adaptor-associated kinase 1

LP-935509 is a selective, brain-permeable, small molecule competitive inhibitor of articulin-2-associated kinase 1 (AAK1) with an IC50 of 3.3 nM and a Ki of 0.9 nM. LP-935509 is a potent inhibitor of BIKE (IC50 of 14 nM) and a moderate inhibitor of GAK (IC50 of 320±40 nM).

AAK1-IN-1 (example 123) is an AAK1 (adaptor associated kinase 1) inhibitor with an IC50 of 2.2 nM. AAK1-IN-1 can be used for neurodegenerative diseases research[1]. Adaptor associated kinase 1 (AAK1) is a member of the Arkl/Prkl family of serine/threonine kinases. AAKl mRNA exists in two splice forms termed short and long. The long form predominates and is highly expressed in brain and heart. AAKl is enriched in synaptosomal preparations and is co-localized with endocytic structures in cultured cells. AAKl modulates clatherin coated endocytosis, a process that is important in synaptic vesicle recycling and receptor-mediated endocytosis[1]. [1]. Guanglin Luo, et al. Biaryl kinase inhibitors. WO2015153720A1.

AAK1-IN-9 (Compound 3) is an inhibitor of AAK1 (adaptor associated kinase 1) with an IC50 value of 10.92 nM, and it is applicable in the study of neurodegenerative diseases.

AAK1-IN-10 (Compound 1-2) is an AAK1 inhibitor with significant enzymatic inhibition of AAK1 (IC50: 9.62 nM). Its primary mechanism involves inhibiting adaptor-associated kinase 1 (AAK1) activity. AAK1-IN-10 exhibits minimal cardiotoxicity (IC50 = 13.7 μM) and can be utilized in research for diabetic neuralgia and postherpetic neuralgia.

AAK1-IN-11 is an inhibitor of AAK1 (adaptor associated kinase 1) with an IC50 of 2 nM, and it exhibits antiviral activity.

BMS-911172 is an AAK1 kinase inhibitor with an IC50 value of 35 nM.

AAK1-IN-2 (compound (S)-31) is a potent, selective, and brain-penetrant Adaptor Protein 2-Associated Kinase 1 (AAK1) inhibitor (IC50 = 5.8 nM) used in neuropathic pain research [1].

AAK1-IN-3 is a quinoline analogue that can be used in the research of neuropathic pain. AAK1-IN-3 is a brain-penetrant inhibitor of adaptor protein 2-associated kinase 1 (AAK1) (IC 50 = 11 nM) [1].

AAK1-IN-4 is a potent and specific inhibitor of adaptor protein-2-associated kinase 1 (AAK1), capable of efficiently penetrating the central nervous system and exhibiting oral bioactivity. It has demonstrated a high degree of selectivity with an AAK1 inhibitory concentration (IC50) of 4.6 nM, a Filt dissociation constant (Ki) of 0.9 nM, and a cellular IC50 of 8.6 nM. AAK1-IN-4 holds promise as a valuable tool in the investigation of neuropathic pain [1].

AAK1-IN-5 is a potent and specific inhibitor of adaptor protein-2-associated kinase 1 (AAK1), characterized by its ability to penetrate the central nervous system and its oral bioavailability. It displays high selectivity, with an AAK1 inhibitory potency (IC 50) of 1.2 nM, a binding affinity (K i) of 0.05 nM, and an inhibitory potency against cellular AAK1 activity (cell IC 50) of 0.5 nM. AAK1-IN-5 holds promise for investigating neuropathic pain in scientific research [1].

AAK1-IN-3 TFA is an adaptor protein 2-associated kinase 1 (AAK1) inhibitor (IC50: 11 nM) that crosses the blood-brain barrier and is a quinoline analogue.AAK1-IN-3 has shown potential for research in neuropathic pain.

BMT-046091 is a potent and selective radioligand which inhibits adaptor-associated kinase 1 (AAK1).