KDOAM25 is a selective inihbitor of the KDM5 family histone demethylases JARID1A, JARID1B, JARID1C and JARID1D with IC50 values < 60 nM.

DBPR114 is a quinazoline-based multi-kinase inhibitor for the treatment of acute myeloid leukemia and other solid tumors.

N-Acetyl lysyltyrosylcysteine amide is a potent, reversible, specific, and non-toxic tripeptide inhibitor of myeloperoxidase (MPO). N-Acetyl lysyltyrosylcysteine amide effectively inhibits MPO generation of toxic oxidants in vivo. N-Acetyl lysyltyrosylcysteine amide reduces neuronal damage and preserves brain tissue and neurological function in the stroked brain. N-Acetyl lysyltyrosylcysteine amide inhibits MPO-dependent hypochlorous acid (HOCl) generation, protein nitration, and LDL oxidation.

NMDAR/TRPM4 inhibitor 8 (Compound 8) is a neuroprotective NMDAR-TRPM4 interaction interface inhibitor but spare the critical healthy NMDAR function.

PCNA-I1 is an inhibitor of proliferating cell nuclear antigen (PCNA) that binds to PCNA trimers (Kd = 0.41 µM) and dose-dependently reduces the level of PCNA associated with chromatin in PC3 cells.

Selective estrogen receptor modulator (SERM), inhibiting mammalian PLD (PLD1 and PLD2)

KY-04031 is a PAK4 inhibitor with IC50 of 0.79 uM, a basic building block in designing novel imidazo[4,5-b]pyridine-based PAK4 inhibitors..

RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation.

CA77.1(CA) is a novel chaperone-mediated autophagy (CMA) activator for the treament of Alzheimer’s disease (AD).

Naxillin is the first non-auxin-like molecule that promotes root branching, activates a subset of auxin-induced transcripts, including AUX/IAA, SAUR and PIN families; induces auxin response in the basal meristem; represents a valuable tool to further decipher the molecular networks involved in lateral root branching.

XD2-149 is a napabucasin PROTAC as an effective degrader of the E3 ligase ZFP91 with IC50 of 1 μM and 0.8 μM in pancreatic cancer cell lines, MIA PaCa-2 and BxPC-3, respectively. XD2-149 also reduces the expression of STAT3, pSTAT3, and NQO1 proteins.

MK-8153 is a potent and selective ROMK (potassium channel, Kir1.1) blocker with IC50 of 2.5 nM in rat ROMK, rKir1.1/HEK293 cells. MK-8153 has a longer projected human half-life (~14 h) than MK-7145, which should provide a reduced peak-to-trough exposure ratio and potentially, a smoother, more extended diuretic response.

DFP00173 (DFP-00173) is a potent and selective aquaporin-3 (AQP3) inhibitor, inhibits glycerol permeability in erythrocytes with IC50 of 0.2 uM..

4-Allylcatechol (4-Allylpyrocatechol, Hydroxychavicol) is an intermediate to synthetic safrole.

CDK4 inhibitor compound 12 is a novel inhibitor of CDK4 with the activity 97 μM.

LP-184 is a highly potent novel alkylating, next-generation analog of irofulven. LP-184 is an DNA damage repair (DDR) inhibitor and and shows broad anti-tumor cytotoxicity across a panel of NSCLC derived cell lines.

AZD8154 is a highly potent, inhaled dual PI3Kγ/PI3Kδ inhibitor with pIC50 of 9.1 and 8.4, respectively.

WRX606 is a nonrapalog inhibitor. WRX606 formed a ternary complex with FK506-binding protein-12 (FKBP12) and FKBP−rapamycin-binding (FRB) domain of mTOR, resulting in the allosteric inhibition of mTORC1. WRX606 inhibited the phosphorylation of not only the ribosomal protein S6 kinase 1 (S6K1) but also eIF4E-binding protein-1 (4E-BP1). Hence, WRX606 efficiently suppressed tumor growth in mice without promotion of metastasis. These results suggest that WRX606 is a potent lead compound for developing anticancer drugs discovered by in silico and in cell methods.

EN4, a covalent ligand that targets cysteine 171 (C171) of MYC, is selective for c-MYC over N-MYC and L-MYC. EN4 inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis.

AG-636 is an orally available inhibitor of dihydroorotate dehydrogenase (DHODH) with potential antineoplastic activity.

ACBI1 is a potent and cooperative PROTAC degrader of SMARCA2, SMARCA4 and PBRM1 with DC50 of 6 nM, 11 nM and 32 nM for SMARCA2, SMARCA4 and PBRM1 in MV-4-11 cells, respectively. ACBI1 is composed of a bromodomain ligand, a linker, and the E3 ubiquitin ligase VHL. ACBI1 induces anti-proliferative effects and apoptosis.

ML267 a potent Sfp phosphopantetheinyl transferase (PPTases) inhibitor with an IC50 of 0.29 μM. ML267 also inhibits AcpS-PPTase with an IC50 of 8.1 μM. ML267 possesses specific Gram-positive-targeted bactericidal activities.

Teplinovivint is a Wnt pathway inhibitor.

(S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively).

PI4KA inhibitor-1 is a novel Phosphatidylinositol 4-kinase type IIIα (PI4KA) inhibitor.