TAOK inhibitor 43 is a novel potent, selective, ATP-competitive TAO Kinase (TAOK) inhibitor with IC50 of 11 and 15 nM against TAOK1 and TAOK2, respectively; increases the mitotic population, the percentages of mitotic cells displaying amplified centrosomes and multipolar spindles, induces cell death, and inhibits cell growth in centrosome-amplified SKBR3 or BT549 breast cancer cell models.

Acivicin is a glutamine analog that irreversibly inhibits glutamine-dependent amidotransferases involved in nucleotide and amino acid biosynthesis (Kis = 10 and 560 μM for anthranilate synthase and glutamate synthase, respectively).

A 1,2,5-thiadiazolidin-3-one-1,1-dioxide scaffold for design of protein tyrosine phosphatase-1B (PTP1B) inhibitor.

E3 ligase Ligand 4 is a ligand of E3 ligase, used in PROTAC technology.

LC-2 is a potent and first-in-class degrader of endogenous KRAS G12C with DC50 values between 0.25 and 0.76 μM. LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines.

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..

Tafenoquine succinate (SB-252263, Tafenoquine, WR 238605) is a long-acting, orally active anti-malarial agent to prevent malaria that is holoendemic for Plasmodium falciparum..

GSK-F1 is a potent inhibitor of PI4KA.

AY 9944 is a specific cholesterol biosynthesis inhibitor. AY 9944 inhibits the 7-dehydro cholesterol Δ7-reductase (DHCR7) enzyme (IC50=13 nM). AY 9944 causes hypocholesterolemia and accumulation of 7DHC. At high doses, AY 9944 inhibits also in cultured embryos sterol Δ7-Δ8 isomerase, which causes the accumulation of cholest-8-en-3β-ol.

NMDAR/TRPM4 inhibitor 9 (Compound 9) is a neuroprotective NMDAR-TRPM4 interaction interface inhibitor but spare the critical healthy NMDAR function.

BMS-986202 is a clinical Tyk2 inhibitor that binds to Tyk2 JH2 with IC50 of 0.19 nM and shows remarkably selectivity over other kinases including Jak family members.

PBT434 is a novel quinazolinone compound with effect of lowering cellular iron levels, prevents iron mediated neurodegeneration and α-synuclein toxicity in multiple models of Parkinson disease; inhibits iron-mediated redox activity and iron-mediated aggregation of α-synuclein, a protein that aggregates in the neuropathology; prevents loss of substantia nigra pars compacta neurons (SNpc), lowers nigral α-synuclein accumulation, and rescues motor performance in mice model of PD.

GRP-60367 hydrochloride is a first-in-class small-molecule rabies virus (RABV) entry inhibitor with nanomolar potency against some RABV strains. GRP-60367 hydrochloride specifically targets the RABV G protein.

Enantiomer of Entecavir

SSD114 is a novel GABAB positive allosteric modulator.

AZ32 is an orally bioavailable and blood-brain-barrier penetrating ATM inhibitor (AZ32) that radiosensitizes intracranial gliomas in mice.

GR 125,743 is a novel 5-HT1B/1D receptor antagonist.

A-395 potently inhibited the formation of H3K27me3 (via antagonizing EED in the trimeric PRC2 complex (EZH2:EED:SUZ12)) with IC50 = 34 ± 2 nM (Hill Slope = 0.7)

DGY-06-116 is an irreversible covalent, selective Src inhibitor.