Based on high‐throughput screening and scaffold morphing, inhibitor 56 (also known as Roblitinib or FGF401) was identified as an excellent FGFR4‐targeted RCKI and currently is in Phase‐II clinical trial for treating HCC and other solid tumors characterized by positive FGFR4 and KLB expression. Here, FGFR4 is linked to hepatocellular carcinoma.