PFKL activator NA-11 is a small-molecule, selective PFKL activator, inhibits the NOX2-dependent oxidative burst in neutrophils by activating the glycolytic enzyme phosphofructokinase-1 liver type (PFKL).

PDD 00017273 is the first-in-class, selective inhibitor of poly(ADP-ribose) glycohydrolase (PARG) with Kd, biochemical EC50 of 1.45 nM, 26 nM.

A xanthone derivative that fuctions as an EP and DP receptor antagonist.

BCATc Inhibitor 2 is a selective branched-chain aminotransferase (BCAT) inhibitor for research of neurodegenerative diseases. The IC50s of 0.2 μM, 0.8 μM and 3.0 μM for rat cytosolic isoenzyme rBCATc, human cytosolic isoenzyme hBCATc and rat mitochondrial isoenzyme rBCATm, respectively.

MMV390048 is a novel potent Plasmodium PI4K inhibitor with IC50 of 28 nM against intraerythrocytic life cycle stages of P. falciparum (NF54 drug-sensitive strain).

PF-06446846 (PF-6446846) is a potent, highly selective inhibitor of PCSK9 translation with IC50 of 0.3 uM for inhibition the secretion of PCSK9 by Huh7 cells.

GZD856 is a novel and orally bioavailable PDGFRα/β inhibitor with IC50s of 68.6 and 136.6 nM, respectively. Anti-lung cancer activities. Also a Bcr-AblT315I inhibitor with IC50s of 19.9 and 15.4 nM for Bcr-Abl and T315I mutant.

Bruton tyrosine kinase inhibitor

TIC10 inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics

NAcM-OPT is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor, which potently inhibits the DCN1-UBE2M interaction.

LIT-001 trifluoroacetate (LIT001) is the first nonpeptide Oxytocin receptor (OT-R) agonist with EC50 of 55 nM, Emax=96%.

Second generation papaverine analog, acting as an anticholinergic agent

AMG 009 is an orally active, small molecule CRTH2 (chemoattractant receptor-homologous molecule expressed on Th2 cells) and DP (D prostanoid) dual antagonist, which was in preclinical development in the US for the treatment of asthma and allergic rhinitis.

PBT 1033 (PBT 2) is an orally active copper/zinc ionophore. PBT 1033 restores cognition in mouse models of Alzheimer's disease (AD). PB 1033 also has antibacterial activity against Gram-positive bacteria.

SKLB-23bb is an orally bioavailable HDAC6-selective inhibitor and also has microtubule-disrupting ability.

NSC 663284 (SPS8I1;DA3003-1) is a potent inhibitor of the dual specificity protein phosphatase Cdc25 with Ki of 9/95//89 nM for Cdc25A/Cdc25B2/Cdc25C, displays 20- and 450-fold more selective over VHR or PTP1B phosphatases.

BAPTA/AM is a membrane permeable form of BAPTA, a selective chelator of Ca2+.

Daunomycinone (NSC-109351) is a metabolite of daunomycin. Daunomycin is an antibiotic with antitumor activity.

Carubicin HCl is an anthracycline antineoplastic antibiotic isolated from the bacterium Actinomadura carminata. Carubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis.

Zotarolimus (ABT-578, A 179578) is a semi-synthetic analogue of rapamycin, inhibits FKBP-12 binding with IC50 of 2.8 nM and shows less potent systemic immunosuppression than rapamycin.

Pristinamycin IA (Mikamycin B) is a cycle-peptidic macrolactone antibiotic. Pristinamycin IA is a substrate of P-glycoprotein and inhibits its function. Pristinamycin IA is active against StaphyloEoccus and Srreptococcus.

Photochlor, also known as HTTP, is a lipophilic, second-generation, chlorin-based photosensitizer. Upon intravenous administration, HPPH selectively accumulates in the cytoplasm of cancer or pre-cancerous cells. When laser light is applied, a photodynamic reaction between HPPH and oxygen occurs, resulting in the production of cytotoxic free radicals and singlet oxygen and free radical-mediated cell death. Compared to the first-generation photosensitizer porfimer sodium, HPPH shows improved pharmacokinetic properties and causes only mild skin photosensitivity which declines rapidly within a few days after administration.

Tildipirosin is a 16-membered macrolide used as an antibiotic in veterinary medicine. Like other macrolides, it inhibits protein synthesis in bacteria and blocks the production of biofilms.

Topotecan Hydrochloride (SKF 104864A Hydrochloride) is a Topoisomerase I inhibitor with potent antineoplastic activities.

Daptomycin is a lipopeptide antibiotic with rapid in vitro bactericidal activity against gram-positive organisms.

Anidulafungin

PF-05105679 is a potent, selective TRPM8 channel inhibitor with IC50 of 103 nM (human TRPM8 currents inhibition).

Brequinar sodium (DuP-785, Brequinar, NSC 368390) is a potent and selective inhibitor of DHODH with IC50 of 20 nM, triggers differentiation in the ER-HoxA9, U937, and THP1 cells with an ED50 of 1 uM.

Brequinar (DUP785) is a potent inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of 5.2 nM for human DHODH. Brequinar has potent activities against a broad spectrum of viruses. Brequinar also has an anti-SARS2 activity.

APD597(JNJ-38431055) is a GPR119 agonist intended for the treatment of type 2 diabetes, with EC50 of 46 nM for hGPR119.