K-Ras G12C-IN-4, compound 1, is a potent Covalent Inhibitor of KRAS.

AZD7507 (AZD-7507) is a potent, selective, orally available CSF-1R (c-FMS) with IC50 of 32 nM.

MF-766 (MF766) is a highly potent and selective EP(4) antagonist with binding Ki of 0.23 nM, displays no significant affinity (>7000-fold selectivity) against other PG receptors (IC50>1500 nM); behaved as a full antagonist with an IC50 of 1.4 nM (shifted to 1.8 nM in the presence of 10% HS) in the functional assay; exhibits blockade of inhibition of TNFa-induced IP10 release by the specific EP4 agonist L-000902688 (IC50=9.5 nM); demonstrates potency and efficacy of in the rat AIA model measuring inhibition of paw swelling.

Tetramethylglycerol (Tetramethylglycoluril) is a small molecule that acts on GABA Receptor, with anti-anxiety activity.

Rebamipide mofetil is an orally active prodrug of Rebamipide (OPC12759). Rebamipide is a mucoprotective agent. Rebamipide induces COX-2 expression, increases PGE2 levels, and enhances gastric mucosal defense in a COX-2-dependent manner.

MAP4K4-IN-17 is a potent and highly selective MAP4K4 inhibitor with IC50 of 14.9 nM, showes improved overall drug-like properties compared to PF-06260933.

Synucleozid hydrochloride (NSC 377363 hydrochloride) is a potent inhibitor of the SNCA mRNA that encodes alpha-synuclein protein (IC50=1.5 uM). Synucleozid selectively targets the alpha-synuclein mRNA 5? UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson's disease[1]. IC50 & Target: IC50: 1.5 uM (SNCA IRE RNA)[1] In Vitro: Synucleozid (0.25-1 uM; 24 hours) abrogates cytotoxicity induced by alpha-synuclein preformed fibrils, which act as seeds and recruit endogenous alpha-synuclein to aggregate[1]. Synucleozid (0-1 uM; 24 hours) binds to the A bulge near the base of the IRE hairpin, reduced levels of alpha-synuclein in a dose-dependent manner with an IC50 of 500 nM, and inhibits alpha-synuclein protein expression in SH-SY5Y neuroblastoma cells[1]. Synucleozid (100 nM-100 uM; 24 hours) binds to 2-AP-labeled and native IRE RNA with similar affinities. It decreases 2-AP emission with an EC50 value of 2.7 uM, recovery of 2-AP emissions is observed as a function of unlabeled SNCA IRE RNA (RNA-0) concentration, affording a competitive Kd of 1.5 uM[1]. Synucleozid (0.25-1 uM; 24 hours) decreases alpha-synuclein and other proteins that have IREs in their mRNA's UTR including APP, PrP, Ferritin and TfR as a dose-dependent mannner. All panels is completed in SH-SY5Y cells, except for PrP protein which is assessed in Neuro-2A cells[1].

MK-8591 (Islatravir, MK8591, EFdA) is a nucleoside analog that exhibits remarkable potency against wild-type and drug-resistant HIVs, inhibits HIV-1 reverse transcriptase with multiple mechanisms.

AA-Z-YVAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor with anti-inflammatory and anti-tumor activities.

Nacubactam (OP 0595, RG 6080, RO 7079901) is a diazabicyclooctane that inhibits class A and C β-lactamases with IC50 of <1 uM, also acts as a PBP2-active antibacterial.

2BAct (eIF2B activator 2BAct) is a novel, highly selective, CNS-permeable small molecule eIF2B activator with EC50 of 33 nM in cell-based reporter assays.

Pamiparib (BGB-290, BGB290) is a highly potent, selective and brain penetrant PARP1/2 inhibitor with potent anti-tumor activity.

MYLS22 is a first-in-class and selective optic atrophy 1 (OPA1) inhibitor. MYLS22 can target endothelial OPA1 to curtail tumor growth and inhibits angiogenesis by impinging on NFkB activity and on angiogenic gene expression.

SHIN1 is a potent dual inhibitor of human serine hydroxymethyltransferase 1/2 (SHMT1/2).

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)..