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. 2021 Jul 22;64(15):11354–11363. doi: 10.1021/acs.jmedchem.1c00701

Table 1. Notum Activities for 4-(Indolin-1-yl)-4-oxobutanoate Esters.

graphic file with name jm1c00701_0009.jpg

compound R Notum OPTSa IC50 (nM) Notum TCF/LEF EC50 (nM)
1 Me 93 ± 20 530 ± 47
2 H (acid) 3100 ± 920  
3 Et 190 ± 45 300 ± 60
4 CH2CHF2 12 ± 2.8  
5 CH2Ph 64 ± 14  
6 CH(CH3)2 4300 ± 400  
7 C(CH3)3 inactiveb  
a

All values are mean ± s.d. (n = 4), experiments quoted to 2 s.f.

b

<10% I @ 10 μM.