BRD-K98645985 is a class of 12-membered macrolactam and a BAF transcriptional repression inhibitor with an EC50 of ~2.37 µM. BRD-K98645985 binds ARID1A-specific BAF complexes, prevents nucleosomal positioning, and potently reverses HIV-1 latency, and without T cell activation or toxicity.

SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G.

Novel FABP4/5 inhibitor, inhibiting lipolysis in 3T3-L1 adipocytes and in primary human adipocytes

Novel potent and cell-active PARG inhibitor, selectively killing BRCA-mutant and PARP inhibitor-resistant cancer cells

TX1-85-1 is a potent, selective, ATP-competitive Her3 (ErbB3) inhibitor with IC50 of 23 nM, forms a covalent bond with Cys721 located in the ATP-binding site of Her3.

A potent, selective, orally active S1P1 antagonist with IC50 of 2.5 nM Ca2+ mobilization assays, without activity on S1P2, S1P3 and S1P4 (IC50>10 uM).

Ralmitaront, also known as WHO 11130, RO 6889450 and RG7906, is a neuroleptic.

ML299 is a potent, CNS penetrant, dual phospholipase PLD1/PLD2 probe with IC50 of 6 nM/20 nM, respectively.

A BIX-01294 derivative that inhibit malaria parasite histone methyltransferases, resulting in rapid and irreversible parasite death.

CLK inhibitor T3 (T3) is a highly potent, selective, and cell-based stable CDC-like kinase (CLK) inhibitor with 0.67, 15 and 110 nM for CLK1,2 and 3, respectively.

Novel Orally Available Polymerase Inhibitor, Showing Efficacy Against a Lethal Morbillivirus Infection in a Large Animal Model

R243 is a potent, small molecule CCR8 antagonist that inhibits CCR8 signaling and chemotaxis, inhibits CCL1-induced Ca2+ flux and CCL1-driven peritoneal macrophages aggregation at 0.2 uM.

Ribocil is a synthetic mimic of riboflavin 5’-monophosphate (FMN) that competes with the natural ligand to inhibit FMN riboswitch-mediated expression of ribB.

ONO-8130 is an orally available EP1 receptor antagonist.

TRIM-473 is a novel ligand for the PRY-SPRY domain of the E3 RING ligase TRIM58 with EC50 of 5.3 μM.

PS 210 is a potent, specific activator of PDK1 that target the PIF-binding pocket of PDK1, does not alter the activity of any of the 121 kinases (S6K, PKB/Akt or GSK3)..

ATP competitive tyrosine kinase inhibitor

MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM.

Novel cyclin dependent kinase inhibitor

MELK-8a is a novel MELK inhibitor.

MC180295 (MC-180295, MC 180295) is a novel potent, highly selective CDK9 inhibitor with IC50 of 5 nM, displays >22-fold selectivity over other CDKs.

Cedazuridine (E7727) is a novel cytidine deaminase inhibitor, and a componet of ASTX727 for treatment of hematologic malignancies..

MAZ51 is an indolinone that selectively antagonizes the activation of VEGFR3 by VEGFC (IC50 = 1 µM) without blocking VEGFC-mediated stimulation of VEGFR2.

3-Hydroxy-4-methoxyacetophenone(Acetoisovanillone; Isoacetovanillone) is an active compound isolated from P. spinosa. Isoacetovanillone possesses anti-inflammatory activity and prevented injuries due to administration of acetic acid in the colon.

HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1.

Cerivastatin is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin reduces low-density lipoprotein cholesterol levels. Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect.

Lubiprostone, also known as RU-0211, is a medication used in the management of chronic idiopathic constipation, predominantly irritable bowel syndrome-associated constipation in women and opioid-induced constipation. It was initially approved by the U.S. Food and Drug Administration (FDA) in 2006. Lubiprostone is a bicyclic fatty acid derived from prostaglandin E1 that acts by specifically activating ClC-2 chloride channels on the apical aspect of gastrointestinal epithelial cells, producing a chloride-rich fluid secretion. These secretions soften the stool, increase motility, and promote spontaneous bowel movements (SBM).

Cdk1/2 Inhibitor III is a selective Cdk1/2 inhibitor, with an IC50 of 2.1 μM for CDK1/cyclin B.

RU-TRAAK-2 is a completely reversible TRAAK inhibitor, shows no activity for non-K2P channels (Kv1.2, Slo1 and GIRK2).

LY2365109 is a potent and selective GlyT1 inhibitors with IC50 value of 15.8 nM.