A cell-permeable benzochromene that selectively impairs the viability and growth of IGF2-overexpressing hepatocellular carcinoma cells, binds to MFP-2, stimulates the expression of IGFBP-1 and SOCS-3 through activation of STAT6.

A potent, selective, brain penetrant PDE10A inhibitor with Ki of 4 nM.

A potent blocker of voltage-gated potassium channels Kv7 (KCNQ) that enhances ACh release from rat hippocampal slices in vitro with EC50 of 0.7 uM.

Firategrast is an orally bioavailable alpha4 beta1/alpha4 beta7 integrin antagonist designed to reduce trafficking of lymphocytes into the central nervous system (CNS).

RET-IN-14 (compound 49) is a potent RET inhibitor with IC50s of <0.51 nM, 9.3 nM, 1.3 nM, 9.2 nM, 15 nM for RET (WT), RET (G810R), RET (V804M), BTK and BTK (C481S), respectively. RET-IN-14 has the potential for tumors research

FM26 (compound 25) is a potent and allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists with an IC50 of 264 nM. FM26 has a distinct isoxazole chemotype and effectively reduces IL-17a mRNA production in EL4 cells.

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.

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

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.

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

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.

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.

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

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.

INCB13739 (INCB-13739) is a potent, selective, oral 11βHSD1 inhibitor (IC50=1.1 nM) with high seelctivity over other dehydrogenases, glucocorticoid and mineralocorticoid receptors..

NVP-CLR457 (compound 40) is an orally active, potent and balanced pan-class I PI3K inhibitor. NVP-CLR457 shows a clear dose-dependent PK/PD/efficacy relationship. NVP-CLR457 has antitumor activity.

Fluorobexarotene (compound 20) is a potent retinoid-X-receptor (RXR) agonist, with a Ki value of 12 nM and an EC50 value of 43 nM for RXRα receptor. Fluorobexarotene possesses an apparent RXR binding affinity that is 75% greater than Bexarotene.

DS69910557 is a potent, selective and orally activehuman parathyroid hormone receptor 1 (hPTHR1) antagonist. DS69910557 has antagonistic activity for PTHR1 with an IC50 value of 0.08 μM.

ITI-214 is a potent, selective phosphodiesterase 1 (PDE1) inhibitor with Ki of 58 pM, displays >1,000-fold selectivity over PDE4A/4D and other PDE isoforms.