DN-1289 is a potent and selective dual DLK/LZK inhibitor. DN1289 demonstrated excellent in vivo plasma half-life across species and is anticipated to freely penetrate the central nervous system with no brain impairment based on in vivo rodent pharmacokinetic studies and human in vitro transporter data. Proximal target engagement and disease relevant pathway biomarkers were also favorably regulated in an in vivo model of amyotrophic lateral sclerosis.

BI685509 is a soluble guanylate cyclase (sGC) activator taken orally, with potential to treat diabetic and kidney diseases. In both rat and human platelets, BI685509 was found to restore/enhance cGMP, but had no effect on the functionality of nitric oxide pathways. BI685509 is currently undergoing phase 2 trials for the treatment of diabetic nephropathy, with the aim of improving kidney function.

RMC-5552 is a potent and selective inhibitor of mTORC1. RMC-5552 inhibits phosphorylation of mTORC1 pS6K and p4EBP1 with IC50s of 0.14 nM and 0.48 nM, respectively. RMC-5552 has anti-cancer activity.

EG-011 is the first-in-class and potent Wiskott-Aldrich syndrome protein (WASP) activator. EG-011 activates the auto-inhibited form of WASP with strong actin polymerization. EG-011 has selective anti-tumor activity in lymphomas.

ENT-01 shows promise in the treatment of constipation in those with Parkinson's disease (PD) by preventing or reducing the formation of αS aggregates that form in enteric neurons. ENT-01 has undergone Phase 2b clinical trials to evaluate the safety and efficacy of the orally administered drug for the alleviation of constipation in those with PD.

UCB7362 is an orally active and potent antimalarial plasmepsin X (PMX) inhibitor, with an IC50 of 7 nM. UCB7362 inhibits parasite growth.

AN15368 (AN 15368) is a small molecule prodrug activated by parasite carboxypeptidases to yield a compound that targets the messenger RNA processing pathway in Trypanosoma cruzi (T. cruzi), exhibits potent in vitro activity against T.

UR-MB108 (Compound 57) is a potent, selective ABCG2 (BCRP) inhibitor with an IC50 of 79 nM. UR-MB108 is stable in blood plasma.

BI-0474 is a potent KRASG12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models.

JNJ-64264681 is a covalent, irreversible BTK inhibitor with potent whole blood activity and exceptional kinome selectivity. JNJ-64264681 demonstrated excellent oral efficacy in both cancer and autoimmune models with sustained in vivo target coverage amenable to once daily dosing and has advanced into human clinical studies to investigate safety and pharmacokinetics.

AZD-1656 is a glucokinase (GK) activator potentially for the treatment of type 2 diabetes and obesity.

CH7057288 (CH-7057288) is a novel potent and selective pan-TRK inhibitor with IC50 of 1.1/7.8/5.1 nM for TRKA/TRKB/TRKC, respectively.

AZD1390 is a first-in-class orally available and CNS penetrant ATM inhibitor with an IC50 of 0.78 nM in cells and >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases

GST-HG131 is a specific inbihitor of hepatitis B virus (HBV) surface antigen, belongs to dihydrobenzopyridooxazepine (DBP) series. GST-HG131 exhibits excellent and specific HBV antigens inhibition with EC50 of 28.2 nM (HBsAg) and 16.0 nM (HBeAg), respectively, but also it is safety for animal.

ICeD-2 is a inducer of cell death, can induce HIV-1 infected cell kill. ICeD-2-mediated HIV-1 infected cell kill is dependent on HIV-1 protease activity. ICeD-2 potently blocks hydrolysis of Gly-Pro-AMC by dipeptidyl peptidase DPP8 and DPP9. ICeD-2 shows strong stabilization of DPP9 in PBMCs.

GNE-064 (compound 5) is a selective, oral and highly soluble inhibitor of the SMARCA4, SMARCA2 and PBRM1 bromodomains 5. GNE-064 inhibits SMARCA4 with an IC50 of 0.035 μM and inhibits SMARCA2 with an EC50 of 0.10 μM. GNE-064 possess Kds with 0.01, 0.016, 0.018 and 0.049 μM for SMARCA4, SMARCA2, PBRM1 bromodomains 5 and PBRM1 bromodomains 2, repectively. GNE-064 can be used as a chemical probe for the research of drug synthesis.

Mitiperstat is the potent inhibitor of myeloperoxidase (MPO). Mitiperstat is particularly useful in the research of prophylaxis of cardiovascular disorders such as heart failure and coronary artery disease related conditions (extracted from patent US20160152623A1).

SPH3127 (DRI 18) is a novel, highly potent, and orally active direct renin inhibitor (recombinant human-renin IC50=0.4 nM, human plasma renin activity IC50=0.45 nM). SPH3127 shows antihypertensive effect and can be used in essential hypertension research.

Amgen-23 (compound 23) is a potent sphingosine kinases (SPHK) inhibitor with IC50 values of 20 nM and 1.6 μM for SPHK1 and SPHK2, respectively. Amgen-23 can be used for researching anticancer.

CC-99677 is a potent, covalent, and irreversible inhibitor of the mitogen-activated protein (MAP) kinase-activated protein kinase-2 (MK2) pathway in both biochemical (IC50=156.3 nM) and cell based assays (EC50=89 nM).

Wnt/β-catenin agonist 1 (compound 3f) is a Wnt/β-catenin signalling pathway agonist, with an EC50 of 0.27 μM.

CHF-6366 is a potent M3 muscarinic antagonist and β2-adrenergic receptors agonist with pKi values of 10.4 and 11.4, respectively. CHF-6366 is also a weak calcium channel inhibitor (IC50~50 μM). CHF-6366 inhibits bronchoconstriction in guinea pigs.

BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC50= 5 nM. BI-4142 showed efficacy against HER2 exon 20 insertion-driven tumors, while preserving EGFR wt signaling.

TAS1553 is a potent, orally active protein–protein interaction (PPI) inhibitor with an IC50 values of 0.0396 μM. TAS1553 inhibits DNA replication and reduces intracellular dATP pool. TAS1553 induces apoptosis. TAS1553 can be used for cancer research.

MK-0159 is a CD38 enzymatic inhibitor. Mice treated with MK-0159 show strong protection from myocardial damage upon cardiac I/R injury compared to those treated with NAD+ precursors (nicotinamide riboside) or another CD38 inhibitor.

BMS-986339 is an orally active, potent FXR agonist. BMS-986339 forms H-bond with His298 and ASN287 residues.

AHL-030 is a potent and selective EDC3-targeted ligands. AHL-030 is also an stress granules (SGs) enhancer and results in a 2-fold increase in SGs per arsenite-treated cell.

HHS-166 shows dose-dependent inhibition of arsenite-induced stress granule (SG) formation, and liganded G3BP1 Y40 in the NTF2 dimerization domain of this essential nucleating protein for SG regulation.

BMS-986120 (BMS986120) is a potent, selective, orally bioavailable, and reversible PAR4 antagonist with Kd of 0.098 nM for human PAR4.

WX-081, an anti-tuberculosis agent, displays excellent anti-mycobacterial activity against M. tuberculosis H37Rv and low cytotoxicity.