Development of the lead-oriented synthesis as a solution to provide large arrays of quality lead generating screening libraries with strictly controlled properties is dependent on access to the novel molecular scaffolds. Such starting points must be small enough to enable significant diversity of the derivatives and, at the same time, must possess molecular properties allowing for wide variations of the substituents within lead-like chemical space.
Express Lead Library is a new product of Enamine that offers unprecedented fast access to the novel lead-like libraries at affordable prices. Such libraries can be synthesized and delivered in only 2-3 weeks. We have carefully selected 3 758 most interesting core building blocks from our stock collection to compose a basis of Express Lead Library. They fall in the following categories:
Bridged
137
Spiro
306
Medium-sized rings
239
Fused saturated rings
152
Fused aromatic & saturated rings
507
Saturated rings
175
Aromatic-saturated rings
1 058
Isolated rings
470
Aromatic rings
247
Monocyclic
467
The core building blocks can be grouped in clusters sharing common or bioisosteric cores. Each such cluster can yield diverse multidimensional screening libraries in just one synthesis step! Express lead library or any part of it can be also provided as SDF so that one can run virtual screening to identify the most promising synthesis candidates. Cherry picking will not influence price. Examples of the core building block clusters are pictured below.
