| Autor: |
Guintu C; Genomics Institute of the Novartis Research Foundation, San Diego, California 92121, USA., Kwok M, Hanlon JJ, Spalding TA, Wolff K, Yin H, Kuhen K, Sasher K, Calvin P, Jiang S, Zhou Y, Isbell JJ |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of biomolecular screening [J Biomol Screen] 2006 Dec; Vol. 11 (8), pp. 933-9. Date of Electronic Publication: 2006 Nov 07. |
| DOI: |
10.1177/1087057106294289 |
| Abstrakt: |
Many companies possess a compound collection consisting of purified compounds and of unpurified products from combinatorial libraries. Using commercial and proprietary compounds as examples, this report provides clear examples of the significant impact purification can have on the activity observed for a compound and highlights the need to retest the purified compounds prior to creating structure-activity relationships. Crude mixtures made with commercial compounds led to an increase in the number of false positives in the SXR-GAL4 assay as compared with their pure and purified counterparts. An examination of proprietary compounds in an HIV assay resulted in the purification of 61 active crude synthetic mixtures. Of these 61 compounds, 32 were 5-fold less active and 2 were 5-fold more active after purification. This report details a semiautomated process developed and implemented for cherry-picking, tracking, and selectively purifying compounds found active in high-throughput screening campaigns. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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