Inhibitor of vasoconstrictor responses to sympathetic nerve stimulation, potentiating the actions of adrenaline and noradrenaline, increasing the blood glucose concentration and decreasing the appetite

First-In-Class Antagonist against the Adrenomedullin-2 (AM2) Receptor

Novel broad-spectrum inhibitor of coronavirus and enterovirus replication, targeting the main protease (Mpro or 3CLpro)

Novel potent histamine H3 receptor antagonist

Novel hepatitis B surface antigen (HBsAg) inhibitor for the treatment of hepatitis B virus infection

Next-generation NSAID-like γ-secretase modulator (GSM) with improved in vitro potency and brain penetration, effectively lowering Aβ42 production in cells and in amyloid precursor protein transgenic mice

Negative control as an inactive IDH1 inhibitor

Novel potent transrepression-selective liver X receptor modulator with anti-inflammatory activity

Potent inhibitor of bacterial type IIA topoisomerases

Selective inhibitor of iE-DAP-stimulated IL-8 release via the NOD1 signaling pathway

Novel potent inhibitor of bacterial type IIA topoisomerases

Novel potent protein kinase C-related kinase 1 (PRK1) inhibitor with IC50 of 40±8.7 nM)

Negative control for GSK073

Antimalarial

Highly potent, selective, SAM-competitive, and cell-active EZH2 inhibitor

Negative control for GSK8814

Selective glucocorticoid receptor agonist (SEGRA)

Novel agonist of the orphan nuclear receptors steroidogenic factor-1 (SF-1, NR5A1) and liver receptor homologue-1 (LRH-1, NR5A2)

Novel potent and selective BET pan-BD2 inhibitor

Negative control for GSK789

Novel Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitor

Novel potent inhibitor of EchA6

Novel stabilizer of Zα 1 -antitrypsin, blocking Zα 1 -antitrypsin polymerisation in vitro, reducing intracellular polymerisation and increasing the secretion of Zα 1 -antitrypsin threefold in an iPSC model of disease

Negative control for GSK699

Novel PCAF/GCN5 degrader, modulating PCAF/GCN5 immune cell function through a PROTAC approach

Novel, soluble, permeable, and selective BRD7/9 inhibitor

Novel ATM inhibitor with cancer cell specific radiosensitization activity

Potent polo-like kinase 1 (PLK1) inhibitor

Novel inhibitor of the Ribonuclease H Activity of HIV-1 Reverse Transcriptase

Novel potent EchA6 inhibitor