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. Author manuscript; available in PMC: 2022 Nov 19.
Published in final edited form as: J Med Chem. 2022 Sep 22;65(19):13264–13287. doi: 10.1021/acs.jmedchem.2c01106

Table 4.

Summary and Comparative Analysis of the Biological Activity of Type I (1), Type II (48), and Type III (15) Inhibitors and the Negative Control Compound 26 on LIMK1 and LIMK2 in Thermal Shift Assay (DSF), In Vitro Activity by RapidFire MS, and Cellular Activity by NanoBRET

DSF ΔTm [°C]
 RapidFire MS IC50 [nM]
 NanoBRET IC50 [nM]
compound LIMK1 LIMK2 LIMK1 LIMK2 LIMK1 LIMK2
Type I
1 (LIMKi3)		   6.7 ± 0.3   3.7 ± 0.3 16.6 ± 4 11.6 ± 3 62 ± 19 17 ± 3.9
Type II
48 (TH470)		 17.8 ± 0.4 20.6 ± 4 7 ± 2 20 ± 3 9.8 ± 1.7 13 ± 4.3
Type III
15 (TH257)		   5.6 ± 2.0 12.8 ± 0.1 83.8 ± 14 15.5 ± 2 238 ± 97 91 ± 34
neg. control
26 (TH263)		   1.2 ± 1.0   0.7 ± 0.1 >50,000 >50,000 >25,000 >25,000