Intended for healthcare professionals


A revolution in drug discovery

BMJ 2000; 321 doi: (Published 09 September 2000) Cite this as: BMJ 2000;321:581

Combinatorial chemistry still needs logic to drive science forward

  1. Nigel Beeley (, vice president and chief chemical officer,
  2. Abi Berger (, science editor
  1. Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA
  2. BMJ

    Several new drugs now in phase II clinical trials have got there at speed. Gone are the days of laboriously slow organic chemistry. New techniques and a rapidly changing culture surrounding drug development have revolutionised the time it now takes to get drugs from discovery to market. Bristol-Myers Squibb, for example, reported recently that BMS-201038, an inhibitor of microsomal triglyceride transport protein that lowers plasma cholesterol concentrations, is already, after a relatively short period of time, in phase II clinical trials.

    A key component of any drug discovery programme is synthetic organic chemistry, which has analogies with Lego blocks. Chemical building blocks are assembled according to precise rules, creating molecules of increasing complexity. Some of these blocks hold others in position, while others are capable of interacting with a biochemical target (such as the active site of an enzyme or a receptor). Some blocks are there to modify the metabolism of molecules and others modify the overall structure to improve drug delivery. “Combinatorial chemistry” is the process by which millions of molecular constructions can …

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