Z-DEVD-AFC is a cell-permeant substrate for caspase-3, which causes a shift in fluorescence uponcleavage of the AFC fluorophore. Z-DEVD-AFC can be used to detect caspase-3-like enzymes activity.

Malformin A1, a cyclic pentapeptide isolated from Aspergillus niger, possess a range of bioactive properties including antibacterial activity. Malformin A1 shows potent cytotoxic activities on human colorectal cancer cells. Malformin A1 induces apoptosis by activating PARP, caspase 3, -7, and -9.

Indolicidin acetate is a potent antimicrobial peptide purified from the cytoplasmic granules of bovine neutrophils.

Arginase inhibitor 1 is a potent inhibitor of human arginases I and II with IC50s of 223 and 509 nM, respectively.

9-(2-Deoxy-2-fluoroarabinofuranosyl)guanine|2'-FANA-G

ACH-000143 is a novel potent melatonin receptor agonist with EC50 of 0.06 nM/0.32 nM against MT1/MT2. ACH-000143 leads to a reduction in body weight gain similar to dapagliflozin with superior results on hepatic steatosis and triglyceride levels in high-fat diet rats.

ICCB280 is a potent inducer of C/EBPα. ICCB280 exhibits anti-leukemic properties including terminal differentiation, proliferation arrest, and apoptosis through activation of C/EBPα and affecting its downstream targets (such as C/EBPε, G-CSFR and c-Myc).

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.

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.

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.

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

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.

Nucleozin targets influenza A nucleoprotein (NP), a multifunctional, RNA-binding protein necessary for virus replication.

IRAK inhibitor 1 is an interleukin-1 receptor associated kinase 4 (IRAK-4) inhibitor.

PF-3450074 (PF74) is a small molecule HIV capsid protein, destabilized the viral capsid in vitro.

SNAP-94847 is a selective, high-affinity, and competitive MCH1 receptor (MCH1-R) antagonist with Ki of 1.69 nM.

PWT143 (ME-401), is an orally bioavailable inhibitor of the delta isoform of phosphatidylinositide 3-kinase (PI3K), with potential antineoplastic activity.

NVP-LCQ195 (AT9311; LCQ195) is a small molecule heterocyclic inhibitor of CDK1, CDK2, CDK3 and CDK5 with IC50 of 1-42 nM.

LS-192629 is a novel OT-R antagonist.

GDC-0623 is a potent, ATP-uncompetitive inhibitors of MEK1(Ki=0.13 nM, +ATP).

A potent and selective antagonist of CXCR4 with IC50 of 13 nM in a CXCR4 125I-SDF inhibition binding assay.

NAB-14 is a potent, selective negative allosteric modulator of GluN2C/2D-containing NMDA receptors with IC50 of 580 nM, >800-fold selective over GluN2A/GluN2 receptors; inhibits triheteromeric (GluN1/GluN2A/GluN2C) NMDARs with modestly reduced potency and efficacy compared to diheteromeric (GluN1/GluN2C/GluN2C) receptors; inhibits GluN2D-mediated synaptic currents in rat subthalamic neurons and mouse hippocampal interneurons, but has no effect on synaptic transmission in hippocampal pyramidal neurons.

PF-915275 is a potent and selective inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) (Ki ＜ 1 nM) with good preclinical pharmacokinetic properties.IC50 value: ＜ 1 nM (Ki)[2]Target: 11βHSD1in vitro: PF-915275 maintains potency in our cellular assay against human 11βHSD1 (HEK293, EC50 = 5 nM) and is selective against human 11βHSD2 (HEK293, 1.5% inhibition 10 μM). PF-915275 displays only weak affinity for the rodent choline transporter (Ki = 9.6 μM) and the hamster melatonin MT3 receptor (Ki = 9.6 μM) in the Cerep Bioprint screening panel. PF-915275 has good in vitro pharmacokinetic properties. In particular, PF-915275 is categorized as a low clearance compound (liver microsome assays) with high permeability (Caco2 assay). [2]in vivo: As a prelude to in vivo studies with PF-915275, the rat pharmacokinetic properties of this compound were determined. PF-915275 has an excellent pharmacokinetic profile characterized by low clearance, long half-life and good oral bioavailability. [2]

Delafloxacin meglumine (ABT492 meglumine; RX-3341 meglumine; WQ-3034 meglumine) is a broad-spectrum fluoroquinolone antibiotic. Delafloxacin has a broad spectrum of activity that includes drug-resistant Staphylococcus aureus, Streptococcus pneumoniae, and