AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, activating Wnt signaling, increases bone mass in rats.

AZD2098 is a potent CC-chemokine receptor 4 (CCR4) inhibitor, used for asthma research.

AZD1981 is a potent, selective CRTh2 (DP2) receptor antagonist with IC50 of 4 nM, showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1

AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1/2.

AZD1152 (barasertib), pro-drug of barasertib-hQPA, is a selective Aurora B kinase inhibitor, AZD1152 inhibited the proliferation various types of human leukemia cells with an IC50 ranging from 3 nM to 40 nM.

AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with Ki of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity against CDK2, CDK5, CDK1 and Erk2.

AZ6102 is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows 5 nM Wnt pathway inhibition in DLD-1 cells.

AZ505 is a potent and highly selective inhibitor of the oncogenic protein SMYD2(IC50=0.12 uM) with potential anticancer activity, >600 fold than SMYD3(IC50>83.3 uM); DOT1L(IC50>83.3 uM);EZH2(IC50>83.3 uM).

AZ3451 is a potent and selective allosteric antagonist of protease-activated receptor 2 (PAR2)

AZ-33 is a inhibitor of LDH-A with an IC50 of 0.5 μM.

AZ3146 is a potent and selective monopolar spindle 1 (Mps1) kinase inhibitor (IC50 = 35 nM); less potent to FAK, JNK1, JNK2, and Kit.

AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM, 8-fold selectivity over mTOR.

Axitinib is a non-selective receptor kinase inhibitor of Flt and Flk proteins. This compound also inhibits VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-β and c-KIT with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM, respectively. Axitinib is studied as an ant

AX-024 is the first-in-class inhibitor of T cell receptor (TCR); AX-024 is an orally available inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation (IC50 value 1 nM).

AWD 131-138(Imepitoin) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.

AVN-944(VX-944) is a selective, noncompetitive inhibitor of the enzyme directed against human IMPDH with Ki of 6-10 nM for IMPDH1/IMPDH2.

AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R (Ki=91 pM).

AVL-292 is a covalent, highly selective, orally active small molecule inhibitor of Btk currently being evaluated in a Phase 1b clinical trial in relapsed.

AUY922 (NVP-AUY922) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Phase 1/2.

Autophinib is a novel potent autophagy inhibitor, inhibiting autophagy induced by starvation or Rapamycin by targeting the lipid kinase VPS34.

Auten-99 is a novel inhibitor of the myotubularin phosphatase Jumpy (also called MTMR14), acrossing the blood-brain barrier and exerting potent neuroprotective effects.

Aurora A inhibitor I is a selective Aurora A inhibitor (Aurora A: IC50=0.0034 μM; Aurora B IC50=3.4 μM), (B/A ratio=1000).

Auristatin E is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAE analog and cytotoxin in Antibody-drug conjugates.

Atovaquone is a medication used to treat or prevent for pneumocystis pneumonia, toxoplasmosis, malaria, and babesia.

Atipamezole(MPV1248) is an alpha-adrenoceptor antagonist with high affinity and selectivity for the alpha 2-receptor.

ATB-346 is a novel hydrogen sulphide-releasing derivative of naproxen with markedly reduced toxicity.

Atazanavir is a HIV protease inhibitor with Ki of 2.66 nM.

AT9283 is a small molecule a multi-targeted inhibitor with of 4, 1.2, 1.1 and approximate 3 nM for Bcr-Abl(T3151), Jak2 and Jak3, aurora A and B, respectively.

AT7867 is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively; little activity outside the AGC kinase family.

AT7519 is a novel multi-CDK inhibitor for CDK1/cyclin B, CDK2/Cyclin A, CDK3/Cyclin E, CDK4/Cyclin D1, CDK5/p35 and CDK6/Cyclin D3 with IC50 of 210 nM, 47 nM, 360 nM, 100 nM, 13 nM and 170 nM, respectively.