquitin ligase VHL.

GSK3-IN-1 (compound 11) is a GSK-3 inhibitor with an IC50 value of 12 μM. GSK3-IN-1 can be used in the research of diabetes[1].

Sigma-1 receptor antagonist 2 is a potent and selective sigma 1 receptor (σ1 R) antagonist with Kis of 3.88 and 1288 nM for σ1 and σ2 receptor, respectively[1].

Sigma‑1 receptor antagonist 1 (compound 137) is a potent and selective sigma-1 receptor (σ1R) antagonist, with a high binding affinity to σ1R receptor (Ki = 1.06 nM). Sigma‑1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain[1].

(E/Z)-ZINC09659342 is an inhibitor of Lbc-RhoA interaction[1].

Reserpine is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).

Lepidiline A shows cytotoxic activity against HL-60 cells with an IC50 of 32.3 μM.

KCC009, a transglutaminase 2 (TG2) inhibitor, induces p53-independent radiosensitization.

Allopurinol sodium is a potent xanthine oxidase inhibitor (IC50 values of 0.2 to 50 μM). Allopurinol sodium can be used for the research of hyperuricemia and gout. Antileishmanial effect[1][2].

Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.

GDC-2394 is an orally active and selective NLRP3 inhibitor, and also inhibits IL-1β with IC50s of 0.4 μM (human IL-1β) and 0.1 μM (mouse IL-1β). GDC-2394 inhibits NLRP3-induced caspase-1 activity without inhibiting NLRC4-dependent inflammasome activation.

PLX8394 (PLX-8394) is a next-generation, orally available, small-molecule BRAF inhibitor with IC50 values of 3.8 nM, 14 nM and 23 nM for BRAF (V600E), WT BRAF and CRAF, respectively.PLX8394 suppresses mutant BRAF cells without activating the MAPK pathway in cells bearing upstream activation, overcame several known mechanisms of resistance to first-generation RAF inhibitors.PLX8394 inhibits ERK signaling by specifically disrupting BRAF-containing dimers, including BRAF homodimers and BRAF-CRAF heterodimers, but not CRAF homodimers or ARAF-containing dimers.As a BRAF-specific dimer breaker, PLX8394 selectively inhibits ERK signaling in tumors driven by dimeric BRAF mutants, including BRAF fusions and splice variants as well as BRAF V600 monomers, but spares RAF function in normal cells in which CRAF homodimers can drive signaling.