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.

Propargylcholine bromide is a choline analogue containing terminal propargyl that can be incorporated into all classes of Choline-containing phospholipids such as phosphatidylcholine and sphingomyelin, labeling Choline-containing phospholipids. Propargylcholine bromide-labeled phospholipid molecules can be visualized in cells with high sensitivity and spatial resolution.

Sobetirome(GC-1; QRX-431) is a member of a class of compounds known as selective thyromimetics.

Indibulin is a synthetic small molecule with antimitotic and potential antineoplastic activities. Indibulin binds to a site on tubulin that is different from taxane- or Vinca alkaloid-binding sites, destabilizing tubulin polymerization and inducing tumor cell cycle arrest and apoptosis. This agent has been shown to be active against multidrug-resistant (MDR) and taxane- resistant tumor cell lines. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

PS48 is a PDK1 (phosphoinositide-dependent protein kinase 1) activator which binds to the HM/PIF binding pocket rather than the ATP-binding site.

FDL-169 is a novel and potent CFTR (Cystic fibrosis transmembrane conductance regulator) corrector being developed by Flatley Discovery Lab for treating cystic fibrosis (CF) patients who carry the F508del mutation

UNC2541 is a potent and MerTK-specific inhibitor that exhibits sub-micromolar inhibitory activity in the cell-based ELISA. In addition, an X-ray structure of MerTK protein in complex with 11 was resolved to show that these macrocycles bind in the MerTK ATP pocket. UNC2541 showed IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM.

TG4-155 is a brain penetrant EP2 antagonist (KB = 2.4 nM) that is over 1000-fold less effective at EP4 (KB = 11.4 µM) and a panel of other receptors and channels. It blocks the induced expression of inflammatory markers in microglial cells.

GNF-5837 is a potent pan-Trk inhibitor which display antiproliferative effects in cellular Ba/F3 assays (IC50 values are 7, 9 and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively).

FITM is a nove mGlu1 inhibitor. FITM shows high affinity (Ki = 2.5 nM, fig. S2) and selectivity for mGlu1 over mGlu5.

FAUC 365 is a highly dopamine D3 receptor-selective antagonist with Ki values of 0.5 nM, 340, 2600, and 3600 nM at D3, D4.4, D2short, and D2Long receptors, respectively. FAUC 365 can be used for the research of schizophrenia, and Parkinson's disease.

Entasobulin is a β-tubulin polymerization inhibitor with potential anticancer activity.

CAY10594 is a potent phospholipase D2 inhibitor. CAY10594 ameliorates acetaminophen-induced acute liver injury by regulating the phosphorylated-GSK-3β/JNK axis.