Table 3.
Binding properties of SPAK and OSR1 binding inhibitors.
Molecule | Chemical structure | Binding target (IC50) | Selectivity for target | Reference |
---|---|---|---|---|
Stock 1S-50699 | ![]() |
SPAK (IC50 = 37,000 nM) | MAPK not inhibited at 200 μM. | [89] |
Stock 2S-26016 | ![]() |
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) | ![]() |
SPAK (IC50 = 40,500 nM) SPAK + MO25 (IC50 = 41,300 nM) |
≥50% inhibition of 6/140 kinases (at 10 μM). | [71] |
HK01 | ![]() |
MO25 (IC50 = 78,000 ± 4000 nM) | MST3 not inhibited at 500 μM. | [90] |