Compound 32 (HER2) is a potent and selective covalent inhibitor of HER2/WT and HER2/YVMA with IC50 of 49 nM and 42 nM, respectively.

IDE397 is a potent inhibitor of MAT2A, which is developed to selectively exploit this synthetic lethal vulnerability in MTAP−/− tumors.

AK59-51TB (AK59) is a STING degrader leveraging HERC4, a HECT-domain E3 ligase.

UNC8153 TFA is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a Kd of 24 nM. UNC8153 TFA reduces the cellular levels of both NSD2 protein and the H3K36me2 chromatin mark. UNC8153 TFA contains a simple warhead that confers proteasome-dependent degradation of NSD2.

NecroX-7 is a potent free radical scavenger and a HMGB1 (high-mobility group box 1) inhibitor. NecroX-7 can be used as an antidote to acetaminophen toxicity. NecroX-7 exerts a protective effect by preventing the release of HMGB1 in ischemia/reperfusion injury. NecroX-7 inhibits the HMGB1-induced release of TNF and IL-6, as well as the expression of TLR-4 and receptor for advanced glycation end products. NecroX-7 can be used graft-versus-host disease (GVHD) research.

NecroX-2 is a small molecule necrosis modulator and potent antioxidant molecule, which can be bound to some types of radicals and especially NAPQI.

PRMT5 inhibitors; PRMT5 inhibitors;

PDE4B-IN-2 is an orally active and selective PDE4B inhibitor with an IC50 of 15 nM. PDE4B-IN-2 inhibits PDE4D (IC50=1.7 µM). PDE4B-IN-2 exhibits potent anti-inflammatory effects.

IM-54 is a cell permeable, potent and selective inhibitor of necrosis.

BSJ-03-204 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-03-204 is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 does not induce IKZF1/3 degradation and has anti-cancer activity.

VK-2019 is a selective EBNA1 inhibitor. VK-2019 was developed as a highly specific inhibitor of EBNA1 DNA binding activity and is currently in phase 1 development as a treatment for EBV-associated carcinomas. EBNA1 is an Epstein Barr virus (EBV) protein expressed in all EBV-associated cancers. EBNA1 plays a critical role in the replication and maintenance of EBV episomes in latently infected cells.

Acifran (AY 25712), an antihyperlipidemic agent, is an orally active agonist of GPR109A (HM74A) and GPR109B, the high and low affinity receptors for Niacin.

Ipsapirone, also known as BAY q 7821, is a new pyrimidinylpiperazine ligand potent and specific for 5-HT1A receptors. Ipsapirone hydrochloride has potential therapeutic use in affective disorders.

Novel potent inhibitor of dihydroorotate dehydrogenase (DHODH)

Neuropathiazol selectively induces neuronal differentiation of primary hippocampal neural progenitor cells. It is more potent and selective compared to retinoic acid. Also suppresses astrocyte differentiation.

EGFR-IN-99 (compound 1a) is a potent EGFR and HER2 Exon 20 insertion mutant inhibitor. EGFR-IN-99 has excellent antiproliferative activity against DFCI127 cells, with an EC50 of 11.5 nM. EGFR-IN-99 can be used for the research of non-small cell lung cancer (NSCLC).

Peroxisome proliferator-activated receptor-α/γ (PPAR α/γ) dual agonist

IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.

PE 154 are known to associate with β-amyloid plaques, and histological co-localization of AChE and Ab peptides is well established in Alzheimer’s disease. PE-154 is a fluorescent inhibitor of both AChE and BChE with IC50 values of 280 pM and 16 nM. PE-154 stains Aβ plaques in both rodent and human tissue samples, and does not cross react with phospho-tau.

Anavex2-73 is a muscarinic/σ1 ligand. ANAVEX2-73 (0.01-3.0 mg/kg i.p.) alleviated the scopolamine- and dizocilpine-induced learning impairments. ANAVEX2-73 (300 μg/kg) also reversed the learning deficits in mice injected with Aβ(25-35) peptide, a non-transgenic Alzheimer's disease model. The neuroprotective activity of ANAVEX2-73, its mixed cholinergic/σ(1) activity, its low active dose range and its long duration of action together reinforce its therapeutic potential in Alzheimer's disease.

Novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe

H2L5186303 is a potent and selective LPA2 receptor (lysophosphatidic acid 2 receptor) antagonist with an IC50 of 9 nM.

OBX02-011 is a potent, reversible, fourth-generation EGFR tyrosine kinase inhibitor (TKI) that overcomes the EGFR C797S mutation, inhibits triple mutants Del19/T790M/C797S and L858R/T790M/C797S with IC50 of 0.134 and 2.09 nM, respectively.

TES-1025 (TES1025) is a potent, selective inhibitor of human ACMSD (α-Amino-β-carboxymuconate-ε-semialdehyde decarboxylase) with IC50 of 13 nM, increases NAD+ levels in cellular systems.