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.

MKC-1 is an orally bioavailable, small-molecule, bisindolylmaleimide cell cycle inhibitor with potential antineoplastic activity. MKC-1 and its metabolites inhibit tubulin polymerization, blocking the formation of the mitotic spindle, which may result in cell cycle arrest at the G2/M phase and apoptosis.

NBI 31772 is a nonpeptide ligand that releases insulin-like growth factor-1 (IGF-1) from its binding protein (IGFBP; Kis = 1-24 nM for the six human subtypes of IGFBP).1,2 As the released IGF-1 is biologically active, NBI 31772 is used to assess the role of IGF-1 in cells and animals, including in neuron survival, skeletal muscle regeneration, and glucose homeostasis.3,4,5

SKF-89976A was used to study the role of adenosine receptors in uptake of GABA transport.

Ro 60-0175 is a potent, selective 5-HT2C receptor agonist with pKi of 9, 7.5, 5.4, 5.2 and 5.6 for human 5-HT2C, 2A, 1A, 6 and 7 receptors respectively.

BAY-179 is a potent, selective, and species cross-reactive complex I inhibitor (IC50=79 µM).

Bretazenil, also known as Ro 16-6028, is GABA A receptor agonist potentially for the treatment of anxiety disorders. Bretazenil differs from traditional 1,4-benzodiazepines by being a partial agonist and because it binds to α1, α2, α3, α4, α5 and α6 subunit containing GABAA receptor benzodiazepine receptor complexes. 1,4-benzodiazepines bind only to α1, α2, α3 and α5 GABAA benzodiazepine receptor complexes.

CJ033466 is a novel and selective 5-HT4 receptor partial agonist with an EC50 of 9 nM and has gastroprokinetic effect.

Emivirine is a non-nucleoside reverse transcriptase inhibitors (NNRTIs) that displays potent and selective anti-human immunodeficiency virus type 1 (HIV-1) activity.

GSK329 is a potent and selective diarylurea inhibitor of the cardiac-specific kinase TNNI3K. GSK329 exhibits positive cardioprotective outcomes in the model of ischemia/reperfusion cardiac injury.

CAY10444 (BML-241) is a sphingosine-1-phosphate 3 (S1P3) antagonist. CAY10444 inhibits by 37% S1P-induced increases in Ca2+ in HeLa cells expressing S1P3 receptors[1].

(±)-ErSO is the racemate of ErSO. ErSO is a selective anticipatory unfolded protein response (a-UPR) activator.