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

Table 3.

Binding properties of SPAK and OSR1 binding inhibitors.

Molecule Chemical structure Binding target (IC50) Selectivity for target Reference
Stock 1S-50699 graphic file with name 41401_2020_474_Figj_HTML.gif SPAK (IC50 = 37,000 nM) MAPK not inhibited at 200 μM. [89]
Stock 2S-26016 graphic file with name 41401_2020_474_Figk_HTML.gif SPAK (IC50 = 16,000 nM)

MAPK not inhibited at 200 μM.

Non-inhibitory analog of Stock 2S-26016 did not affect SPAK and NCC phosphorylation.

[89]
ZT-1a (allosteric) graphic file with name 41401_2020_474_Figl_HTML.gif

SPAK (IC50 = 40,500 nM)

SPAK + MO25 (IC50 = 41,300 nM)

≥50% inhibition of 6/140 kinases (at 10 μM). [71]
HK01 graphic file with name 41401_2020_474_Figm_HTML.gif MO25 (IC50 = 78,000 ± 4000 nM) MST3 not inhibited at 500 μM. [90]