Enumeration of 166 Billion Organic Small Molecules in the Chemical Universe Database GDB-17

被引:926
作者
Ruddigkeit, Lars [1 ]
van Deursen, Ruud [2 ]
Blum, Lorenz C. [1 ]
Reymond, Jean-Louis [1 ]
机构
[1] Univ Bern, Dept Chem & Biochem, NCCR TransCure, CH-3012 Bern, Switzerland
[2] Ecole Polytech Fed Lausanne, Biomol Screening Facil, NCCR Chem Biol, Sch Life Sci, CH-1015 Lausanne, Switzerland
基金
瑞士国家科学基金会;
关键词
VIRTUAL EXPLORATION; DIVERSITY; DISCOVERY; DESIGN; SPACE; INHIBITORS; TRENDS; ATOMS;
D O I
10.1021/ci300415d
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Drug, molecules consist of a few tens of atoms connected by covalent bonds. Haw many such molecules are possible in total and what is their structure? This question is of pressing interest in: medicinal. chemistry to help solve the problems of drug potency, selectivity, and toxicity and reduce attrition rates by pointing to new molecular series. To better define the unknown chemical space, we have enumerated 166.4 billion molecules of up to 17 atoms of C, N, O, S, and halogens forming the Chemical-universe. database GDB-17, covering a size range containing many drugs and typical for lead compounds. GDB-17 contains Millions of isomers of known drugs,. including analogs: with high, shape : similarity to the parent drug. Compared to known molecules in PubChem, GDB-17 molecules are much richer in nonaromatic hetero- cycles, quaternary centers, and stereoisomers, densely populate the third dimension in shape space and represent many more scaffold types.
引用
收藏
页码:2864 / 2875
页数:12
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