Selective blocker of the Aquaporin-1 ion channel conductance, slowing cancer cell migration

LEM-14 is a specific inhibitor of histone lysine methyltransferase NSD2 (MMSET/WHSC1) with in vitro IC50 of 132 uM, and that is inactive against the closely related NSD1 and NSD3..

Bractoppin is a potent, small-molecule chemical inhibitor that specific selectively blocks phosphopeptide recognition by the BRCA1 tBRCT domain with binding IC50 of 74 nM; shows no inhibition for recognition of cognate biotinylated phosphopeptides to the TOPBP1 tBRCT 7/8, or GRB2 SH2 proteins; engages BRCA1 tBRCT residues recognizing pSer in the consensus motif, pSer-Pro-Thr-Phe, plus an abutting hydrophobic pocket; inhibits substrate recognition detected by Förster resonance energy transfer, and diminishes BRCA1 recruitment to DNA breaks, in turn suppressing damage-induced G2 arrest and assembly of the recombinase, RAD51; selectively interrupts BRCA1 tBRCT-dependent signals evoked by DNA damage.

Novel inhibitor of the VP40 matrix protein

PU-H54 is potent, selective Grp94 inhibitor.

Positive Allosteric Modulators (PAMs) of mGlu5 with Competitive MPEP-Site Interaction

Potent, reversible, and ATP-competitive inhibitor of human Thymidylate kinase (TMPK)

Inhibitor of placental alkaline phosphatase (PLAP)

Talinolol is a beta(1)-adrenergic receptor antagonist and a probe drug for P-glycoprotein (P-gp) activity in humans.

hPGDS-IN-1 is a potent, selective hPGDS inhibitor with IC50 of 12 nM in FP or EIA assays..

α-Adrenergic blocker

A discontinued antiemetic drug used in post-operative care

Novel NMDA receptor antagonist

Novel non-toxic fluorescent probe to label the renal proximal tubules in zebrafishReference1) The small molecule probe PT-Yellow labels the renal proximal tubules in zebrafish; Chem Commun (Camb). 2015;51(2):395-8. doi: 10.1039/c4cc08075k. Epub 2014 Nov 1

Novel ligand for the Methyl-lysine Binding Protein, 53BP1.

Novel highly potent BET bromodomain inhibitor with more than 100-fold higher cellular potency than the corresponding monovalent antagonist JQ1

Anti-inflammatory drug

Novel inhibitor of human betaine-homocysteine S-methyltransferase (BHMT)References: 1) Strakova J, Gupta S, Kruger WD, Dilger RN, Tryon K, Li L, Garrow TA. Inhibition of betaine-homocysteine S-methyltransferase in rats causes hyperhomocysteinemia and redu

Gene-selective LXR modulator that mediates potent transcriptional activation of ABCA1 gene expression while exhibiting minimal effects on SREBP-1c

Full 5-HT1A serotonin receptor agonist; more active enantiomer.

A GABA antagonist that acts via the benzodiazepine binding site of ag containing GABA receptors

Novel activator of the transient receptor potential channel ML3 (TRPML3)

Psychostimulant that displays neuroprotective and antiparkinsonian activity in a primate model of Parkinson's disease