CS-3150 (Esaxerenone, XL-550) is a highly potent, selective and orally active non-steroidal mineralocorticoid receptor antagonist with IC50 of 9.4 nM; displays >1,000-fold selectivity over other steroid hormone receptors, glucocorticoid receptor, androgen receptor and progesterone receptor; inhibits aldosterone-induced transcriptional activation of human mineralocorticoid receptor with IC50 of 3.7 nM, shows superior potency to that of spironolactone and eplerenone; suppresses aldosterone-induced decrease in urinary Na(+)/K(+) ratio, inhibits blood pressure elevation induced by DOCA/salt-loading in rats.

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.

LDC195943(IMT1) is a highly specific inhibitor of human mitochondrial RNA polymerase (POLRMT).

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