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Producing quality clinical candidates less prone to late stage failure is greatly facilitated by better integration of the relevant high throughput functions and the inclusion of ADME/toxicology further upstream in the discovery process. We describe the tasks and their integration in the context of the design, make and test triad.

Producing quality clinical candidates less prone to late stage failure is greatly facilitated by better integration of the relevant high throughput functions and the inclusion of ADME/toxicology further upstream in the discovery process. We describe the tasks and their integration in the context of the design, make and test triad.

We found 8-azidoadenosine 5'-diphosphate to be a phosphoryl acceptor in the enzymatic conversion of 1,3-diphosphoglyceric acid to 3-phosphoglycerate. This has allowed us to synthesize in a single-step procedure carrier-free 8-azidoadenosine 5'-[y-32p]triphosphate, requiring no further purification of the end product. The synthesized 8-azidoadenosine 5'-[?,-32p]triphosphate has been characterized and shown to meet all the criteria for a specific photoreactive ATP analogue.

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