AAK1 inhibitor 1
AAK1 inhibitor 1 (SGC-AAK1-1) is a potent, selective inhibitor of AAK1 and BMP2K/BIKE ((BMP-2 inducible kinase)) that potently targets the ATP-binding site (AAK1 Ki =9.1 nM, BIKE Ki= 17 nM); disaplays excellent kinase selectivity, only three kinases (RIOK1 KD=72 nM, RIOK3 KD=290 nM, and PIP5K1C KD=260 nM) were observed to bind SGC-AAK1-1 within 30-fold of the KD of AAK1 in a KINOMEscan assay; has potency for ectopically expressed full-length AAK1- and BIKE-Nluc fusion proteins (AAK1 IC50=230 nM; BIKE IC50=1.5 uM)in a live cell NanoBRET assay.
BMS-901715 (BMS901715) is a potent, selective adapter protein-2 associated kinase 1 (AAK1) inhibitor.
BMT-090605 (BMT 090605, BMT090605) is a potent, selective adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50 0.6 nM; weakly inhibits BIKE and GAK with IC50 of 45 and 60 nM, respectively.
LP-935509 is a potent, selective and brain-penetrant adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50 of 3.3 nM; inhibited μ2 protein phosphorylation in HEK293 cells overexpressing human AAK1 with IC50 of 2.8 nM; also potent inhibits closely related BIKE and GAK with IC50 of 14 nM and 320 nM, respectively in a panel of 389 kinases; reduces pain response in phase II formalin and reverses fully established pain behavior in vivo.
AAK1 inhibitor 25A
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