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.

Ansornitinib is an orally active dual kinase inhibitor that inhibits platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR2). Ansornitinib can be used as an antifibrotic agent in lung, liver, kidney, and gastrointestinal fibrotic diseases.

Kakeimide is a potent GH3 inhibitor that selectively targets IAA-conjugating GH3 proteins at subnanomolar concentrations in vitro, shows auxin-like activity by inhibiting endogenous IAA catabolism.

ARQ 621 is an allosteric, and selective Eg5 mitotic motor protein inhibitor. Phase 1.

MNI137 is a potent and selective negative allosteric modulator for group II mGluRs. MNI137 has IC50s values of 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization.

(R)-ZINC-3573 is a potent, selective agonist of the atypical opioid receptor MRGPRX2 (EC50=0.76 uM), showing little activity against 315 other GPCRs and 97 representative kinases.

H3B-120 is a competitive, selective and allosteric inhibitor of carbamoyl phosphate synthetase 1 (CPS1) with IC50 of 1.5 μM and Ki of 1.4 μM. H3B-120 exhibits anti-tumor activity.

(S)-ZINC-3573 is a negative control for (R)-ZINC 3573. (S)-ZINC-3573 displays no activity at MRGPRX2 at concentrations below 100 μM.

PSB1115 is a highly selective, water-soluble, human A2B adenosine receptor antagonist. PSB1115 has Ki values are 53.4, > 10000 and > 10000 nM at human A2B, A1 and A3 receptors respectively. It produces potent analgesic effects in vivo.