High-throughput and high-content screening of large chemical libraries is a proven way to identify novel small molecules that target and modulate disease-associated biological systems and phenotypes. The Australian Cancer Research Foundation (ACRF) Drug Discovery Centre for Childhood Cancer, located within Children’s Cancer Institute Australia at the Lowy Cancer Research Centre in Sydney, was established to provide the infrastructure and know-how for small molecule screening to the cancer research community. The Drug Discovery Centre has been in operation for five years and, in that time, has completed several screening projects in childhood and adult cancer cell-based assays using diversity, known bioactive and targeted chemical compound libraries. The Centre operates on a subsidised fee-for-service basis and provides expertise and assistance in scaling assays for high-throughput and robotic screening, isolating chemical compounds that affect specific cancer cellular activities and providing researchers with small molecule hits to be used in further drug development or as biological tools. In this poster, we outline the different drug discovery services available and highlight actual case studies of successful small- and large-scale screening projects performed within the Centre. It is the goal of this facility to provide the cancer research community with state-of-the-art technology for discovering new therapeutics and tools for better understanding cancer biology.