LTGO-33 is a potent, selective inhibitor of voltage-gated sodium channel NaV1.8 with IC50 of 44 nM (hNaV1.8), 600-fold selectivity against NaV1.1-NaV1.7 and NaV1.9.

MZ-101 is a potent, selective inhibitor of glycogen synthase 1 (GYS1) with IC50 of 41 nM (human GYS1), with no inhibition against GYS2.

BAY-9835 is the first orally bioavailable ADAMTS7 inhibitor with IC50 of 6 nM, which is selective against a range of off-targets and metalloproteases except for ADAMTS12.

NAMPT activator (NAT) is a potent, small molecule activator of nicotinamide phosphoribosyltransferase (NAMPT) with ITC KD of 500 nM.

CRD733 (ASP4901) is a potent, selective cGMP-specific PDE9 (phosphodiesterase 9) inhibitor.

NSC74429 is a CNS-active, small molecule PHLPP inhibitor with IC50 of <5 uM, shows neuroprotective activity in primary rat cortical neurons in STS assay.

CS27109 is a potent, selective thyroid hormone receptor-β (THR-β) agonist with AC50 value of 1.98 uM, 12.6-fold selectivity over THR-α.

EN171 covalently targets both C38 and C96 on 14−3−3 to enhance 14−3−3 interactions with ERα, YAP, and TAZ, leading to impaired estrogen receptor and Hippo pathway transcriptional activity.

(R)-SKBG-1 is a covalent small molecule ligand of RNA-binding protein NONO, engages NONO Cys145 and suppress an array of cancer-relevant genes and impair cancer cell proliferation.

5M-8OH-Q is a specific small molecule inhibitor of UDP-glucose glycoprotein glucosyltransferase (UGGT), binds a CtUGGTGT24 “WY” conserved surface motif conserved across UGGTs (Kd=47 uM) but not present in other GT24 family glycosyltransferases.

AGI-25696 (AGI 25696) is a potent and selective inhibitor of methionine adenosyltransferase MAT2A, blocks the growth of MTAP-deleted tumors in vivo.

C902 is a small-molecule inhibitor targeting LIN28-let-7 interaction, shows dose-dependent inhibition in an EMSA validation assay with IC50 of 5 uM.

DB2313 is a small-molecule transcription factor PU.1 inhibitor abrogating DNA binding by PU.1 with Kd of 29 nM.

DS55980254 (DS 55980254) is potent, selective and orally active PTDSS1 (phosphatidylserine synthetase 1) inhibitor, suppresses phosphatidylserine (PS) production activity of PTDSS1 (IC50=100 nM) in cell-free assays, but not that of PTDSS2.

Kakeimide is a potent GH3 inhibitor that selectively targets IAA-conjugating GH3 proteins at subnanomolar concentrations in vitro, shows auxin-like activity by inhibiting endogenous IAA catabolism.

Macrocyclic peptide D4-2 is a macrocyclic peptide consisting of 15 amino acids that binds to the ectodomain of mouse SIRPα (Kd=10 nM, IgV-B6 SIRPα) and efficiently blocks CD47-SIRPα interaction in an allosteric manner (IC50=0.18 uM).

Ninerafaxstat 3HCl (CV-8972) is a small molecule compound that promotes glucose oxidation, decreases fatty acid oxidation and improve overall mitochondrial respiration, inhibits the growth and proliferation of cancer cells.

NOX-6-18 is a potent, selective GPR132 antagonist with IC50 of 17 nM.

PAT1inh-A0030 is a potent and selective SLC26A6 (putative anion transporter 1, PAT1) inhibitor with IC50 of 1.0 uM, shows no activity on relevant ion transporters/channels (SLC26A3, SLC26A4, SLC26A9, CFTR, TMEM16A).

PAT1inh-B01 is a small-molecule, selective SLC26A6 (putative anion transporter 1, PAT1) inhibitor, could fully inhibit PAT1-mediated anion exchange with IC50 of 350 nM.

Varoglutamstat (PQ912) is a potent glutaminyl cyclase (QC) inhibitor with Ki values of 20-65 nM for human, rat, and mouse QC activity.

PSB-CB-27 is a potent, selective antagonist of GPR18 with IC50 of 650 nM, shows no inhibition on GPR55 and low affinity for CB1/CB2 receptors.