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. 2020 Jul 28;42(4):508–517. doi: 10.1038/s41401-020-0474-7

Table 2.

Binding properties of SPAK and OSR1 inhibitors.

Molecule Chemical structure Binding target (IC50) Selectivity for target Reference
Stock 1S-14279 (allosteric) graphic file with name 41401_2020_474_Figf_HTML.gif SPAK (IC50 = 260 nM) >50% inhibition in 2/48 kinases (at 10 μM). [81]
Closantel (allosteric) graphic file with name 41401_2020_474_Figg_HTML.gif SPAK (IC50 = 770 nM) >50% inhibition in 6/48 kinases (at 10 μM). [81]
Rafoxanide (allosteric) graphic file with name 41401_2020_474_Figh_HTML.gif

SPAK (T233E) (IC50 = 1303 nM)

OSR1 (T185E) (IC50 = 818 nM)

OSR1 + MO25 (IC50 = 1391 nM)

Not reported.

Likely to be similar to Closantel, due to structural similarity.

 [82]
Verteporfin(allosteric) graphic file with name 41401_2020_474_Figi_HTML.gif

SPAK (T233E) (IC50 = 330 nM)

OSR1 (T185E) (IC50 = 207 nM)

 ≥70% inhibition of 8/140 kinases (at 1 μM). [83]