En route, it passes through the areas of Little India, Newton Road, Farrer Road, Singapore Botanic Gardens, Bukit Timah and Bukit Panjang.

"Bukit Timah" in Malay means "tin bearing hill".

The British surrendered to the Japanese at the Old Ford Motor Factory at Upper Bukit Timah Road.

Along the road, major landmarks include Tan Kah Kee MRT station, Anglo-Chinese School (Barker Road), Balmoral Plaza, Coronation Plaza, Hwa Chong Institution, Sixth Avenue MRT station, Kandang Kerbau Women's and Children's Hospital, Kampong Java Park, King Albert Park, Little India MRT station, Hwa Chong International School, Methodist Girls' School, National Junior College, Nanyang Girls' High School, Newton Food Centre, Newton, Singapore Botanic Gardens, Singapore Institute of Management, Tekka Centre, Ngee Ann Polytechnic at the junction of Clementi Road and Upper Bukit Timah Road.

Businesses and organisations located along Bukit Timah Road include: