Vibozilimod (example 33) is a S1p1 receptor agonist (extracted from patent WO2012140020A1).

.Valemetostat is an antineoplastic agent.

Dopamine D2 receptor agonist-2 (compound 36) is a potent dopamine D2 receptor biased agonism ligand with an Ki value of 11.2 nM. Dopamine D2 receptor agonist-2 can be used to research antipsychosis[1].

c-Fms-IN-13 (compound 14) is a potent FMS kinase inhibitor with an IC50 value of 17 nM. c-Fms-IN-13 can be used as an anti-inflammatory agent[1].

RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant relaxin family peptide 3 (RXFP3) antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC50 values of 2.36 μM for RXFP3, 7.82 and 13.86 μM for ERK1 and ERK2 phosphorylation, respectively. RLX-33 can block the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats. RLX-33 can be used for the research of metabolic syndrome[1].

Lepidiline C shows cytotoxic activity against HL-60 cells with an IC50 of 27.7 μM.

ISR-IN-1 (Compound 48) is an inhibitor of the integrated stress response.

ISR-IN-2 (Compound 47) is an inhibitor of the integrated stress response .

UCM05 (G28UCM) is a potent inhibitor of fatty acid synthase (FASN) shows activity against HER2+ breast cancer xenografts and is active in anti-HER2 drug-resistant cell lines[1]. UCM05 is a Filamentous temperature-sensitive protein Z (FtsZ) inhibitor and inhibits the growth of the Gram-positive bacterium B. subtilis with MIC values of 100 μM but lack activity on the Gram-negative bacterium E. coli[2].

BSP16 is a potent, orally active stimulator of interferon genes (STING) agonist. BSP16 can selectively stimulate the STING pathway. BSP16 can be used for the research of cancer.

α-Lapachone shows trypanocidal activity[1].

GSK 3186899 (GSK-3186899, DDD853651) is a novel specific inhibitor of parasite cdc-2-related kinase 12 (CRK12), shows activity against L. donovani in intra-macrophage assay with EC50 value of 1.4 uM, and shows good selectivity against mammalian THP-1 host cells (EC50> 50 uM).

MM-3122 is a selective inhibitor of host cell serine protease TMPRSS2 (transmembrane protease serine 2) with IC50 of 0.34 nM against recombinant full-length TMPRSS2 protein.

MYF-03-176 is an orally active and potent anticancer agent. MYF-03-176 shows strong antitumor efficacy in MPM mouse xenograft model via oral administration[1].

YX-2-107 is a CRBN-recruiting and specific CDK6-degrading PROTAC with IC50 of 0.69 and 4.4 nM for CDK4 and CDK6 in vitro, selectively degardes CDK6 in Ph+ BV173 ALL cells with a degradation constant of 4 nM.YX-2-107 does not affect expression of IKZF1 and IKZF3, and does not degarde CDK4 protein.YX-2-107 inhibits S-phase entry, cell proliferation, RB phosphorylation, and FOXM1 expression and induces the selective degradation of CDK6 in Ph+ BV173 and SUP-B15 cells.|PROTAC YX-2-107 is bioavailable in mice and pharmacologically active in suppressing Ph+ ALL proliferation in a mouse xenograft of Ph+ ALL, comparable or superior to that of the CDK4/6 enzymatic inhibitor palbociclib.

A947 is a potent and selective SMARCA2 PROTAC with DC50 of 39 pM in W1573 cells. A947 shows 28-fold selectivity over SMARCA4 and notably exhibits no unexpected off-target effects at high concentration.

MS9715 (MS-9715) is a NSD3-targeting PROTAC designed by linking BI-9321, a NSD3 antagonist, which binds NSD3's PWWP1 domain, with an E3 ligase VHL ligand.MS9715 achieves effective and specific targeting of NSD3 and associated cMyc node in tumor cells.MS9715 effectively suppresses growth of NSD3-dependent hematological cancer cells.MS 9715 effectively suppresses NSD3-and cMyc-associated gene expression programs, resembling effects of the CRISPR-Cas9-mediated knockout of NSD3.

TD165(TD 165) is a PROTAC-based cereblon (CRBN) degrader that degrads Cav1.2α with the DC50 of 20.4 nM, comprising a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group.

Siponimod, also known as BAF-312, is a a potent and orally selective S1P Receptor Modulator with EC50 value of 0.39nM for S1P1 receptors and 0.98nM for S1P5 receptors, respectively. Development of sphingosine-1-phosphate receptor 1 (S1P1) modulators to dampen inflammation and its sequelae is becoming increasingly promising for treating medical conditions characterized by significant immunopathology.

4-CPPC is the first reversible and selective inhibitor of pro-inflammatory protein macrophage migration inhibitory factor-2 (MIF-2) with Ki of 33 uM, 13-fold selectivity for human MIF-2 versus human MIF-1.

6-Thioguanosine (6-Mercaptoguanosine), an active nucleoside, is an Azathioprine metabolite. 6-Thioguanosine has immunosuppressive effects.

A-196 is a potent and selective chemical inhibitor of SUV420H1 and SUV420H2 that inhibits the di- and trimethylation of H4K20me in multiple cell lines.

AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC50 of 14 nM.

ALB-127158A, also known as ALB-127158(a), is a MCH1 antagonist for the treatment of obesity.

Alpha-Lipoic Acid Choline Ester, also known as alpha-LACE, EV-06 or UNR844, is a drug candidate potentially for the treatment of presbyopia. Alpha-LACE was designed to permeate biological membranes with the incorporation of the cationic choline head grou

Apostatin-1 (Apt-1) is a novel TRADD inhibitor.Apostatin-1 inhibits RIPK1-dependent apoptosis (RDA) with IC50 of 1.28 μM and shows no significant off-target activity on 97 kinases in KINOME scan profiling.Inhibition of TRADD by Apostatin-1 blocks apoptosi

AVP-786 is a novel, next-generation investigational drug product consisting of a combination of deudextromethorphan, and an ultra-low dose of quinidine.

BAY-1816032 (BAY1816032) is a highly potent, selective, orally active BUB1 mitotic checkpoint serine/threonine kinase with IC50 of 7 nM, displays excellent selectivity on a panel of 395 kinases.

BMS-1166 Hcl salt is a potent PD-1/PD-L1 interaction inhibitor with IC50 of 1.4 nM in a homogenous time-resolved fluorescence binding assay.

CeMMEC1 is a novel potent inhibitor of the second bromodomain of TAF1, binding neither the first nor the second bromodomain of BRD4.