Publication Details (including relevant citation information):
Medicinal Chemistry Communications (2011), 2, 977-981
A high throughput chemical screening campaign has led to the identification of 3-aminobenzo[b]thiophene-2-carboxamides as LIMK1 inhibitors. Evolution of bicyclic hits to the tricyclic 4-aminobenzothieno[3,2-d]pyrimidine, using a traditional medicinal chemistry SAR guided approach, resulted in a significant increase in potency. Further elaboration has seen the 7-phenyl-4-aminobenzothieno[3,2-d]pyrimidine emerge as a LIMK1 inhibitor lead candidate.