NCI-006 is a potent new inhibitor of lactate dehydrogenase (LDH) that disrupts tumor growth in mice. LDH inhibition slows tumor growth but rapidly redirects pyruvate to support mitochondrial metabolism. Inhibiting both mitochondrial complex 1 and LDH suppresses metabolic plasticity of glycolytic tumors in vivo, significantly prolonging tumor growth inhibition.

BI-4924 (BI 4924) is a potent, selective NADH/NAD+-competitive PHGDH inhibitor with IC50 of 2 nM.BI-4924 splays high selectivity against the majority of other dehydrogenase targets.

TAS-119 is a potent, selective and orally active Aurora A inhibitor with an IC50 of 1.0 nM. TAS-119 shows high selectivity for Aurora A over other protein kinases, including Aurora B (IC50 of 95 nM). TAS-119 has potent antitumor activites.

KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1/2

ACT-541468 is a dual orexin receptor antagonist.

Sodium channel blocker. Suppresses tetrodotoxin (TTX)-resistant Na+ currents approximately twice as selectively as TTX-sensitive currents. Antinociceptive; displays analgesic effects in animal models of inflammatory and neuropathic pain.

EB-42486 is a novel, potent, and highly selective G2019S-LRRK2 inhibitor (IC50 < 0.2 nM).

ISO-1 is a macrophage migration inhibitory factor (MIF) antagonist with an IC50 of 7 μM.

PF-06821497 (compound 23a) is a potent, selective and orally active Enhancer of Zeste Homolog 2 (EZH2) inhibitor, with a Ki value <0.1 nM against mutant Y641N EZH2. Exhibits robust tumor growth inhibition.

Branaplam (LMI070; NVS-SM1) hydrochloride is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC50 of 20 nM for SMN. Branaplam hydrochloride inhibits human-ether-a-go-go-related gene (hERG) with an IC50 of 6.3 μM. Branaplam hydrochloride elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model.

FMK 9a is an autophagin-1 inhibitor with IC50 values of 80 and 73 μM in FRET and LRA assay.

SSR-240612 is a bradykinin B1 receptor antagonist potentially for the treatment of chronic pain.

GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect.

VU0360172 is a positive allosteric modulator of mGlu5 receptors (EC50 = 16 nM; Ki = 195 nM). VU0360172 is selective for mGlu5 and it displays no significant activity at mGlu1, mGlu2 or mGlu4 receptors.

Cadralazine is a peripheral arteriolar vasodilator and an antihypertensive drug.

Beclamide is a drug that possesses anticonvulsant activity. It is no longer used. Beclamide is possibly metabolized to 3-chloropropanoic acid in vivo, which binds to the GHB receptor. It has been used as a sedative and as an anticonvulsant. It was studied in the 1950s for its anticonvulsant properties, as a treatment for generalised tonic-clonic seizures. It was not effective for absence seizures. Interest in the drug resumed in the 1990s for its psychiatric properties as an adjunct in the treatment of schizophrenia. While not classified as a DEA controlled substance in the United States, this product can only be sold STRICTLY to universities and research institutions. This product will not be sold to individuals or shipped to residential addresses.

SPP-86 is a potent RET inhibitor.

AOD-9604 is a potential anti-obesity peptide based on human growth hormone. AOD9604 was originally developed after research on mice, but subsequent studies in human have shown no efficacy for the potential treatment of obesity.

Viridicatol is a fungal metabolite that has been found in various Penicillium species as well as Phoma with antimicrobial properties.