Novel rapamycin derivative, targeting polycystic kidneys due to the high expression of the folate receptor (FRα), lacking the extra-renal effects of unconjugated rapamycin, in particular immunosuppressive effects

Novel potent antimalarial agent, binding to ferriprotoporphyrin-IX (FeIII-PPIX) (Kd = 33 nM) against chloroquine-resistant and sensitive strains of Plasmodium falciparum

Potent, selective, noncompetitive glutamate mGluR5 receptor antagonist

Non-steroidal anti-inflammatory drug, being used for symptomatic relief for rheumatoid arthritis, osteoarthritis, and mild to moderate pain

Non-steroidal antiinflammatory agent

Novel oral iron therapy agent, being effective in correcting iron deficiency anemia in patients with inflammatory bowel disease

Novel ferroptosis inducer, killing selected cancer cell lines by harnessing reactive oxygen species (ROS)

Iron chelator, mediating iron transport in Streptomyces pilosus

Natural potent colchicine site binding microtubule-destabilizing agent with anti-proliferation and anti-metastasis activity via PAK1 and p21-mediated signaling in breast cancer cells

Selective orthosteric agonist of human FFA2

Selective and moderately potent positive allosteric modular (PAM)-agonist of the FFA3 receptor

Novel PAM-antagonist of the function of C3 at FFA3

Novel fluorescent probe as an excellent VMAT2 substrate capable of detecting VMAT2 activity in intact cells using fluorescence microscopy

Potent, reversible, ATP-competitive inhibitor against PDGFRβ, FGFR-1, and VEGFR-2 (IC50 = 20, 90, and 240 nM, respectively) and effectively suppresses VEGF-stimulated proliferation of HMVECs (EC50 = 420 nM).

Novel, covalent, highly potent, and exquisitely specific FGFR4 inhibitor

Novel potent and selective covalent inhibitor of FGFR4 kinase

Novel highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4, exhibiting excellent potency against FGFR4, FGFR4V550L, and FGFR4V550M with nanomolar activity in both the biochemical and cellular assays while sparing FGFR1/2/3

Novel potent and selective FGFR4 inhibitor, covalently binding to FGFR4 protein

Novel potentl and selective covalent FGFR inhibitor, inhibiting proliferation of FGFR-amplified cancer cell lines with low nM IC50 values

Novel regulator of transcription factor PU.1-DNA binding interactions, acting as a weak agonist that recruits PU.1 to DNA

Novel inhibitor of the Wnt/β-catenin transcriptional activity, demonstrating significant increased rate of apoptosis in Huh7 and PLC/PRF

Novel light-regulated diltiazem derivative, photoswitching LTCC in pancreatic β cells, cardiomyocytes and mouse hearts