AF-353 is a novel, orally bioavailable, highly potent and selective P2X3/P2X2/3 receptor antagonist.

AF38469 is a potent, selective, orally bioavailable Sortilin inhibitor with IC50 of 330 nM, shows no activity against the NTR1 receptor as well as a panel of targets known to bind acidic molecules (δ-Opioid, GPR40, PPARδ, EP1, Angiotensin AT1, Endothelin

AF64394 is a potent, selective GPR3 inverse agonist with pIC50 of 7.3, displays >100-fold selectivity over GPR6 and GPR12.

Afatinib is an irreversible EGFR/HER2 inhibitor with an IC50 of 14 nM for in vitro potency against HER2.

AFN-1252(Debio 1452) is a potent inhibitor of enoyl-acyl carrier protein reductase (FabI), inhibited all clinical isolates of Staphylococcus aureus and Staphylococcus epidermidis at concentrations of ≤0.12 μg/ml.

Afoxolaner is an isoxazoline that inhibits insect and acarine ligand-gated chloride channels, in particular those gated by the neurotransmitter gamma-aminobutyric acid (GABA), blocking pre and post synaptic transfer of chloride ions across cell membranes.

Aftin-4, an amyloid forty-two inducer, activates γ-secretase, promoting the generation of amyloid-β-1-42 (Aβ1-42) from amyloid-β protein precursor.

Afuresertib (GSK2110183) is a potent pan-AKT inhibitor that demonstrated synergy with bortezomib in preclinical models of multiple myeloma (MM).

Afuresertib (GSK2110183) is a potent, orally bioavailable Akt inhibitor with Ki of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.

AG 1406 is a selective inhibitor of the receptor tyrosine kinase VEGF receptor 2 .

AG-120 is a first-in-class, orally available, selective, potent inhibitor of the mutated IDH1 protein.

AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM. It is at least 1000-fold more potent than the benzamides.

AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor with IC50 of 3 nM.

AG-1557 is an ultra-potent inhibitor of epidermal growth factor receptor tyrosine kinase (EGFRK).

AG-17 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 460 µM in the human epidermoid carcinoma cell line A431.

AG-18(RG-50810; Tyrphostin A23) inhibits EGFR with IC50 of 40 μM.

AG-221 is an orally available, selective, potent inhibitor of the mutated IDH2 protein.

AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC50 of 14 nM.

AG-490 (Tyrphostin B42) is an inhibitor of EGFR, ErbB2 and JAK2 with IC50 of 0.1 μM, 13.5 μM, and ~10 μM, respectively.

AG-494 is an inhibitor of epidermal growth factor receptor kinase with an IC50 value of 1 µM in HT-22 cells.

AG-881 is a potent and selective orally available inhibitor of mutated forms of both isocitrate dehydrogenase type 1 (IDH1) in the cytoplasm and type 2 (IDH2).

AG-99 is an inhibitor of EGF receptor kinase with an IC50 value of 10 µM in the human epidermoid carcinoma cell line A431.