In current effort, we designed and synthesised novel 3-amino-5-substituted pyrozolopyridine derivatives and assessed their kinase-inhibitory activities against ALK-L1196M gatekeeper mutant as well as against ALK-wt, and their antiproliferative activities on Ba/F3 cells transformed with ALK-wt/ALK-L1196M and on H2228 non-small cell lung cancer cells harbouring EML4-ALK. The gene discussed is EML4; the disease is non-small cell lung carcinoma.