Ontology highlight
ABSTRACT:
SUBMITTER: Babaoglu K
PROVIDER: S-EPMC2655312 | biostudies-literature | 2008 Apr
REPOSITORIES: biostudies-literature
Babaoglu Kerim K Simeonov Anton A Irwin John J JJ Nelson Michael E ME Feng Brian B Thomas Craig J CJ Cancian Laura L Costi M Paola MP Maltby David A DA Jadhav Ajit A Inglese James J Austin Christopher P CP Shoichet Brian K BK
Journal of medicinal chemistry 20080312 8
High-throughput screening (HTS) is widely used in drug discovery. Especially for screens of unbiased libraries, false positives can dominate "hit lists"; their origins are much debated. Here we determine the mechanism of every active hit from a screen of 70,563 unbiased molecules against beta-lactamase using quantitative HTS (qHTS). Of the 1,274 initial inhibitors, 95% were detergent-sensitive and were classified as aggregators. Among the 70 remaining were 25 potent, covalent-acting beta-lactams ...[more]