BLI-489 is a bicyclic penem inhibitor that inhibits class A, C, and D beta-lactamases with synergistic effects with piperacillin; The combination of piperacillin-BLI-489 demonstrated improved activity compared to that of piperacillin-tazobactam against the problematic extended-spectrum beta-lactamase- and AmpC-expressing strains.

BL-6020/979 (SNT207979) is an orally available, selective, potent MC4R antagonist with IC50 of 19 nM; weakly binds to MC-3 and MC-5 receptors with IC50 of 2.7 uM and 0.89 uM, respectively, >10,000-fold selectivity over MC-1R; demonstrates in animal models and presents a promising candidate suitable for further development towards a first-in-class treatment option for cachexia.

BJG-03-025 is a potent, highly selective FAK tyrosine kinase inhibitor with biochemical IC50 of 20.2 nM.BJG-03-025 demonstrates excellent kinome selectivity was profiled by KINOMEscan screening, PLK1 proved to be a false positive with IC50 of 8.3 uM, 100-300-fold selective for FAK.BJG-03-025 displays antiproliferative activity in three-dimensional (3D)-breast and gastric cancer models and impacts cellular signaling and migration.BJG-03-025 decreased phosphorylated FAK (pFAK Y397) in gastric cancer CDH1–/–RHOAY42C/+ organoid model, decreased aberrant signaling and proliferation of gastric cancer organoids.

bio-THZ1 is a biotinylated version of THZ1 and binds irreversibly to CDK7.

BIO-2007817 is a small-molecule positive allosteric modulator of Parkin E3 ligase with EC50 of 0.17 uM (TR-FRET).BIO-2007817 stimulated Parkin autoubiquitination as measured by Western blots in a concentration-dependent manner, was also able to induce the appearance of monoubiquitinated forms of Miro1.BIO-2007817 induced the appearance of slower-migrating Parkin species in a concentration-dependent manner with maximal efficacy at 20 uM in Parkin autoubiquitination assay.BIO-2007817 does not affect the rate of Parkin translocation to mitochondria nor the number of mitochondria within lysosomes.

BI-8668 (BI 8668) is a highly potent and selective epithelial sodium channel (ENaC) inhibitor, inhibits Na+ current with IC50 of 17 nM (Ussing chamber assay); BI-8668 inhibits ENaC-mediated water permeability through cell monolayers of the cell line M-1 (M-1 cells: mouse kidney tubules cells) with 81% inhibition at 3 uM.

BI-4916 (BI-4916) is the prodrug of BI-4924, which is a potent, selective NADH/NAD+-competitive PHGDH inhibitor with IC50 of 2 nM.

BI-4020 (BI 4020) is a potent, next generation, wt-sparing inhibitor of EGFR mutant T790M and/or C797S, and EGFRdel19 T790M C797S (0.2 nM).BI-4020 inhibits not only the triple mutant EGFRdel19 T790M C797S variant but also the double mutant EGFRdel19 T790M and primary mutant EGFRdel19 while sparing activity against EGFRwt.BI-4020 shows high potency on EGFR mutant cells, high kinome selectivity, and good DMPK properties.BI-4020 exhibites tumor regressions in the human PC-9 (EGFRdel19 T790M C797S) triple mutant NSCLC xenograft model in mice.

BI-1915 (BI 1915) is a highly potent, selective inhibitor of Cathepsin S (CatS) with IC50 of 17 nM for in vitro use, no significant inhibition on Cathepsin L/K/B (IC50>10 uM); BI-1915 effectively blocks the specific ovalbumin induced IL-2 secretion in T-cells with an EC50 value of 2.8 nM. BI-1915 shows excellent selectivity against related cathepsins with IC50 values of >10 µM (Cat K and Cat B) and >30 µM (Cat L).

BI-1124 (BI 1124) is a highly potent, selective inhibitor of Cathepsin S (CatS) with IC50 of 7 nM, >40-fold selectivity over Cathepsin L/K/B; BI-1124 had a superior PK profile and showed dose-dependent inhibition of the ovalbumin induced IL-2 secretion in a T cell receptor transgenic DO11 mouse model with an IC50 of 0.3 mg/kg.

Benzopyran-G1 is a selective inhibitor of cardiac acetylcholine-activated inwardly rectifying K+ current (IKACh), composed of Kir3.1/Kir3.4 heterotetrameric and Kir3.4 homotetrameric channel subunits.

BDM88855 is a novel allosteric efflux-pump inhibitor that potentiate antibiotic activity in E. coli through inhibition of its primary RND transporter, AcrAB-TolC.BDM88855 binds to a unique site on the transmembrane domain of the AcrB L protomer, lined by key catalytic residues involved in proton relay, boost antibiotic activity in E. coli by inhibiting the AcrAB-TolC efflux pump.

BDM88855 Hcl is a novel allosteric efflux-pump inhibitor that potentiate antibiotic activity in E. coli through inhibition of its primary RND transporter, AcrAB-TolC.BDM88855 binds to a unique site on the transmembrane domain of the AcrB L protomer, lined by key catalytic residues involved in proton relay, boost antibiotic activity in E. coli by inhibiting the AcrAB-TolC efflux pump.

BC-N102 is a first-in-class novel small molecule inhibitor for targeting oncogenic and hormonal signaling in ER-positive breast cancer.BC-N102 exhibits anticancer activity against breast cancer cell lines via interfering with cell cycle regulatory proteins and hormonal receptors signaling in vitro (IC50=0.04-10 uM), no significant activities against a normal breast cell line.BC-N102 exhibits potent antitumor activity at tolerated doses in an ER+ human xenograft breast cancer model.BC-N102 induces arrest of the cell cycle at G0/G1 phase, downregulates the expression of CDK2 and CDK4 independent of the ER in breast cancer cell lines.

BC-DXI-495 is a specific small molecule inhibitor of AIMP2-DX2-HSP70 interaction, specifically reduced the levels of DX2 (IC50=4.2 uM) but not AIMP2-F, and the viability of lung cancer cells (EC50=14 uM).BC-DXI-495 bound to DX2 with KD of 14 uM.BC-DXI-495 specifically reduced the levels of endogenous DX2 protein but not of AIMP2-F , affected the DX2 protein level, but not mRNA level.BC-DXI-495 inhibited DX2-dependent cell growth, significantly diminished tumor growth in a xenograft model of H460 cells, with little effect on body weigh.BC-DXI-495 significantly suppressed the growth and weight of tumors expressing DX2 WT, but not L80A mutant.

BAY-155 (BAY155) is a novel, potent and selective menin-MLL inhibitor with binding IC50 of 8 nM, 10-fold better compared to that of MI-503; BAY-155 demonstrated a significantly enhanced selectivity profile compared to MI-503 in a panel of assays covering numerous safety pharmacology-relevant targets including GPCRs, ion channels and transporters. BAY-155 shows anti-proliferative activity in a large cell line panel, exhibits specific therapeutic activityin AML/ALL models.

Bamocaftor (VX-659) is a next-generation CFTR corrector, restores F508del-CFTR protein function.

Azoffluxin (CMLD012336) is a bis-benzodioxolylindolinone that synergizes with fluconazole against C. auris through the inhibition of efflux pump Cdr1, thus increasing intracellular fluconazole levels.Azoffluxin increases intracellular accumulation of fluconazole (FLC) by inhibiting Cdr1-mediated efflux in C. auris.Azoffluxin potentiates intracellular acting compounds against C. auris, to a similar degree as deletion of CDR1.Azoffluxin is active against diverse C. auris strains, azoffluxin potentiated fluconazole in multiple isolates from three of the four major clades. The clade III isolates from South Africa were the exception.Azoffluxin enhances fluconazole (FLC) activity against azole-resistant C. albicans isolates.Azoffluxin not only enhanced fluconazole activity but also reduced fungal burden by ~1000-fold as a single agent in mice infected with drug-resistant C. auris.

Azo-EMD is a cell permeable, photoswitchable compound that inhibits mitotic kinesin Eg5 more potently in its light-induced cis form, used for optical control mitosis.Under UV light conditions, HeLa cells undergo mitotic arrest, as evidenced by the formation of a monopolar spindle.

AZD1332 is a potent, selective, ATP-competitive neurotrophic tyrosine kinase receptor (NRTK;TRK) inhibitor with IC50 of <10 nM; inhibits phosphorylation of TrkA/B/C in MCF10A cells overexpressing TrkA and NIH3T3 cells over expressing TrkA, TrkB, or TrkC with IC50 of <5 nM, inhibits a panel Baf3 survival driven by TrkA, TrkB, or TrkC with EC50 of 2 nM, AZD 1332 is orally available.

AZ7 (PI4KA inhibitor 7) is a potent, selective PI4KA inhibitor with pIC50 of 8.2, >100-fold selectivity over PI4Kβ, PI3Kα and PIP5Kγ.AZ7 inhibited the accumulation of IP1 (pIC50 6.3) caused a qualitative reduction in cellular PIP, PIP2 and PIP3 levels.PI4KA inhibitor 7 inhibited cell growth with pGI50 values of >5.0 in 91 of the cell lines in a panel of 183 cancer cell lines.

AZ3 (PI4KB inhibitor 3) is a seletive PI4KB inhibitor with pIC50 of 7.8, shows good lipid kinase selectivity (pIC50 5.1, 4.7 and 4.0 for PI4Kα, PI3Kα and PIP5Kγ respectively).

AXKO-0046 (AXKO0046) is the first highly selective, small molecule inhibitor of human lactate dehydrogenase B (LDHB), exhibits uncompetitive LDHB inhibition with EC50 of 42 nM.AXKO-0046 selectively inhibited LDHB activity in an uncompetitive manner with respect to NADH and pyruvate, no inhibitory activity against LDHA at 300 uM.AXKO-0046 did not bind in the catalytic site of the enzyme but significantly bound to LDHB in the novel allosteric site of the tetramer.AXKO-0046 is a promising chemical probe to elucidate the role of LDHB-associated pathways in cancer metabolism.

Autotaxin-IN-13 ( ATX-i) is a highly potent, selective Autotaxin inhibitor with IC50 of 6 nM.Autotaxin showed sufficient oral bioavailability and low plasma clearance in vivo as well as a suitable half-life to allow for bid or food admix dosing.

Autoquin is a novel autophagy inhibitor (IC50=0.56 uM) by indirect modulation of the activity of the lysosomal enzymes acid sphingomyelinase and acid ceramidase; Autoquin showed a dose‐dependent inhibition of EGFP‐LC3 puncta after 3 hours upon autophagy induction by amino acid starvation in the primary screening assay. Autoquin is a lysosomotropic compound that acts as a functional inhibitor of acid sphingomyelinase, increases lysosomal mass and sequesters Fe2+ to the lysosomes in MCF7 cells, causing an increase in lysosomal reactive oxygen species.

Autophazole is a novel autophagy inhibitor, promotes cancer cell death via caspase activation.Autophazole was internalized into lysosomes of cells where it induced lysosomal membrane permeabilization (LMP), promoted LMP-mediated apoptosis.LMP induced by Autophazole caused release of cathepsins from lysosomes into the cytosol. Cathepsins in the cytosol cleaved Bid to generate tBid, which subsequently activated Bax to induce mitochondrial outer membrane permeabilization (MOMP).Autophazole is a new chemical probe in efforts aimed at gaining a better understanding of the autophagic process.

Autophagy inducer D61 is a small molecule autophagy inducer with antibacterial activity, induces LC3II and promotes aggregation of LC3II near Salmonella.D61 (25 uM) reduced the bacterial load (GFP signal in RAW 264.7 macrophages) by 20-fold, with IC50 of 1.3 μM in the SAFIRE assay.D61 antibacterial activity depends on the VPS34 complex and on ATG5.D61 also reduced Salmonella load in the spleens and livers of infected mice.D61 antibacterial activity in macrophages is synergistic with the antibiotic chloramphenicol but that this synergy is largely independent of the known autophagy-stimulating activity of chloramphenicol.Salmonella enterica is a natural bacterial pathogen of humans and animals that causes systemic infection or gastroenteritis.

Atg4B inhibitor 21f is a potent competitive inhibitor for Atg4B with Ki of 3.1 uM.Atg4B inhibitor 21f enhanced the anticancer activity of anti-CRPC drugs via autophagy inhibition.

AstraZeneca CCR4 antagonist is a potent, selective CCR4 antagonist, inhibits CCR4 ligand macrophage-derived chemokine (MDC/CCL22) in CCR4+CD4+ T cells.

ASR490 (ASR 490) is a small molecule that binds to NRR of Notch1, specifically inhibits Notch1-mediated survival of colorectal cancer cells (IC50=0.6-1.2 uM); ASR490 overcomes Notch1 overexpression and inhibits the growth of HCT/Notch1 transfectants, reduces Notch1-mediated tumor burden in xenografts.