T1042

Granisetron hydrochloride (Granisetron HCl) is a serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients.

HT1042 is an inhibitor of the β5i component of the 20S proteasome complex, it is used to aid in the treatment of inflammatory diseases, autoimmune and hematologic malignancies.

AVE5688, an inhibitor of glycogen phosphorylase (GP), has IC50 values of 430 nM and 915 nM, and Kd values of 170 nM and 530 nM for rmGPb and rmGPa, respectively. It is suitable for research on type 2 diabetes.

Avarofloxacin (JNJ-Q2) is a broad-spectrum fluoroquinolone antibacterial drug under development for treating acute bacterial skin and skin structure infections, as well as community-acquired pneumonia.

Avibactam free acid is a potent β-lactamase inhibitor exhibiting covalent and reversible properties, capable of inhibiting TEM-1, P99, and CTX-M-15 at nanomolar concentrations. Avibactam free acid and Ceftazidime may be combined for treating urinary tract infections.

AWZ1066S is a highly specific anti-Wolbachia drug candidate for the short-course treatment of filariasis (EC50: 2.5 nM in cell assay).

AZ-3 is a potent and selective JAK1 inhibitor (IC50: 34 nM).

AZ084 is a potent, selective, allosteric, and orally active CCR8 antagonist (Ki: 0.9 nM) with potential to treat asthma.

AZ12601011 is an orally active, selective and potent TGFBR1 kinase inhibitor.AZ12601011 inhibits the release of inflammatory factors, interleukin (IL)-1β, IL-6 and tumor necrosis factor-α, and inhibits the growth of breast tumors.AZ12601011 directly binds to TGF-βR1 and blocks downstream Smad3 activation, which can be used to prevent renal fibrosis.

AZ505 ditrifluoroacetate is an effective and selective SMYD2 inhibitor (IC50: 0.12 μM).

AZ82 is a selective inhibitor of kinesin-like protein KIFC1 (HSET/KIFC1), with a Ki of 43 nM and an IC50 of 300 nM for KIFC1.

Tizaterkib (AZD-0364) is a potent and selective ERK2 inhibitor.