T6397

Atracurium besylate (51W89) is a non-depolarizing neuromuscular blocking agent with short duration of action. Its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alternate non-depolarizing neuromuscular blocking agents.

Canocapavir (ZM-H1505R) is a novel orally available HBV coat protein modulator with antiviral activity that induces conformational changes in the linker region of the HBV core protein, and can be used for the treatment of hepatitis B virus.

EZH2-IN-11 is a potent inhibitor of E2HZ, demonstrating research potential for various cancer types as shown in numerous studies exploring the oncogenic activity of EZH2.

hCA I-IN-2 (Compound 6d) is a selective inhibitor of human carbonic anhydrase I (hCA I) with inhibition constants (Ki) as follows: 18.8 nM for hCA I, 375.1 nM for hCA II, 1721 nM for hCAIX, and 283.9 nM for hCAXII.

hCAXII-IN-3 (Compound 6o) is a selective inhibitor of human carbonic anhydrase XII (hCAXII) with a Ki of 10.0 nM.

MI-773 is a potent inhibitor of the MDM2-p53 protein interaction (PPI) with a high affinity for MDM2 and a Kd value of 8.2 nM. MI-773 exhibits antitumour effects.

MAT2A-IN-1 is a potent inhibitor of MAT2A, displaying proliferative activity in MTAP-deficient cancer cells. MAT2A is highly expressed in several tumours, including gastric, colon, liver, and pancreatic cancers. MAT2A-IN-1 shows significant potential for cancer research.

AZ13824374 is a potent and selective ATAD2 inhibitor with anti-proliferative effects in breast cancer. pIC50 values for AZ13824374 against ATAD2 in the ATAD2 FRET and ATAD2 NanoBRET assays were 8.2 and 6.2, respectively.

GSK3739936 is a potent inhibitor of HIV-1 allosteric integrase (IC50: 11.1 nM, EC50: 1.7 nM). GSK3739936 is also a weak inhibitor of CYP with an IC50 >24.3 μM. It has good pharmacokinetic properties with rapid absorption, low to moderate clearance and good oral bioavailability.

FAK-IN-2 is a potent, orally active adherens spot kinase (FAK) inhibitor (IC50: 35 nM) that exhibits antitumour effects. FAK-IN-2 covalently inhibits FAK autophosphorylation in a dose-dependent manner and also inhibits tumour cell formation and migration and induces apoptosis.

Ziprasidone (CP-88059) mesylate trihydrate is an orally active 5-HT and dopamine receptor antagonist in rats, showing affinity for D2, 5-HT2A, and 5-HT1A receptors with Ki values of 4.8 nM, 0.42 nM, and 3.4 nM, respectively.