T6139

A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.

D18 is an immune modulator that acts as a dual agonist for TLR7/8 (with EC50 values of 24 nM for hTLR7 and 10 nM for hTLR8, respectively). It enhances the expression of PD-L1 through epigenetic regulation, thereby increasing the sensitivity of tumors to PD-1/PD-L1 blockade. Additionally, D18 functions as a cytotoxin for ADC synthesis, specifically for the ADC HE-S2 [1].

Antileishmanial agent-3 (Compound 13) effectively inhibits the growth of *Leishmania major* [1].

NLRP3-IN-10 (ZVN26391) is a potent NLRP3 inhibitor. NLRP3-IN-10 inhibits IL-1β release with an IC50 value of 251.1 nM. NLRP3-IN-10 attenuates ASC speck formation, leading to suppress activation of NLRP3 inflammasome.

IAA65 is a potent and highly selective transient receptor potential ankyrin 1 (TRPA1) inhibitor (IC50 = 4.3 nM). It demonstrates significant analgesic activity in animal models of inflammatory and neuropathic pain by competitively blocking TRPA1-mediated calcium influx in sensory neurons.

Neuraminidase-IN-5 (Compound 5b), a dihydrofurocoumarin derivative, acts as a potent neuraminidase (NA) inhibitor, exhibiting significant inhibition with an IC 50 of 0.02 μM. Given NA's role in influenza pathogenesis, this compound emerges as a promising candidate for anti-influenza drug development [1].

Mt KARI-IN-4 (compound 5c) is a highly effective inhibitor of Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI), with a Ki of 5.48 μM. It also inhibits Mtb H37Rv, displaying a minimum inhibitory concentration (MIC) of 0.78 μM, and exhibits low cytotoxicity, with an IC50 over 72 μg/mL against human embryonic kidney cells (HEK) [1].

TNIK-IN-4, a powerful TNIK inhibitor, exhibits an IC50 value of 0.61 μM. Furthermore, it demonstrates inhibitory effects on the HCT116 cell line, which is representative of colorectal cancer [1].

AChE/BChE-IN-9 (Compound 7a) is a potent, orally active inhibitor of AChE and BChE, with IC50 values of 5.74 μM and 14.05 μM against hAChE and eqBChE, respectively. It also demonstrates effective antioxidant activity (IC50 = 57.35 μM), chelates iron, and modulates amyloid β 1-42 aggregation. Notably, AChE-IN-16 can cross the blood-brain barrier [1].

Chitin Synthase Inhibitor 3 (Compound 2d) is a potent inhibitor of chitin synthase, exhibiting an IC50 value of 0.16 mM and demonstrating antifungal activity with a minimum inhibitory concentration (MIC) of 1 μg/mL against Candida albicans [1].

Z164597606 is a compound that acts as a selective inhibitor of the enzyme Butyrylcholinesterase (BChE), with IC50 values of 1.3 μM and 1.7 μM for equine BChE and human BChE, respectively. Through a π-π stacking interaction, Z164597606 specifically interacts with the amino acid Trp82 of human BChE. This compound has potential applications in Alzheimer's disease research [1] [2].