Table 4 Inhibitors of Porcupine

CGX1321

1.0 nM

Phase I (NCT03507998): Gastrointestinal tumors;

Phase I (NCT02675946): Solid tumors

[399, 400]

ETC-159

2.9 nM

Phase I (NCT02521844): Advanced solid tumors

[401]

LGK974

0.1 nM

Phase I (NCT01351103): TNBC and other cancers

[16, 63, 398]

GNF-1331

12 nM

Preclinical

[402]

GNF-6231

0.8 nM

Preclinical

[402]

IWP2

27 nM

Preclinical

[384, 403, 404]

IWP-L6

0.5 nM

Preclinical

[405]

IWP-O1

80 pM

Preclinical

[406]

Porcn-IN-1

0.5 ± 0.2 nM

–

[407]

Wnt-C59

74 pM

Preclinical

[398]