Cinobufagin, a kind of Chinese materia medica with antitumor effect, is widely used in clinical practice, especially in anti-liver cancer. IC50 value: Target: In vitro: Cinobufagin inhibited proliferation of cancer cells at doses of 0.1, 1, or 10 μM after 2–4 days of culture. Cytotoxicity of cinobufagin on the DU145 and LNCaP cells was dose-dependent. Cinobufagin increased [Ca2+]i and apoptosis in cancer cells after a 24-hr culture as well as caspase 3 activities in DU145 and PC3 cells and caspase 9 activities in LNCaP cells [1]. Cinobufagin suppresses cell proliferation and causees apoptosis in prostate cancer cells via a sequence of apoptotic modulators, including Bax, cytochrome c and caspases [2].

UCB-9260, an orally active compound, inhibits TNF signalling by stabilising an asymmetric form of the trimer. UCB-9260 is selective for TNF over other superfamily members, and binds TNF with a similar Kd of 13 nM.

EDP-305 is a novel and potent farnesoid X receptor (FXR) agonist, with no/minimal cross-reactivity to TGR5 or other nuclear receptors.

PF00835231(SARS-CoV-2 inhibitor 5h) is areversible-covalent inhibitor of SARS-CoV-2 main protease (Mpro) with EC50 of 4.2 µM. Compound 5h blocks the infectivity and cytopathicity of the virus with high potency and without any detectable cytotoxicity even at 200 µM.PF-00835231 is a potent inhibitor of CoV-2 3CLpro with IC50 of 4 nM and shows suitable pharmaceutical properties to warrant further development as an intravenous treatment for COVID-19.

GRL-1720 is an irreversible, covalent inhibitor of SARS-CoV-2 main protease (Mpro) with EC50 of 15 µM.

Compound 5i is a novel and brain-penetrant O-GlcNAcase inhibitor with IC50 of 46 nM.

JMX0493 is a potent inhibitor of human adenoviruses (HAdVs) with IC50 of 0.78 μM and displays high selectivity index (SI>100) and 2.5-fold virus yield reduction compared to niclosamide. JMX0493 targets the HAdV entry pathway that prevents viral particle disassembly and subsequent release from the endosome.

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CH7233163 is a novel selective inhibitor of various types of EGFR mutants including L858R/T790M/C797S, L858R/T790M, Del19/T790M, Del19, and L858R, showing potent antitumor activities

Reuterin is a broad-spectrum antimicrobial agent active against Gram positive and Gram negative bacteria, as well as yeasts, moulds and protozoa. Reuterin is produced by specific strains of Lactobacillus reuteri during anaerobic metabolism of glycerol. Reuterin also demonstrates potent antimicrobial activity against a broad panel of human and poultry meat campylobacter spp. Isolates.

Lefamulin acetate is a pleuromutilin antibiotic that is being developed by Nabriva Therapeutics for the treatment of acute bacterial skin and skin-structure infections.

A potent GSK3β inhibitor with IC50 of 22 nM.

LY2157299 is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM. Phase 2.

Formoterol fumarate(Foradil) is a potent, selective and long-acting β2-adrenoceptor agonist.

Danirixin(GSK1325756) is a selective CXCR2 antagonist.

Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.

OSU-03012(AR-12) is a potent inhibitor of recombinant PDK-1 with IC50 of 5 μM and 2-fold increase in potency over OSU-02067.

EC5026 (BPN-19186) is a first-in-class, potent and orally active soluble Epoxide Hydrolase (sEH) inhibitor. Inhibition of sEH treats pain by stabilizing natural analgesic and anti-inflammatory mediators.

ODM-203 (ODM203) is a potent, selective, dual inhibitor of FGFR and VEGFR tyrosine kinases with approximately equal potency towards recombinant FGFR1, 2, 3 and 4, as well as VEGFR1, 2 and 3 (IC50=5-35 nM).

Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of macitentan, which is dual ETA/ETB antagonist designed for tissue targeting.

ML-109 is a potent and full thyroid stimulating hormone receptor (TSHR) agonist, with an EC50 of 40 nM.

C75 trans is the trans form of C75; C75 is a potent fatty-acid synthase(FASN) inhibitor with IC50 of 35.4 μM(LNCaP cell Proliferation inhibition).

Escitalopram Oxalate is a selective serotonin (5-HT) reuptake inhibitor (SSRI) with Ki of 0.89 nM.

Deferasirox (Exjade)

Elagolix is a Gonadotropin-Releasing Hormone (GnRH) Antagonist.

Efonidipine(NZ-105) Hcl monoethanolate is a dual T-type and L-type calcium channel blocker (CCB).

GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7.

Balixafortide(POL 6326) is a novel potent, selective, peptidic CXCR4 antagonist that interferes with the tumor-protective microenvironment and sensitizes tumor cells to chemotherapy.

SKL2001 is an agonist of the Wnt/β-catenin pathway, with anti-cancer activity.

CP-31398 is a small molecule p53 reactivator that protects p53 from thermal denaturation, not only reactivates mutant p53 but also induces stabilization of wild type p53.